PMID

Data

Article Title

Organization

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

Glaxosmithkline

Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.

Glaxosmithkline

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

Eli Lilly

Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent.

Sungkyunkwan University

Novel multitarget-directed ligands (MTDLs) with acetylcholinesterase (AChE) inhibitory and serotonergic subtype 4 receptor (5-HT4R) agonist activities as potential agents against Alzheimer's disease: the design of donecopride.

Cermn

Discovery and pharmacological profile of new hydrophilic 5-HT(4) receptor antagonists.

University Of Oslo

Synthesis and structure-activity relationship studies in serotonin 5-HT4 receptor ligands based on a benzo[de][2,6]naphthridine scaffold.

Universit£

N-[(1-butyl-4-piperidinyl)methyl]-3,4dihydro-2H-[1,3]oxazino[3,2- a]indole10-carboxamide hydrochloride: the first potent and selective 5-HT4 receptor antagonist amide with oral activity.

Smithkline Beecham Pharmaceuticals

A multivalent approach to the design and discovery of orally efficacious 5-HT4 receptor agonists.

Theravance

Synthesis and preliminary screening of novel indole-3-methanamines as 5-HT4 receptor ligands.

Monash University

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

Glaxosmithkline

First tricyclic oximino derivatives as 5-HT3 ligands.

Universit£

Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).

Smithkline Beecham Pharmaceuticals

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£

Discovery and pharmacological profile of new 1H-indazole-3-carboxamide and 2H-pyrrolo[3,4-c]quinoline derivatives as selective serotonin 4 receptor ligands.

Angelini Santa Palomba Research Center

Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor antagonists.

Suven Life Sciences

Identification of multiple 5-HT4 partial agonist clinical candidates for the treatment of Alzheimer's disease.

Pfizer

Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation.

Theravance

Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749.

Theravance

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

mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I).

Sepracor

An antidepressant that extends lifespan in adult Caenorhabditis elegans.

Howard Hughes Medical Institute

Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers.

Paris-Sud University

5-HT4 receptor ligands: applications and new prospects.

Paris-Sud University

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

Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.

Aventis Pharmaceuticals

N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.

Eli Lilly

Synthesis and structure-activity relationships of a new model of arylpiperazines. 5. Study of the physicochemical influence of the pharmacophore on 5-HT(1a)/alpha(1)-adrenergic receptor affinity: synthesis of a new derivative with mixed 5-HT(1a)/d(2) antagonist properties.

Universidad Complutense

Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.

TBA

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

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).

Siena Biotech

 

5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT_1D receptor agonists

TBA

New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.

Washington University

Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.

Merck Research Laboratories

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

Uppsala University

3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.

Glaxosmithkline

3-arylimino-2-indolones are potent and selective galanin GAL3 receptor antagonists.

Lundbeck Research Usa

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

1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.

Alcon Research

Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies.

Université

Design, synthesis and evaluation of 2-(2-oxoethyl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors.

Hebei University

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

Beijing Normal University

Discovery of G Protein-Biased Antagonists against 5-HT

Korea Institute Of Science And Technology

Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides.

Eli Lilly

Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors.

Umr C8076 (Cnrs)

Discovery of 2,6-Dimethylpiperazines as Allosteric Inhibitors of CPS1.

H3 Biomedicine

Characterization of Specific

Pfizer

New arylpiperazine derivatives as antagonists of the human cloned 5-HT(4) receptor isoforms.

Paris-Sud University

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.

Palack£

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

University Of North Carolina At Chapel Hill

Advancement of multi-target drug discoveries and promising applications in the field of Alzheimer's disease.

Jining Medical University

Novel multi target-directed ligands targeting 5-HT

Normandie Univ

Novel multitarget-directed ligands targeting acetylcholinesterase and ?

Normandie Univ

Synthesis and SAR of Imidazo[1,5-a]pyridine derivatives as 5-HT4 receptor partial agonists for the treatment of cognitive disorders associated with Alzheimer's disease.

Suven Life Sciences

Synthesis and pharmacological properties of a new hydrophilic and orally bioavailable 5-HT4 antagonist.

Drug Discovery Laboratory

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

Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.

Glaxo Research And Development

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

Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT

Suven Life Sciences

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

Northwestern University

Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands.

Suven Life Sciences

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

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

Sanofi-Synthelabo Recherche

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

Janssen Research Foundation

5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.

University Of Oslo

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

Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.

Janssen Research Foundation

SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.

Smithkline Beecham Pharmaceuticals

Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.

Paris-Sud University

(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist.

Smithkline Beecham Pharmaceuticals

SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.

Sanofi Recherche

Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.

Cnrs Upr 9023

Cloning and expression of a human serotonin 5-HT4 receptor cDNA.

Janssen Research Foundation

Pharmacological comparison between [3H]GR 113808 binding sites and functional 5-HT4 receptors in neurons.

Cnrs Upr 9023

Design, synthesis, and biological evaluation of new 5-HT4 receptor agonists: application as amyloid cascade modulators and potential therapeutic utility in Alzheimer's disease.

Cnrs