437 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
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 LLC
Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists.
Janssen Research and Development LLC
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.
Synthesis and pharmacological evaluation of new biphenylic derivatives as CB2 receptor ligands.
Universit£ di Pisa
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
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket.
Abbott Healthcare Products BV
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£ degli Studi di Siena
Tricyclic pyrazoles. Part 8. Synthesis, biological evaluation and modelling of tricyclic pyrazole carboxamides as potential CB2 receptor ligands with antagonist/inverse agonist properties.
Universit£ degli Studi di Sassari
Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists.
Universit£ di Ferrara
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£ degli Studi di Sassari
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
Discovery of a high affinity and selective pyridine analog as a potential positron emission tomography imaging agent for cannabinoid type 2 receptor.
Institute of Pharmaceutical Sciences
Novel azoles as potent and selective cannabinoid CB2 receptor agonists.
Ipsen Innovation
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
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 Inc
Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands.
Universit£ di Pisa
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£ degli Studi di Siena
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
trans-Caryophyllene is a natural agonistic ligand for peroxisome proliferator-activated receptor-a.
Korea University
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 Inc
Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds.
Boehringer Ingelheim Pharma GmbH & Co. KG
Identification of a highly potent and selective CB2 agonist, RQ-00202730, for the treatment of irritable bowel syndrome.
RaQualia Pharma Inc
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 and Company
CB2-selective cannabinoid receptor ligands: synthesis, pharmacological evaluation, and molecular modeling investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides.
Universit£ di Pisa
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£ di Sassari
Ultrapure ajulemic acid has improved CB2 selectivity with reduced CB1 activity.
Corbus Pharmaceuticals, Inc.
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
Design, synthesis, and binding mode prediction of 2-pyridone-based selective CB2 receptor agonists.
Shionogi Pharmaceutical Research Center
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 Inc
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£ di Ferrara
Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease.
AstraZeneca
Synthesis and SAR studies of 2-oxoquinoline derivatives as CB2 receptor inverse agonists.
University of Kuopio
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£ degli Studi di Siena
Discovery and optimization of 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives as a novel class of selective cannabinoid CB2 receptor agonists.
Merck Research Laboratories
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
Synthesis of quinolinyl and isoquinolinyl phenyl ketones as novel agonists for the cannabinoid CB2 receptor.
Helsinki University of Technology
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
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 Pvt. Ltd
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£ di Ferrara
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£ degli Studi di Siena
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
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 and Company
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
Discovery of S-444823, a potent CB1/CB2 dual agonist as an antipruritic agent.
Shionogi & Co., Ltd
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£ di Pisa
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
Shionogi & Co., Ltd
CB 1/2 dual agonists with 3-carbamoyl 2-pyridone derivatives as antipruritics: reduction of CNS side effects by introducing polar functional groups.
Shionogi & Co., Ltd
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
1-Bromo-3-(1',1'-dimethylalkyl)-1-deoxy-¿(8)-tetrahydrocannabinols: New selective ligands for the cannabinoid CB(2) receptor.
Clemson University
Synthesis and biodistribution of [11C]A-836339, a new potential radioligand for PET imaging of cannabinoid type 2 receptors (CB2).
Johns Hopkins Medical Institutions
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£ degli Studi di Siena
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) Ltd
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 Inc
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£ degli Studi di Siena
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
The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.
Pfizer Inc
New tetrazole-based selective anandamide uptake inhibitors.
Sapienza University of Rome
5-Sulfonyl-benzimidazoles as selective CB2 agonists.
Johnson & Johnson Pharmaceutical Research & Development
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 Co., Ltd
Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists.
reen Cross Corporation
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.
Universit£ di Pisa
N-Alkylidenearylcarboxamides as new potent and selective CB(2) cannabinoid receptor agonists with good oral bioavailability.
Taisho Pharmaceutical Co., Ltd
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£ degli Studi di Siena
Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors.
Universit£ degli Studi di Siena
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
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.
Universit£ de Lille 2
New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies.
Institute of Biomolecular Chemistry
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£ Catholique de Louvain
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 Co.
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
¿-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) Ltd
Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor.
Universit£ degli Studi di Siena
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 Co.
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
Design and evaluation of a novel fluorescent CB2 ligand as probe for receptor visualization in immune cells.
University of Montana
Homology modeling in tandem with 3D-QSAR analyses: a computational approach to depict the agonist binding site of the human CB2 receptor.
Universit£ di Genova
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 Ltd
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
Aryl 1,4-diazepane compounds as potent and selective CB2 agonists: optimization of drug-like properties and target independent parameters.
Boehringer Ingelheim Pharmaceuticals Inc
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
Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists.
Merck & Co. Inc
Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia.
Merck Research Laboratories
1,4-Diazepane compounds as potent and selective CB2 agonists: optimization of metabolic stability.
Boehringer Ingelheim Pharmaceuticals Inc
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£ degli Studi di Siena
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
Expansion of SAR studies on triaryl bis sulfone cannabinoid CB2 receptor ligands.
Merck Research Laboratories
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
Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists.
Abbott Healthcare Products BV
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 Corporation
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 Corporation
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
Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors.
Merck Research Laboratories
Novel sulfamoyl benzamides as selective CB(2) agonists with improved in vitro metabolic stability.
Adolor Corporation
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 Corporation
Discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists.
Adolor Corporation
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 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 Inc
Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas.
Vernalis (R&D) Ltd
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
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
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 Corporation
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
1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists.
National Central University
CB2 selective sulfamoyl benzamides: optimization of the amide functionality.
Adolor Corporation
Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.
Amgen Inc
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 Corporation
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 & Co., Ltd
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity.
Green Cross Corporation
Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism.
Sapienza University of Rome
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 Inc
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
Rational design, synthesis and biological evaluation of new 1,5-diarylpyrazole derivatives as CB1 receptor antagonists, structurally related to rimonabant.
Università di Genova
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)
Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity.
Evotec (UK) Ltd
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
Pharmacomodulations around the 4-oxo-1,4-dihydroquinoline-3-carboxamides, a class of potent CB2-selective cannabinoid receptor ligands: consequences in receptor affinity and functionality.
Université de Lille 2
New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.
AstraZeneca R&D Montreal
Sulfonamide derivatives as new potent and selective CB2 cannabinoid receptor agonists.
Taisho Pharmaceutical Co., Ltd
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 di Pisa
Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring.
Schering-Plough Research Institute
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds.
Shionogi & Co., Ltd
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 & Co., Ltd
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
Biaryl cannabinoid mimetics--synthesis and structure-activity relationship.
Adolor Corporation
Self-assembling cannabinomimetics: supramolecular structures of N-alkyl amides.
Department of Chemistry and Applied Biosciences
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.
GlaxoSmithKline
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
Synthesis and biological evaluation of several structural analogs of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand.
Teikyo University
Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives.
Bayer HealthCare
1-Alkyl-2-aryl-4-(1-naphthoyl)pyrroles: new high affinity ligands for the cannabinoid CB1 and CB2 receptors.
Clemson University
Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity.
University of Piemonte Orientale
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
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Merck Research Laboratories
Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.
Schering-Plough Research Institute
1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Clemson University
Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.
University of Nottingham
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
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
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
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, LLC
Synthesis, Molecular Pharmacology, and Structure-Activity Relationships of 3-(Indanoyl)indoles as Selective Cannabinoid Type 2 Receptor Antagonists.
West Virginia University
Variously substituted 2-oxopyridine derivatives: Extending the structure-activity relationships for allosteric modulation of the cannabinoid CB2 receptor.
University of Pisa
Synthesis and testing of novel phenyl substituted side-chain analogues of classical cannabinoids.
University of Tennessee-Memphis
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
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
New cannabinoid receptor antagonists as pharmacological tool.
Instituto de Qu£mica M£dica (CSIC)
Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.
University of Tennessee Health Science Center
Treatment of Metabolic Disorders with CB-1 Receptor Inverse Agonists.
Therachem Research Medilab (India) Pvt. Ltd.
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
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
A perspective review on fatty acid amide hydrolase (FAAH) inhibitors as potential therapeutic agents.
Assam University (A Central University)
Discovery of PEGylated 6-Benzhydryl-4-amino-quinazolines as Peripherally Restricted CB
Janssen Research & Development
Synthesis of the Major Mammalian Metabolites of THCV.
National Research Council of Italy
The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors.
Janssen Research & Development, L.L.C.
Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity.
Universit£ degli Studi di Siena
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
Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors.
China Pharmaceutical University
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£ degli Studi di Sassari
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
Medicinal properties of terpenes found in Cannabis sativa and Humulus lupulus.
Univerisity of Eastern Finland (UEF)
Functionalized 6-(piperidin-1-yl)-8,9-diphenyl purines as inverse agonists of the CB1 receptor - SAR efforts towards selectivity and peripheralization.
RTI International
Structure-activity relationships of thiazole and benzothiazole derivatives as selective cannabinoid CB2 agonists with in vivo anti-inflammatory properties.
German University in Cairo
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
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
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
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£ degli Studi di Siena
Synthesis and pharmacology of a very potent cannabinoid lacking a phenolic hydroxyl with high affinity for the CB2 receptor.
Clemson University
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
1,2-Dihydro-2-oxopyridine-3-carboxamides: the C-5 substituent is responsible for functionality switch at CB2 cannabinoid receptor.
Universit£ di Pisa
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
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide (SR144528).
University of Texas-Pan American
3-Carboxamido-5-aryl-isoxazoles as new CB2 agonists for the treatment of colitis.
Universit£ Lille Nord de France
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 Pharmaceutical Research Center
Discovery of 7-oxopyrazolo[1,5-a]pyrimidine-6-carboxamides as potent and selective CB(2) cannabinoid receptor inverse agonists.
Universit£ di Ferrara
Design, synthesis, and biological evaluation of aminoalkylindole derivatives as cannabinoid receptor ligands with potential for treatment of alcohol abuse.
The University of Kansas
Microwave-assisted synthesis of quinoline, isoquinoline, quinoxaline and quinazoline derivatives as CB2 receptor agonists.
University of Eastern Finland
Virtual screening of novel CB2 ligands using a comparative model of the human cannabinoid CB2 receptor.
University of Kuopio
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.
Universit£ di Catania
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
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
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
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
University of Pisa
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 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£ degli Studi di Bari Aldo Moro
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
Discovery of S-217622, a Non-Covalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19
Shionogi Pharmaceutical Research Center
Carbonic anhydrase inhibitors. Phenols incorporating 2- or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae ß-carbonic anhydrase.
Ataturk University
Inhibition of the Flavin-Dependent Monooxygenase Siderophore A (SidA) Blocks Siderophore Biosynthesis and Aspergillus fumigatus Growth.
Virginia Tech
Capture-Tag-Release: A Strategy for Small Molecule Labeling of Native Enzymes.
Fairfield University
2-Prenylated m-dimethoxybenzenes as potent inhibitors of 15-lipo-oxygenase: inhibitory mechanism and SAR studies.
Ferdowsi University of Mashhad
Synthesis, anti-inflammatory, analgesic, 5-lipoxygenase (5-LOX) inhibition activities, and molecular docking study of 7-substituted coumarin derivatives.
Nirma University
A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition.
Jawaharlal Nehru Centre for Advanced Scientific Research
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.
Yogi Vemana University
Development of 2-(Substituted Benzylamino)-4-Methyl-1, 3-Thiazole-5-Carboxylic Acid Derivatives as Xanthine Oxidase Inhibitors and Free Radical Scavengers.
Jamia Hamdard
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.
University of Leipzig
The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.
Mayo Clinic
Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Torrey Pines Institute for Molecular Studies
A novel competitive class of α-glucosidase inhibitors: (E)-1-phenyl-3-(4-styrylphenyl)urea derivatives.
Gyeongsang National University
Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety.
SmithKline Beecham Pharmaceuticals Ltd
The C-terminal domain of the mGluR1 metabotropic glutamate receptor affects sensitivity to agonists.
CNS Research
Properties of the VIP-PACAP type II receptor stably expressed in CHO cells.
Université Libre de Bruxelles
Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties.
Novo Nordisk A/S
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.
Merck Research Laboratories
A 2.13 A structure of E. coli dihydrofolate reductase bound to a novel competitive inhibitor reveals a new binding surface involving the M20 loop region.
University of Prince Edward Island
Discovery and optimization of nonpeptide HIV-1 protease inhibitors.
Parke-Davis Pharmaceutical Research
Identification of novel fragment compounds targeted against the pY pocket of v-Src SH2 by computational and NMR screening and thermodynamic evaluation.
University College London
The development of cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors.
Merck Research Laboratories