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169 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.EBI
University Of Belgrade
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.EBI
University Of Illinois At Chicago
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI
The Alexander Shulgin Research Institute
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.EBI
City University Of New York
Therapeutic Potential of 5-HT6 Receptor Agonists.EBI
Universit£
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.EBI
City University Of New York
Discovery of Novel Indazole Derivatives as Highly Potent and Selective Humanß3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects.EBI
Asahi Kasei Pharma
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.EBI
University Of Illinois At Chicago
Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity.EBI
Boehringer Ingelheim (Canada)
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.EBI
Universit£
a2-adrenoceptor antagonists: synthesis, pharmacological evaluation, and molecular modeling investigation of pyridinoguanidine, pyridino-2-aminoimidazoline and their derivatives.EBI
Trinity College
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.EBI
Novartis Pharma
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.EBI
University Of Missouri
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.EBI
Universit£
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.EBI
Novartis Institutes For Biomedical Research
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.EBI
National Institute Of Diabetes And Digestive And Kidney Diseases
Guanidine-baseda2-adrenoceptor ligands: Towards selective antagonist activity.EBI
Trinity College
Identification of a new selective dopamine D4 receptor ligand.EBI
Florida A&M University
2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.EBI
Janssen-Cilag
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.EBI
TBA
Favourable involvement ofa2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement.EBI
University Of Camerino
Might the observeda(2A)-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?EBI
Universit£
Fruitful adrenergica(2C)-agonism/a(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.EBI
Universita` Di Camerino
Rigid analogues of thea2-adrenergic blocker atipamezole: small changes, big consequences.EBI
Pierre Fabre Research Center
Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?EBI
Universita Degli Studi Di Camerino
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.EBI
Universit£
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.EBI
Smithkline Beecham Pharmaceuticals
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2.EBI
Janssen-Cilag
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.EBI
Janssen-Cilag
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.EBI
Janssen Research Foundation
Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.EBI
Savannah State University
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.EBI
Neurosearch Sweden
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).EBI
The University Of Sydney
Methylation of imidazoline related compounds leads to loss ofa2-adrenoceptor affinity. Synthesis and biological evaluation of selective I1 imidazoline receptor ligands.EBI
University Of Strasburg
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.EBI
Amgen
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.EBI
Pfizer
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.EBI
National Institute Of Mental Health
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.EBI
University Of Li£Ge
Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with highs1 receptor affinity.EBI
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.EBI
National Institute Of Mental Health
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.EBI
H. Lundbeck
Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular).EBI
Westfalische Wilhelms-Universitat
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.EBI
Hunter College And The Graduate Center Of The City University Of New York
Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.EBI
Universitat De Barcelona
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.EBI
Tom'S Of Maine
Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists.EBI
Pfizer
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI
Abbott Laboratories
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.EBI
Kyowa Hakko Kogyo
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.EBI
Janssen-Cilag
trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist.EBI
Purdue University
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.EBI
Pfizer
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI
Novartis Institutes For Biomedical Research
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.EBI
Taisho Pharmaceutical
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.EBI
Pfizer
Selective optimization of side activities: another way for drug discovery.EBI
Prestwick Chemical
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.EBI
Alcon Research
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).EBI
Virginia Commonwealth University
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.EBI
Warner-Lambert
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.EBI
National Taiwan University
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.EBI
Allergan
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.EBI
Smithkline Beecham Pharmaceuticals
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.EBI
Synaptic Pharmaceutical
A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.EBI
Ohio State University
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.EBI
Abbott Laboratories
Yohimbine dimers exhibiting binding selectivities for human alpha2a- versus alpha2b-adrenergic receptors.EBI
University Of Tennessee
Design and synthesis of novel dihydropyridine alpha-1a antagonists.EBI
Synaptic Pharmaceutical
Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines.EBI
Medical University Of Gdansk
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.EBI
The University Of Sydney
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.EBI
Wyeth Research
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.EBI
The University Of Sydney
3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for thea(2)-adrenoceptor compared to the imidazoline I(1) receptor.EBI
Medical University Of Gdansk
5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.EBI
Wyeth Research
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI
National Institute Of Mental Health
Spiroindolones, a potent compound class for the treatment of malaria.EBI
Swiss Tropical And Public Health Institute
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.EBI
Purdue University
Synthesis and in vitro binding studies of piperazine-alkyl-naphthamides: impact of homology and sulphonamide/carboxamide bioisosteric replacement on the affinity for 5-HT1A, alpha2A, D4.2, D3 and D2L receptors.EBI
University Of LièGe
Synthesis and in vivo evaluation of [11C]MPTQ: a potential PET tracer for alpha2A-adrenergic receptors.EBI
Columbia University
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).EBI
Siena Biotech
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.EBI
Amgen
5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists.EBI
Wyeth Research
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.EBI
University Of Medicine And Dentistry Of New Jersey-Robert Wood Johnson Medical School And The Informatics Institute Of Umdnj
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.EBI
Arena Pharmaceuticals
Further studies on arylpiperazinyl alkyl pyridazinones: discovery of an exceptionally potent, orally active, antinociceptive agent in thermally induced pain.EBI
Dipartimento Di Scienze Farmaceutiche
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.EBI
Novartis Institutes For Biomedical Research
Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.EBI
Sirtris Pharmaceuticals
The Role of Receptor Binding in Drug DiscoveryEBI
TBA
6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists.EBI
Pfizer
Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.EBI
Pfizer
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.EBI
Institute Of Nuclear Chemistry Johannes Gutenberg-University Mainz
Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential.EBI
Vanderbilt University
Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist.EBI
Pfizer
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.EBI
National Institute Of Mental Health
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.EBI
Merck Research Laboratories
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.EBI
Pfizer
Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.EBI
Università
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.EBI
National Institute Of Mental Health
Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.EBI
Juvantia Pharma
Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists.EBI
Schering-Plough Research Institute
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.EBI
Florida A&M University
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.EBI
Columbia University College Of Physicians And Surgeons
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.EBI
Alcon Research
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.EBI
Columbia University College Of Physicians And Surgeons
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.EBI
Chungbuk National University
Synthesis and biological studies of yohimbine derivatives on human alpha2C-adrenergic receptors.EBI
University Of Tennessee
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.EBI
Taisho Pharmaceutical
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.EBI
Janssen-Cilag
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.EBI
Johnson & Johnson Pharmaceutical Research & Development
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.EBI
University Of Kansas
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.EBI
Merck
Indolebutylamines as selective 5-HT(1A) agonists.EBI
Merck
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety.EBI
Janssen-Cilag
Binding of beta-carbolines at 5-HT(2) serotonin receptors.EBI
Virginia Commonwealth University
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants.EBI
Johnson & Johnson Pharmaceutical Research & Development
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.EBI
Universita Di Camerino
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.EBI
Pharmazeutisches Institut Der UniversitäT Freiburg
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.EBI
Synaptic Pharmaceutical
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.EBI
Merck
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.EBI
The R. W. Johnson Pharmaceutical Research Institute
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.EBI
The R. W. Johnson Pharmaceutical Research Institute
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.EBI
Synaptic Pharmaceutical
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign prEBI
Abbott Laboratories
Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.EBI
Allergan
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.EBI
Allergan
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.EBI
Smithkline Beecham Pharmaceuticals
Design, synthesis, and structure-activity relationships of a new series of alpha-adrenergic agonists: spiro[(1,3-diazacyclopent-1-ene)-5,2'-(1',2',3',4'- tetrahydronaphthalene)].EBI
Institut De Recherches Servier
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.BDB
Yogi Vemana University
Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile.BDB
Broad Institute
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.BDB
Chulabhorn Research Institute
Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues.BDB
Peking University
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University Of Leipzig
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents.BDB
University Of Wisconsin-Madison
Direct Staudinger-Phosphonite Reaction Provides Methylphosphonamidates as Inhibitors of CE4 De-N-acetylases.BDB
University Of Toronto
Organocatalyzed solvent free an efficient novel synthesis of 2,4,5-trisubstituted imidazoles for a-glucosidase inhibition to treat diabetes.BDB
Comsats Institute Of Information Technology