PMID

Data

Article Title

Organization

Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.

The University Of Newcastle

SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.

Glaxosmithkline

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

Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.

Eli Lilly

Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.

University Of Kansas

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

Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome.

National Institute Of Biological Sciences, Beijing

Novel N-acyl-carbazole derivatives as 5-HT7R antagonists.

Yonsei University

Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.

The Alexander Shulgin Research Institute

Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.

City University Of New York

Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.

Yonsei University

Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.

Merck Sharp & Dohme Research Laboratories

Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.

Glaxosmithkline

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).

The University Of Sydney

Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.

H. Lundbeck

Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers.

Universit£

Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.

National Institute Of Biological Sciences

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.

National Institute Of Mental Health

Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.

University Of Namur

Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.

National Institute Of Mental Health

Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.

Aska Pharmaceutical

Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.

Hunter College And The Graduate Center Of The City University Of New York

High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.

Purdue University

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories

Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.

F. Hoffmann-La Roche

Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.

F. Hoffmann-La Roche

2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.

Universit£

A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.

Alcon Research

Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).

Virginia Commonwealth University

Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).

Purdue University

From hit to lead. Analyzing structure-profile relationships.

Universities Of Lille

(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.

Virginia Commonwealth University

CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.

University Of South Florida

Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.

Bristol-Myers Squibb

Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.

National Institute Of Mental Health

A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.

Università

Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.

University Of Medicine And Dentistry Of New Jersey-Robert Wood Johnson Medical School And The Informatics Institute Of Umdnj

 

Derivatives of 2-arylcyclopropylamine: Synthesis and interactions with 5-HT_1A receptors.

TBA

 

Synthesis and biological activity of C-5 modified derivatives of (+)-AJ76 and (+)-UH232: Increased dopamine D₃ receptor preference and improved pharmacokinetic properties

TBA

Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.

Institute Of Nuclear Chemistry Johannes Gutenberg-University Mainz

Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.

Uppsala University

Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.

Ucb Pharma

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.

National Institute Of Mental Health

An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.

Predix Pharmaceuticals

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.

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.

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.

Columbia University College Of Physicians And Surgeons

Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.

F. Hoffmann-La Roche

Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.

Abbott

Discovery of Highly Potent Serotonin 5-HT

Northwestern University

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.

Beijing Normal University

Structure-Based Design of a Chemical Probe Set for the 5-HT

University Of California

Discovery of G Protein-Biased Ligands against 5-HT

Korea Institute Of Science And Technology

Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT

Jagiellonian University Medical College

Pharmacological Analysis of the Anti-inflammatory and Antiallodynic Effects of Zinagrandinolide E from

Universidad Nacional Aut£Noma De M£Xico

Discovery of G Protein-Biased Antagonists against 5-HT

Korea Institute Of Science And Technology

Binding of beta-carbolines at 5-HT(2) serotonin receptors.

Virginia Commonwealth University

Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors.

Virginia Commonwealth University

Structure-Activity Relationship of Heterocyclic P2Y

National Institute Of Diabetes And Digestive And Kidney Diseases

Identification of a novel series of selective 5-HT7 receptor antagonists.

Glaxosmithkline

Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.

Universita Di Camerino

N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.

Merck Sharp & Dohme Research Laboratories

Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.

Columbia University College Of Physicians And Surgeons

Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge

University Of Mississippi

2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.

Virginia Commonwealth University

3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.

Merck Sharp & Dohme Research Laboratories

Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D

National Institute Of Neurological Disorders And Stroke

Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D

University Of North Carolina At Chapel Hill

Design and in Vivo Characterization of A

Medical College Of Wisconsin

3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT

University Of Minnesota Twin Cities

Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.

Drug Discovery Laboratory

Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.

Glaxosmithkline

Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.

Glaxosmithkline

Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.

Texas Tech University Health Sciences Center

Discovery of ?-Arrestin Biased Ligands of 5-HT

Korea Institute Of Science And Technology

Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products.

University Of The Philippines

Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.

University Of Texas At Austin

Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.

Phenex Pharmaceuticals

Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.

Northwestern University

Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.

Case Western Reserve University

WAY-100635 is a potent dopamine D4 receptor agonist.

Purdue University

Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.

Case Western Reserve University

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

S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole.

Institut De Recherches Servier

Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist.

Yamanouchi Pharmaceutical

Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.

Case Western Reserve University

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

Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.

Case Western Reserve University

SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties.

Sanofi-Synthelabo Recherche

In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.

WestfÄLische Wilhelms-UniversitÄ

The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.

Case Western Reserve University

The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.

Janssen Research Foundation

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

A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).

Smithkline Beecham Pharmaceuticals

RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.

Roche Bioscience

Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.

Sri International

GR127935: a potent and selective 5-HT1D receptor antagonist.

Glaxo Research And Development

Expression of functional mouse 5-HT5A serotonin receptor in the methylotrophic yeast Pichia pastoris: pharmacological characterization and localization.

Max-Planck-Institut

Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization.

Cnrs

Molecular biology of 5-HT receptors.

University Of Alberta

Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain.

The Scripps Research Institute

The mouse 5HT5 receptor reveals a remarkable heterogeneity within the 5HT1D receptor family.

Cnrs