570 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
Probing the carboxyester side chain in controlled deactivation (-)-d(8)-tetrahydrocannabinols.
Northeastern University
New pyridazinone-4-carboxamides as new cannabinoid receptor type-2 inverse agonists: Synthesis, pharmacological data and molecular docking.
University of Sassari
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor.
Pontificia Universidad Cat£Lica De Chile
Discovery of novel Tetrahydrobenzo[b]thiophene and pyrrole based scaffolds as potent and selective CB2 receptor ligands: The structural elements controlling binding affinity, selectivity and functionality.
German University In Cairo
Tetrahydropyrazolo[4,3-c]pyridine derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists.
Janssen Research and Development
Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists.
Janssen Research and Development
A critical review of both the synthesis approach and the receptor profile of the 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide and analogue derivatives.
Neuroscienze Pharmaness S.C.A R.L.
Discovery of KLS-13019, a Cannabidiol-Derived Neuroprotective Agent, with Improved Potency, Safety, and Permeability.
Kannalife Sciences
Synthesis and pharmacological evaluation of new biphenylic derivatives as CB2 receptor ligands.
Universit£
Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain.
University of Siena
Identification of Novel GPR55 Modulators Using Cell-Impedance-Based Label-Free Technology.
Instituto De Qu£Mica M£Dica
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 7. Synthesis and Pharmacological Evaluation of 4-Quinolone-3-carboxamides and 4-Hydroxy-2-quinolone-3-carboxamides as High Affinity Cannabinoid Receptor 2 (CB2R) Ligands with Improved Aqueous Solubility.
Universit£
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Tricyclic pyrazoles. Part 8. Synthesis, biological evaluation and modelling of tricyclic pyrazole carboxamides as potential CB2 receptor ligands with antagonist/inverse agonist properties.
Universit£
Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists.
Universit£
Pyrazole antagonists of the CB1 receptor with reduced brain penetration.
Rti International
Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists.
Universit£
Synthesis and biological evaluation of (3',5'-dichloro-2,6-dihydroxy-biphenyl-4-yl)-aryl/alkyl-methanone selective CB2 inverse agonist.
University of Tennessee Health Science Center
Combining Mass Spectrometric Metabolic Profiling with Genomic Analysis: A Powerful Approach for Discovering Natural Products from Cyanobacteria.
University of California Berkeley
Distinct Temporal Fingerprint for Cyclic Adenosine Monophosphate (cAMP) Signaling of Indole-2-carboxamides as Allosteric Modulators of the Cannabinoid Receptors.
University of Auckland
Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.
Zhejiang University
Isolation and Pharmacological Evaluation of Minor Cannabinoids from High-Potency Cannabis sativa.
The University of Mississippi
Novel azoles as potent and selective cannabinoid CB2 receptor agonists.
Ipsen Innovation
Cannabinoid type 1 receptor antagonists modulate transport activity of multidrug resistance-associated proteins MRP1, MRP2, MRP3, and MRP4.
Radboud University Nijmegen Medical Centre
New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity.
University of Pisa
Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis.
University of Lille
Selective, nontoxic CB(2) cannabinoid o-quinone with in vivo activity against triple-negative breast cancer.
Instituto De Qu£Mica M£Dica
Design, syntheses, structure-activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor.
Zhejiang University
Synthesis, radiolabeling and evaluation of novel 4-oxo-quinoline derivatives as PET tracers for imaging cannabinoid type 2 receptor.
Institute of Pharmaceutical Sciences
Structure-activity relationships of substituted 1H-indole-2-carboxamides as CB1 receptor allosteric modulators.
Research Triangle Institute
Cannabidiol (CBD) and its analogs: a review of their effects on inflammation.
University of Massachusetts Medical School
Selective CB2 receptor agonists. Part 1: the identification of novel ligands through computer-aided drug design (CADD) approaches.
Boehringer Ingelheim Pharmaceuticals
Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands.
Universit£
Design, synthesis and in vitro evaluation of novel uni- and bivalent ligands for the cannabinoid receptor type 1 with variation of spacer length and structure.
Julius-Maximilians-Universit£T W£Rzburg
One-pot heterogeneous synthesis of¿(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors.
University of Perugia
Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist.
Universit£
Synthesis and biological evaluation of bivalent cannabinoid receptor ligands based on hCB2R selective benzimidazoles reveal unexpected intrinsic properties.
Julius-Maximilians-Universit£T W£Rzburg
Identification of endocannabinoid system-modulating N-alkylamides from Heliopsis helianthoides var. scabra and Lepidium meyenii.
University of Szeged
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.
University of Missouri
Selective CB2 receptor agonists. Part 3: the optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model.
Boehringer Ingelheim Pharmaceuticals
Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds.
Boehringer Ingelheim Pharma
Identification of a highly potent and selective CB2 agonist, RQ-00202730, for the treatment of irritable bowel syndrome.
Raqualia Pharma
Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists.
Arena Pharmaceuticals
Ligand-based virtual screening identifies a family of selective cannabinoid receptor 2 agonists.
University of Oxford
The SAR development of substituted purine derivatives as selective CB2 agonists for the treatment of chronic pain.
Eli Lilly
CB2-selective cannabinoid receptor ligands: synthesis, pharmacological evaluation, and molecular modeling investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides.
Universit£
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.
Novartis Institutes For Biomedical Research
Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1).
Research Triangle Institute
Tricyclic pyrazoles. Part 6. Benzofuro[3,2-c]pyrazole: a versatile architecture for CB2 selective ligands.
Universit£
Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.
Merck Research Laboratories
Ultrapure ajulemic acid has improved CB2 selectivity with reduced CB1 activity.
Corbus Pharmaceuticals
The cannabinoid acids, analogs and endogenous counterparts.
The University of Massachusetts Medical School
Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.
Bristol-Myers Squibb
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
Arena Pharmaceuticals
Evaluation of (Z)-2-((1-benzyl-1H-indol-3-yl)methylene)-quinuclidin-3-one analogues as novel, high affinity ligands for CB1 and CB2 cannabinoid receptors.
University of Arkansas For Medical Sciences
Novel antiobesity agents: synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21.
Instituto De Qu£Mica M£Dica
Highly potent and selective cannabinoid receptor 2 agonists: initial hit optimization of an adamantyl hit series identified from high-through-put screening.
F. Hoffmann-La Roche
Trisubstituted Sulfonamides: a New Chemotype for Development of Potent and Selective CB
University of Pittsburgh
Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55.
University of Bonn
Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation.
University of Pittsburgh
Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists.
Universit£
Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease.
Astrazeneca
Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies.
Ucb Pharma
Design, synthesis, and pharmacological characterization of indol-3-ylacetamides, indol-3-yloxoacetamides, and indol-3-ylcarboxamides: potent and selective CB2 cannabinoid receptor inverse agonists.
Universit£
Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists.
Msd
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Merck Research Laboratories
Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists.
Schering-Plough Research Institute
Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain.
Glaxosmithkline
2-Amino-5-aryl-pyridines as selective CB2 agonists: synthesis and investigation of structure-activity relationships.
Glaxosmithkline
Development of CoMFA and CoMSIA models of affinity and selectivity for indole ligands of cannabinoid CB1 and CB2 receptors.
Universidade Federal Do Rio De Janeiro
Predictive models of Cannabinoid-1 receptor antagonists derived from diverse classes.
Korea Research Institute of Chemical Technology
Synthesis and CB1 receptor activities of novel arachidonyl alcohol derivatives.
University of Kuopio
Structure-activity relationships of 2-arylamido-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide derivatives as cannabinoid receptor agonists and their analgesic action.
Nycomed Pharma
Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents.
Rti International
Diphenyl purine derivatives as peripherally selective cannabinoid receptor 1 antagonists.
Research Triangle Institute
Lead discovery, chemistry optimization, and biological evaluation studies of novel biamide derivatives as CB2 receptor inverse agonists and osteoclast inhibitors.
University of Pittsburgh
7-Alkyl-3-benzylcoumarins: a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists.
University of Bonn
4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis.
University of Lille
7-Oxo-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxamides as selective CB(2) cannabinoid receptor ligands: structural investigations around a novel class of full agonists.
Universit£
2-Arylbenzofuran-based molecules as multipotent Alzheimer's disease modifying agents.
University of Bologna
Scaffold hopping strategy toward original pyrazolines as selective CB2 receptor ligands.
Avenue De L'Universit£
Investigations on the 4-quinolone-3-carboxylic acid motif. 6. Synthesis and pharmacological evaluation of 7-substituted quinolone-3-carboxamide derivatives as high affinity ligands for cannabinoid receptors.
Universit£
JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.
Jenrin Discovery
Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers.
Astrazeneca
Indole-2-carboxamides as allosteric modulators of the cannabinoid CB1 receptor.
Sapienza University of Rome
C3-heteroaroyl cannabinoids as photolabeling ligands for the CB2 cannabinoid receptor.
University of Hawaii At Manoa
Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents.
TBA
Discovery and optimization of novel purines as potent and selective CB2 agonists.
Eli Lilly
N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration.
Astrazeneca
Design and synthesis of cannabinoid receptor 1 antagonists for peripheral selectivity.
Research Triangle Institute
Identification of a Potent and Selective Cannabinoid CB1 Receptor Antagonist from Auxarthron reticulatum.
TBA
Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: an investigation of the 1,8-naphthyridin-2(1H)-one scaffold.
Universit£
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
Shionogi
CB 1/2 dual agonists with 3-carbamoyl 2-pyridone derivatives as antipruritics: reduction of CNS side effects by introducing polar functional groups.
Shionogi
Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain.
Merck Research Laboratories
Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB2 receptor agonists for pain management.
Abbott Laboratories
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.
National Institute of Mental Health
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
1-Bromo-3-(1',1'-dimethylalkyl)-1-deoxy-¿(8)-tetrahydrocannabinols: New selective ligands for the cannabinoid CB(2) receptor.
Clemson University
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Investigations on the 4-quinolone-3-carboxylic acid motif. 3. Synthesis, structure-affinity relationships, and pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ligands.
Universit£
Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern.
Solvay Pharma
Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists.
Solvay Pharma
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.
Solvay Pharma
Synthesis, cannabinoid receptor affinity, molecular modeling studies and in vivo pharmacological evaluation of new substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. 2. Effect of the 3-carboxamide substituent on the affinity and selectivity profile.
Sapienza University of Rome
Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.
Vernalis (R&D)
Rational design, synthesis, and pharmacological properties of new 1,8-naphthyridin-2(1H)-on-3-carboxamide derivatives as highly selective cannabinoid-2 receptor agonists.
Universita Di Pisa
Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists.
University of Bonn
Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.
University of Innsbruck
6-Methoxy-N-alkyl isatin acylhydrazone derivatives as a novel series of potent selective cannabinoid receptor 2 inverse agonists: design, synthesis, and binding mode prediction.
The University of Texas M.D. Anderson Cancer Center
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.
Amgen
Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo.
Universit£
Design and synthesis of a novel series of N-alkyl isatin acylhydrazone derivatives that act as selective cannabinoid receptor 2 agonists for the treatment of neuropathic pain.
The University of Texas M.D. Anderson Cancer Center
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
Tom'S of Maine
New tetrazole-based selective anandamide uptake inhibitors.
Sapienza University of Rome
Synthesis and pharmacology of 1-deoxy analogs of CP-47,497 and CP-55,940.
Clemson University
Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action.
Taisho Pharmaceutical
Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists.
Reen Cross
Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist.
Merck Research Laboratories
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
N-Alkylidenearylcarboxamides as new potent and selective CB(2) cannabinoid receptor agonists with good oral bioavailability.
Taisho Pharmaceutical
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.
Novartis Institutes For Biomedical Research
Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors.
Universit£
1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists.
Universit£
Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors.
Universit£
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.
Merck Research Laboratories
New cannabidiol derivatives: synthesis, binding to cannabinoid receptor, and evaluation of their antiinflammatory activity.
Ben-Gurion University of The Negev
Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists.
Universit£
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.
Universit£
New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies.
Institute of Biomolecular Chemistry
Potent cannabinergic indole analogues as radioiodinatable brain imaging agents for the CB1 cannabinoid receptor.
Northeastern University
Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity.
Solvay Pharma
Bioisosteric replacements of the pyrazole moiety of rimonabant: synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists.
Solvay Pharma
The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications.
Universit£
Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif.
Instituto De Qu£Mica M£Dica
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.
Universidad Complutense
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.
Bristol-Myers Squibb
Exploration of the pharmacophore of 3-alkyl-5-arylimidazolidinediones as new CB(1) cannabinoid receptor ligands and potential antagonists: synthesis, lipophilicity, affinity, and molecular modeling.
Universit£
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.
Universidad Complutense
The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: insights gained from (E)- and (Z)-naphthylidene indenes.
Kennesaw State University
Potent cyano and carboxamido side-chain analogues of 1', 1'-dimethyl-delta8-tetrahydrocannabinol.
Organix
Structural requirements for binding of anandamide-type compounds to the brain cannabinoid receptor.
Hebrew University
3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands.
Universit£
¿-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.
Astrazeneca R&D Montreal
Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity.
Vernalis (R&D)
Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor.
Universit£
1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamide: an effective scaffold for the design of either CB1 or CB2 receptor ligands.
Sapienza University of Rome
Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.
Bristol-Myers Squibb
Asymmetric synthesis and biological evaluation of N-cyclohexyl-4-[1-(2,4-dichlorophenyl)-1-(p-tolyl)methyl]piperazine-1-carboxamide as hCB1 receptor antagonists.
Shanghai Institute of Materia Medica
Conformationally constrained analogs of BAY 59-3074 as novel cannabinoid receptor ligands.
Northeastern University
Towards rational design of cannabinoid receptor 1 (CB1) antagonists for peripheral selectivity.
Rti International
Homology modeling in tandem with 3D-QSAR analyses: a computational approach to depict the agonist binding site of the human CB2 receptor.
Universit£
Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity.
Abbott Healthcare Products
Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa).
Universita` Del Piemonte Orientale
Fluorinated cannabinoid CB2 receptor ligands: synthesis and in vitro binding characteristics of 2-oxoquinoline derivatives.
The University of Texas
Structure-activity relationship studies of novel pyrazole and imidazole carboxamides as cannabinoid-1 (CB1) antagonists.
Dr. Reddy'S Laboratories
Investigations on the 4-quinolone-3-carboxylic acid motif. 4. Identification of new potent and selective ligands for the cannabinoid type 2 receptor with diverse substitution patterns and antihyperalgesic effects in mice.
Universita Degli Studi Di Siena
Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens.
The University of Mississippi
Synthesis, in vitro and in vivo evaluation of fluorine-18 labelled FE-GW405833 as a PET tracer for type 2 cannabinoid receptor imaging.
Imir K.U. Leuven
Tricyclic imidazole antagonists of the Neuropeptide S Receptor.
Merck Research Laboratories
Development of endocannabinoid-based chemical probes for the study of cannabinoid receptors.
Universidad Complutense De Madrid
Indazole derivatives as novel bradykinin B1 receptor antagonists.
Merck Research Laboratories
Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia.
Merck Research Laboratories
Discovery of indole alkaloids with cannabinoid CB1 receptor antagonistic activity.
Chiba University
1,4-Diazepane compounds as potent and selective CB2 agonists: optimization of metabolic stability.
Boehringer Ingelheim Pharmaceuticals
Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy.
Merck Research Laboratories
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.
Universit£
4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series.
Universite£? Lille-Nord De France
Structure-activity relationships of 2,4-diphenyl-1H-imidazole analogs as CB2 receptor agonists for the treatment of chronic pain.
Merck Research Laboratory
Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.
Sapienza University of Rome
Synthesis, binding studies and molecular modeling of novel cannabinoid receptor ligands.
German University In Cairo
Synthesis and biological evaluation of bivalent ligands for the cannabinoid 1 receptor.
Research Triangle Institute
Novel 1',1'-chain substituted hexahydrocannabinols: 9ß-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 (CB1) agonist.
Northeastern University
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Identification and hit-to-lead optimization of a novel class of CB1 antagonists.
Ligand Pharmaceuticals
Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists.
Abbott Healthcare Products
Discovery of 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-1H-pyrazol-3-yl)-5-tert-butyl-1,3,4-thiadiazole (GCC2680) as a potent, selective and orally efficacious cannabinoid-1 receptor antagonist.
Green Cross
Discovery of cannabinoid-1 receptor antagonists by virtual screening.
Korea Research Institute of Chemical Technology
Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant.
Merck Research Laboratories
Rational design of a novel peripherally-restricted, orally active CB(1) cannabinoid antagonist containing a 2,3-diarylpyrrole motif.
Sanofi-Aventis R&D
Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.
Merck Research Laboratories
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Merck Research Laboratories
Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.
Merck Research Laboratories
Radiosynthesis of novel carbon-11-labeled triaryl ligands for cannabinoid-type 2 receptor.
National Institute of Radiological Sciences
Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach.
Chinese Academy of Sciences
Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors.
National Institute of Mental Health
Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand.
Green Cross
Synthesis and biological evaluation of new potential inhibitors of N-acylethanolamine hydrolyzing acid amidase.
University of Salerno
Synthesis and in vitro biological evaluation of carbon-11-labeled quinoline derivatives as new candidate PET radioligands for cannabinoid CB2 receptor imaging.
Indiana University School of Medicine
Synthesis and structure-activity relationship of substitutions at the C-1 position of Delta9-tetrahydrocannabinol.
Amri
Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier.
7Tm Pharma
Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors.
Merck Research Laboratories
Novel thioamide derivatives as neutral CB1 receptor antagonists.
Astrazeneca R & D M£Lndal
Exploring SAR features in diverse library of 4-cyanomethyl-pyrazole-3-carboxamides suitable for further elaborations as CB1 antagonists.
7Tm Pharma
Novel sulfamoyl benzamides as selective CB(2) agonists with improved in vitro metabolic stability.
Adolor
Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism.
Solvay Pharma
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
Abbott Laboratories
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
Glaxosmithkline
Novel pyridine derivatives as potent and selective CB2 cannabinoid receptor agonists.
Adolor
Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: potent, orally-active 1,4-disubstituted imidazoles.
Pfizer
Discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists.
Adolor
Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.
Merck Research Laboratories
Synthesis and pharmacological evaluation of sulfamide-based analogues of anandamide.
Instituto De Qu£Mica M£Dica
Synthesis and SAR of 1,4,5,6-tetrahydropyridazines as potent cannabinoid CB1 receptor antagonists.
Solvay Pharma
Rapid assessment of a novel series of selective CB(2) agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis.
Pfizer
Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas.
Vernalis (R&D)
Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists.
Gedeon Richter
Total synthesis of photoactivatable or fluorescent anandamide probes: novel bioactive compounds with angiogenic activity.
University of Montpellier
Structure activity relationships of tetrahydrocannabinol analogues on human cannabinoid receptors
TBA
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice.
National Health Research Institutes
Hit-to-lead optimization of pyrrolo[1,2-a]quinoxalines as novel cannabinoid type 1 receptor antagonists.
Gedeon Richter
New resorcinol-anandamide"hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo.
Universita Degli Studi Di Siena
Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.
Merck Research Laboratories
Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a CB1 receptor antagonist with in vivo antiobesity effect.
Zydus Research Centre
Synthesis and structure-activity relationship of novel diarylpyrazole imide analogues as CB1 cannabinoid receptor ligands.
Green Cross
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.
Merck Research Laboratories
Oxadiazole-diarylpyrazole 4-carboxamides as cannabinoid CB1 receptor ligands.
Green Cross
Quantitative structure-activity relationship (QSAR) for a series of novel cannabinoid derivatives using descriptors derived from semi-empirical quantum-chemical calculations.
St. Jude Children'S Research Hospital
Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands.
University of Tennessee-Memphis
Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice.
University of California
Synthesis and CB1 cannabinoid receptor affinity of 4-alkoxycarbonyl-1,5-diaryl-1,2,3-triazoles.
University of New Orleans
1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists.
National Central University
Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.
Amgen
New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide.
Martin-Luther-Universitaet
Diarylimidazolyl oxadiazole and thiadiazole derivatives as cannabinoid CB1 receptor antagonists.
Green Cross
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 3: Synthesis and activity of isosteric analogs.
Shionogi
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity.
Green Cross
Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism.
Sapienza University of Rome
Bornyl- and isobornyl-Delta8-tetrahydrocannabinols: a novel class of cannabinergic ligands.
Northeastern University
Discovery and labeling of high-affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors.
National Institute of Mental Health
Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists.
National Health Research Institutes
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.
Amgen
Comparative molecular dynamics simulations of the potent synthetic classical cannabinoid ligand AMG3 in solution and at binding site of the CB1 and CB2 receptors.
The National Hellenic Research Foundation
Exploring the substituent effects on a novel series of C1'-dimethyl-aryl Delta8-tetrahydrocannabinol analogs.
University of Tennessee-Memphis
Conformationally constrained analogues of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716): design, synthesis, computational analysis, and biological evaluations.
Research Triangle Institute
Analogs of JHU75528, a PET ligand for imaging of cerebral cannabinoid receptors (CB1): development of ligands with optimized lipophilicity and binding affinity.
Johns Hopkins University School of Medicine
Rational design, synthesis and biological evaluation of new 1,5-diarylpyrazole derivatives as CB1 receptor antagonists, structurally related to rimonabant.
Università
Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands.
Central Research Institute
Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor.
Monash University (Parkville Campus)
Semiplenamides A-G, fatty acid amides from a Papua New Guinea collection of the marine cyanobacterium Lyngbya semiplena.
Oregon State University
Antimalarial (+)-trans-hexahydrodibenzopyran derivatives from Machaerium multiflorum.
University of Mississippi
Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity.
Evotec (Uk)
Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity.
Northeastern University
Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: synthesis, biological evaluation, and molecular modeling in the homology model.
Zydus Research Centre
New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.
Astrazeneca R&D Montreal
Conformationally constrained analogues of 2-arachidonoylglycerol.
Northeastern University
C1'-cycloalkyl side chain pharmacophore in tetrahydrocannabinols.
National Hellenic Research Foundation
Sulfonamide derivatives as new potent and selective CB2 cannabinoid receptor agonists.
Taisho Pharmaceutical
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.
TBA
Metabolically labile cannabinoid esters: a 'soft drug' approach for the development of cannabinoid-based therapeutic drugs.
Università
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds.
Shionogi
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds.
Shionogi
The application of 3D-QSAR studies for novel cannabinoid ligands substituted at the C1' position of the alkyl side chain on the structural requirements for binding to cannabinoid receptors CB1 and CB2.
The National Hellenic Research Foundation
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.
Pharmaceutical Research Institute
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.
Schering-Plough Research Institute
Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity.
Bayer Healthcare
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
Merck Research Laboratories
Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.
Merck Research Laboratories
Rimonabant-Based Compounds Bearing Hydrophobic Amino Acid Derivatives as Cannabinoid Receptor Subtype 1 Ligands.
Hun Biological Research Centre, Szeged
Synthesis and biological evaluation of several structural analogs of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand.
Teikyo University
Recent advances in chemistry and bioactivity of marine cyanobacteria Moorea species.
Ningbo University
Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives.
Bayer Healthcare
Overview of cannabidiol (CBD) and its analogues: Structures, biological activities, and neuroprotective mechanisms in epilepsy and Alzheimer's disease.
Shaanxi University of Science & Technology
Pyrrole: An insight into recent pharmacological advances with structure activity relationship.
Jamia Hamdard
Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction.
University of North Carolina At Greensboro
Cannabinoid Receptor Subtype 2 (CB2R) in a Multitarget Approach: Perspective of an Innovative Strategy in Cancer and Neurodegeneration.
Cnr-Institute of Crystallography
1-Alkyl-2-aryl-4-(1-naphthoyl)pyrroles: new high affinity ligands for the cannabinoid CB1 and CB2 receptors.
Clemson University
Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
Instituto De Qu£Mica M£Dica
Covalent cannabinoid receptor ligands - structural insight and selectivity challenges.
University of Otago Dunedin
Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery.
The University of Sydney
Reversible Monoacylglycerol Lipase Inhibitors: Discovery of a New Class of Benzylpiperidine Derivatives.
University of Pisa
Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity.
University of Piemonte Orientale
Improved cyclobutyl nabilone analogs as potent CB1 receptor agonists.
National and Kapodistrian University of Athens
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.
Tianjin University
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.
Massachusetts General Hospital
Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands.
University of Pisa
Structure-Based Design, Optimization, and Development of [
Helmholtz-Zentrum Dresden-Rossendorf (Hzdr)
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
Columbia University College of Physicians and Surgeons
Structural modifications of the cannabinoid side chain towards C3-aryl and 1',1'-cycloalkyl-1'-cyano cannabinoids.
National Hellenic Research Foundation
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Merck Research Laboratories
Synthesis and structure-activity relationship of a novel series of aminoalkylindoles with potential for imaging the neuronal cannabinoid receptor by positron emission tomography.
National Institute On Drug Abuse
1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Clemson University
Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors.
Manros Therapeutics & Perha Pharmaceuticals
Substituted 5,5'-diphenyl-2-thioxoimidazolidin-4-one as CB1 cannabinoid receptor ligands: synthesis and pharmacological evaluation.
Université
Synthesis and antitumour evaluation of indole-2-carboxamides against paediatric brain cancer cells.
Curtin University
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.
Merck Research Laboratories
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.
Schering-Plough Research Institute
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.
Merck Research Laboratories
Carbon-silicon switch led to the discovery of novel synthetic cannabinoids with therapeutic effects in a mouse model of multiple sclerosis.
Shanghaitech University
Design, synthesis, and pharmacological profiling of cannabinoid 1 receptor allosteric modulators: Preclinical efficacy of C2-group GAT211 congeners for reducing intraocular pressure.
Northeastern University
Rational Remodeling of Atypical Scaffolds for the Design of Photoswitchable Cannabinoid Receptor Tools.
Shanghaitech University
Synthesis, Biological Evaluation, and Molecular Modeling Studies of 3,4-Diarylpyrazoline Series of Compounds as Potent, Nonbrain Penetrant Antagonists of Cannabinoid-1 (CB
National Institute On Alcohol Abuse and Alcoholism
Development of 3-(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type-1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior.
Research Triangle Institute
Novel Functionalized Cannabinoid Receptor Probes: Development of Exceptionally Potent Agonists.
The Scripps Research Institute
Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists.
Karlsruhe Institute of Technology (Kit)
Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.
Research Triangle Institute
Potent imidazole and triazole CB1 receptor antagonists related to SR141716.
Neurocrine Biosciences
Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists.
Solvay Pharma
Cannabinoid Receptor Agonists for the Potential Treatment of Pain, Neurological Disorders, Fibrotic Diseases, Obesity, and Many More.
Therachem Research Medilab
Synthesis, Molecular Pharmacology, and Structure-Activity Relationships of 3-(Indanoyl)indoles as Selective Cannabinoid Type 2 Receptor Antagonists.
West Virginia University
An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region.
Forbes Norris Als/Mda Research Center
Synthesis and testing of novel phenyl substituted side-chain analogues of classical cannabinoids.
University of Tennessee-Memphis
Arachidonylsulfonyl derivatives as cannabinoid CB1 receptor and fatty acid amide hydrolase inhibitors.
University of California
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
East China Normal University
Pharmacophoric requirements for the cannabinoid side chain. Probing the cannabinoid receptor subsite at C1'.
National Hellenic Research Foundation
Hemisynthesis and preliminary evaluation of novel endocannabinoid analogues.
Umr Cnrs 5074
The discovery of a potent and selective pyrazolo-[2,3-e]-[1,2,4]-triazine cannabinoid type 2 receptor agonist.
The University of Sydney
Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
University of Pisa
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University of Nebraska Medical Center
Impact of Allosteric Modulation in Drug Discovery: Innovation in Emerging Chemical Modalities.
Therapeutics
New cannabinoid receptor antagonists as pharmacological tool.
Instituto De Qu£Mica M£Dica (Csic)
Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity.
National Institute On Drug Abuse
Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.
University of Tennessee Health Science Center
Homologues and isomers of noladin ether, a putative novel endocannabinoid: interaction with rat cannabinoid CB(1) receptors.
Discaff
Novel 1',1'-chain substituted Delta(8)-tetrahydrocannabinols.
National Hellenic Research Foundation
Treatment of Metabolic Disorders with CB-1 Receptor Inverse Agonists.
Therachem Research Medilab (India)
Synthesis and biological evaluation of indole-2-carboxamides bearing photoactivatable functionalities as novel allosteric modulators for the cannabinoid CB1 receptor.
Texas A&M University
The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis.
University of Pisa
Oxygenated metabolites of anandamide and 2-arachidonoylglycerol: conformational analysis and interaction with cannabinoid receptors, membrane transporter, and fatty acid amide hydrolase.
Utrecht University
Conformational memories and the endocannabinoid binding site at the cannabinoid CB1 receptor.
Kennesaw State University
Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB(1) receptor antagonist N-(piperidinyl)- 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716).
Research Triangle Institute
7-Azaindolequinuclidinones (7-AIQD): A novel class of cannabinoid 1 (CB1) and cannabinoid 2 (CB2) receptor ligands.
University of Arkansas For Medical Sciences
Molecular interaction of the antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1- (2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide with the CB1 cannabinoid receptor.
University of South Carolina
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Bayer
Discovery of PEGylated 6-Benzhydryl-4-amino-quinazolines as Peripherally Restricted CB
Janssen Research & Development
Focused structure-activity relationship profiling around the 2-phenylindole scaffold of a cannabinoid type-1 receptor agonist-positive allosteric modulator: site-III aromatic-ring congeners with enhanced activity and solubility.
Northeastern University
Synthesis of the Major Mammalian Metabolites of THCV.
National Research Council of Italy
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.
Ontario Institute For Cancer Research
The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors.
Janssen Research & Development
Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity.
Universit£
Exploration of Alternative Scaffolds for P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Design, Synthesis, and Physicochemical and Pharmacological Profiling of 7-Hydroxy-5-oxopyrazolo[4,3-
University of Siena
Synthesis and biological evaluation of novel amides of polyunsaturated fatty acids with dopamine.
Institute of Bioorganic Chemistry Ras
Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors.
China Pharmaceutical University
Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators.
University of Aberdeen
Peripherally Selective Cannabinoid 1 Receptor (CB1R) Agonists for the Treatment of Neuropathic Pain.
Research Triangle Institute
Synthesis, molecular modeling and SAR study of novel pyrazolo[5,1-f][1,6]naphthyridines as CB
Universit£
Inhibitors of diacylglycerol lipases in neurodegenerative and metabolic disorders.
Leiden University
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
Northeastern University
Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis.
Instituto De Qu£Mica M£Dica
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
University of Pisa
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
Research Triangle Institute
QSAR analysis of Delta(8)-THC analogues: relationship of side-chain conformation to cannabinoid receptor affinity and pharmacological potency.
Research Triangle Institute
Novel conformationally restricted tetracyclic analogs of delta8-tetrahydrocannabinol.
University of Connecticut
Unique analogues of anandamide: arachidonyl ethers and carbamates and norarachidonyl carbamates and ureas.
Organix
Functionalized 6-(piperidin-1-yl)-8,9-diphenyl purines as inverse agonists of the CB1 receptor - SAR efforts towards selectivity and peripheralization.
Rti International
1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
Universit£
Substrate specificity and stereoselectivity of rat brain microsomal anandamide amidohydrolase.
University of Connecticut
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.
University of Connecticut
Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of Cannabinoid 1 Receptor Positive Allosteric Modulators.
Northeastern University
Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability.
University of Connecticut
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
Divalent cannabinoid-1 receptor ligands: A linker attachment point survey of SR141716A for development of high-affinity CB1R molecular probes.
University of Auckland
Identification of CB1 Receptor Allosteric Sites Using Force-Biased MMC Simulated Annealing and Validation by Structure-Activity Relationship Studies.
University of North Carolina At Greensboro
Structure-activity relationships of thiazole and benzothiazole derivatives as selective cannabinoid CB2 agonists with in vivo anti-inflammatory properties.
German University In Cairo
Enantioselective synthesis and pharmacology of 11-hydroxy-(1'S,2'R)-dimethylheptyl-delta 8-THC.
Clemson University
Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
Alma Mater Studiorum-University of Bologna
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors.
Biological Research Centre of The Hungarian Academy of Sciences
Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo.
Julius Maximilian University of W£Rzburg
The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB
University of Aberdeen
Derivation of a pharmacophore model for anandamide using constrained conformational searching and comparative molecular field analysis.
Saint Louis University School of Medicine
Classical/nonclassical hybrid cannabinoids: southern aliphatic chain-functionalized C-6beta methyl, ethyl, and propyl analogues.
University of Hawaii
Preventing Morphine-Seeking Behavior through the Re-Engineering of Vincamine's Biological Activity.
University of Florida
Isolation of a High-Affinity Cannabinoid for the Human CB1 Receptor from a Medicinal
University of Modena and Reggio Emilia
Polycyclic Maleimide-based Scaffold as New Privileged Structure for Navigating the Cannabinoid System Opportunities.
University of Bologna
Pharmacophoric requirements for cannabinoid side chains: multiple bond and C1'-substituted delta 8-tetrahydrocannabinols.
National Hellenic Research Foundation
Importance of the C-1 substituent in classical cannabinoids to CB2 receptor selectivity: synthesis and characterization of a series of O,2-propano-delta 8-tetrahydrocannabinol analogs.
Kennesaw State University
Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase.
Institute of Science
Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.
Universit£
Head group analogs of arachidonylethanolamide, the endogenous cannabinoid ligand.
University of Connecticut
Synthesis and pharmacology of a very potent cannabinoid lacking a phenolic hydroxyl with high affinity for the CB2 receptor.
Clemson University
Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).
Dalhousie University
(Aminoalkyl)indole isothiocyanates as potential electrophilic affinity ligands for the brain cannabinoid receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Mayo Foundation
Benzimidazole: an emerging scaffold for analgesic and anti-inflammatory agents.
Asbasjsm College of Pharmacy
Design, synthesis, biological evaluation, and comparative docking study of 1,2,4-triazolones as CB1 receptor selective antagonists.
Zhejiang University
Functionally Optimized Neuritogenic Farinosone C Analogs: SAR-Study and Investigations on Their Mode of Action.
University of Basel
1,2-Dihydro-2-oxopyridine-3-carboxamides: the C-5 substituent is responsible for functionality switch at CB2 cannabinoid receptor.
Universit£
Synthesis and preliminary evaluation of a new fluorine-18 labelled triazine derivative for PET imaging of cannabinoid CB2 receptor.
Sanofi R&D
Development of fluorinated CB(2) receptor agonists for PET studies.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Selective cannabinoid receptor type 2 (CB2) agonists: optimization of a series of purines leading to the identification of a clinical candidate for the treatment of osteoarthritic pain.
Lilly Research Laboratories
Identification of CB1/CB2 ligands from Zanthoxylum bungeanum.
National Institute On Aging
Synthetic cannabinoid quinones: preparation, in vitro antiproliferative effects and in vivo prostate antitumor activity.
Instituto De Qu£Mica M£Dica
Mastering tricyclic ring systems for desirable functional cannabinoid activity.
The University of Montana
Peripherally selective diphenyl purine antagonist of the CB1 receptor.
Research Triangle Institute
Discovery of novel tetrahydro-pyrazolo [4,3-c] pyridines for the treatment of neuropathic pain: synthesis and neuropharmacology.
Birla Institute of Technology & Science - Pilani
An effective prodrug strategy to selectively enhance ocular exposure of a cannabinoid receptor (CB1/2) agonist.
Novartis Institutes For Biomedical Research
Selective CB2 agonists with anti-pruritic activity: discovery of potent and orally available bicyclic 2-pyridones.
Shionogi
Discovery of 7-oxopyrazolo[1,5-a]pyrimidine-6-carboxamides as potent and selective CB(2) cannabinoid receptor inverse agonists.
Universit£
Aminoalkylindoles: structure-activity relationships of novel cannabinoid mimetics.
Sanofi Research Division
Microwave-assisted synthesis of quinoline, isoquinoline, quinoxaline and quinazoline derivatives as CB2 receptor agonists.
University of Eastern Finland
Combined 3D QSAR and molecular docking studies to reveal novel cannabinoid ligands with optimum binding activity.
The National Hellenic Research Foundation
Alpha-methylated derivatives of 2-arachidonoyl glycerol: synthesis, CB1 receptor activity, and enzymatic stability.
University of Kuopio
3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data.
University of Kuopio
High affinity electrophilic and photoactivatable covalent endocannabinoid probes for the CB1 receptor.
Northeastern University
Volume learning algorithm artificial neural networks for 3D QSAR studies.
Institute of Bioorganic & Petroleum Chemistry
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.
Universit£
Three-dimensional quantitative structure-activity relationship study of the cannabimimetic (aminoalkyl)indoles using comparative molecular field analysis.
Sanofi Research Division
Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.
University of Pisa
6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB
Janssen Research & Development
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.
Pfizer
Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.
University of Otago
Bioactive products from singlet oxygen photooxygenation of cannabinoids.
The University of Mississippi
2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas' disease.
University of Dundee
Synthesis and pharmacological characterization of functionalized 6-piperazin-1-yl-purines as cannabinoid receptor 1 (CB1) inverse agonists.
Rti International
Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor.
Rti International
( R)- N-(1-Methyl-2-hydroxyethyl)-13-( S)-methyl-arachidonamide (AMG315): A Novel Chiral Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes.
Northeastern University
Novel sulfenamides and sulfonamides based on pyridazinone and pyridazine scaffolds as CB
University of Sassari
Polyphenolic Phytochemicals in Cancer Prevention and Therapy: Bioavailability versus Bioefficacy.
University of Valencia
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
University of Pisa
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.
Universit£
Synthesis of oxidative metabolites of CRA13 and their analogs: Identification of CRA13 active metabolites and analogs thereof with selective CB
Kyung Hee University
Structure-activity relationships of imidazothiazinones and analogs as antagonists of the cannabinoid-activated orphan G protein-coupled receptor GPR18.
University of Bonn
Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system.
University of Bern
Discovery of APD371: Identification of a Highly Potent and Selective CB
Arena Pharmaceuticals
Iodine-Promoted Aromatization of p-Menthane-Type Phytocannabinoids.
University of Eastern Piedmont
Developing pyridazine-3-carboxamides to be CB2 agonists: The design, synthesis, structure-activity relationships and docking studies.
Zhejiang University
Design, synthesis and biological evaluation of GPR55 agonists.
University of North Carolina At Greensboro
Biological evaluation of pyridone alkaloids on the endocannabinoid system.
University of Bern
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
Research Triangle Institute
Amidoalkylindoles as Potent and Selective Cannabinoid Type 2 Receptor Agonists with in Vivo Efficacy in a Mouse Model of Multiple Sclerosis.
East China Normal University
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.
Pfizer
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
University of Ferrara
Perspectives of Cannabinoid Type 2 Receptor (CB2R) Ligands in Neurodegenerative Disorders: Structure-Affinity Relationship (SAfiR) and Structure-Activity Relationship (SAR) Studies.
Universit£
Structure-Activity Relationships and Computational Investigations into the Development of Potent and Balanced Dual-Acting Butyrylcholinesterase Inhibitors and Human Cannabinoid Receptor 2 Ligands with Pro-Cognitive in Vivo Profiles.
Julius Maximilian University of W£Rzburg
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Pfizer
Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists.
Leiden University
Synthesis and binding study of certain 6-arylalkanamides as molecular probes for cannabinoid receptor subtypes.
Cairo University
Molecular basis of cannabinoid CB1 receptor coupling to the G protein heterotrimer Gaiß¿: identification of key CB1 contacts with the C-terminal helix a5 of Gai.
North Carolina Central University
Functionalization of ß-Caryophyllene Generates Novel Polypharmacology in the Endocannabinoid System.
University of Bern
Solid phase synthesis of 1,5-diarylpyrazole-4-carboxamides: discovery of antagonists of the CB-1 receptor.
Bristol-Myers Squibb Research and Development
Identification of novel cannabinoid CB1 receptor antagonists by using virtual screening with a pharmacophore model.
Cns Biological Research
Benzodioxoles: novel cannabinoid-1 receptor inverse agonists for the treatment of obesity.
F. Hoffmann-La Roche
Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.
Wyeth Research
Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.
Mcgill University
Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential.
University of Piemonte Orientale
3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novel cannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects.
Bayer Healthcare
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.
Sanofi-Synthelabo Recherche
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.
Case Western Reserve University
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.
Case Western Reserve University
Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) as a potent cannabinoid receptor agonist with neuroprotective properties.
Bayer
A structure/activity relationship study on arvanil, an endocannabinoid and vanilloid hybrid.
Istituto Di Chimica Biomolecolare
Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.
Novartis Pharma
Evidence for a new G protein-coupled cannabinoid receptor in mouse brain.
Virginia Commonwealth University
In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor.
Japan Tobacco
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.
Abbott Laboratories
Cannabinoid agonist signal transduction in rat brain: comparison of cannabinoid agonists in receptor binding, G-protein activation, and adenylyl cyclase inhibition.
Wake Forest University
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
Sanofi Recherche
Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities.
Virginia Commonwealth University
Synthesis and pharmacological evaluation of analogs of indole-based cannabimimetic agents.
UniversitÀ
Mechanisms of Osteoclastogenesis Inhibition by a Novel Class of Biphenyl-Type Cannabinoid CB(2) Receptor Inverse Agonists.
University of Bern
Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.
Astrazeneca
Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.
Acadia Pharmaceuticals
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.
Universita Del Piemonte Orientale
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.
Pfizer
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
Pfizer
Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity.
Abbott Laboratories