PMID

Data

Article Title

Organization

New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.

Meiji Seika Kaisha

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£

Synthesis and biological evaluation of positron emission tomography radiotracers targeting serotonin 4 receptors in brain: [18F]MNI-698 and [18F]MNI-699.

Molecular Neuroimaging

Design of fluorinated 5-HT(4)R antagonists: influence of the basicity and lipophilicity toward the 5-HT(4)R binding affinities.

University of Southampton

Acidic biphenyl derivatives: synthesis and biological activity of a new series of potent 5-HT(4) receptor antagonists.

University of Oslo

Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.

Theravance

Structure-activity relationship of 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole analogues as 5-HT(6) receptor agonists.

Neurosearch Sweden

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

(1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 receptor antagonist derived from metoclopramide.

Smithkline Beecham Pharmaceuticals

Synthesis and characterization of a iodine-125-labeled pyrrolo[1,2-a]thieno[3,2-e]pyrazine and evaluation as a potential 5-HT4R SPECT tracer.

Universit£

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

 

Quaternised renzapride as a potent and selective 5-HT4 receptor agonist

TBA

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 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

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

Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.

European Research Centre For Drug Discovery and Development (Natsyndrugs)

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

Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.

Pfizer

Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.

Pfizer

Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.

Dainippon Pharmaceutical

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

Benzimidazole derivatives. 2. Synthesis and structure-activity relationships of new azabicyclic benzimidazole-4-carboxylic acid derivatives with affinity for serotoninergic 5-HT(3) receptors.

Universidad Complutense

2,3-Dihydro-2-oxo-1H-benzimidazole-1-carboxamides with selective affinity for the 5-HT(4) receptor: synthesis and structure-affinity and structure-activity relationships of a new series of partial agonist and antagonist derivatives.

Faes

New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.

Cnrs-Biocis

Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.

Universit£

Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.

Universit£

Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT(3) ligands.

Universidad De Alcal£

 

Serotoninergic 5-HT3 and 5-HT4 receptor activities of dihydrobenzofuran carboxylic acid derivatives

TBA

 

Novel benzimidazole-4-carboxylic acid derivatives as potent and selective 5-HT3 receptor ligands

TBA

 

Synthesis and pharmacological activity of a macrocyclic benzamide

TBA

 

New aza(nor)adamantanes are agonists at the newly identified serotonin 5-HT4 receptor and antagonists at the 5-HT3 receptor

TBA

New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage.

Universidad Complutense De Madrid

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

Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors.

TBA

 

Serotonin 5-HT₄ agonist activity of a series of meso-azanoradamantane benzamides

TBA

 

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

TBA

 

Design of a potent 5-HT₄ receptor agonist with nanomolar affinity

TBA

Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.

European Research Centre For Drug Discovery and Development (Natsyndrugs)

Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.

Université

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

Novel sigma receptor ligands: synthesis and biological profile.

University of Catania

Novel thienocycloalkylpyridazinones as useful scaffolds for acetylcholinesterase inhibition and serotonin 5-HT

University of Sassari

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

Lundbeck Research Usa

Discovery and Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT

Suven Life Sciences

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

2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.

Carlsson Research

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

Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.

Merck

Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.

Uppsala University

Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.

Pfizer

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)

Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist.

Universidad Complutense

New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization.

Université

Design, synthesis, and pharmacological evaluation of multitarget-directed ligands with both serotonergic subtype 4 receptor (5-HT4R) partial agonist and 5-HT6R antagonist activities, as potential treatment of Alzheimer's disease.

Normandie Universit£

Benzimidazole derivatives. 3. 3D-QSAR/CoMFA model and computational simulation for the recognition of 5-HT(4) receptor antagonists.

Universidad Complutense

Novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides as potent colonic prokinetic agents.

Dainippon Pharmaceutical

3-D-QSAR/CoMFA and recognition models of benzimidazole derivatives at the 5-HT(4) receptor.

Universidad Complutense

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

Arylcarbamate derivatives of 1-piperidineethanol as potent ligands for 5-HT4 receptors.

Cnrs-Biocis

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

Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.

Solvay Duphar

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

2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.

Meiji Seika Kaisha

Tetrahydrobenzindoles: selective antagonists of the 5-HT7 receptor.

Meiji Seika Kaisha

New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.

Faes

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

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

Institut De Recherches Servier

Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder.

Eli Lilly

Tetrahydrothienopyridylbutyl-tetrahydrobenzindoles: new selective ligands of the 5-HT(7) receptor.

Meiji Seika Kaisha

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

Sanofi-Synthelabo Recherche

Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.

Eli Lilly

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

Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.

Smithkline Beecham Pharmaceuticals

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

Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.

Smithkline Beecham Pharmaceuticals

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

[3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.

Roche Bioscience

SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.

Smithkline Beecham Pharmaceuticals

BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats.

Smithkline Beecham Pharmaceuticals

Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.

SynthÉLabo Recherche

Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.

Cnrs Upr 9023

Peripheral 5-HT4 receptors.

Roche Bioscience

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

Cnrs Upr 9023

[3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.

Synaptic Pharmaceutical

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

Glaxo Research and Development

Novel discriminatory ligands for 5-HT2B receptors.

Smithkline Beecham Pharmaceuticals

Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety.

Smithkline Beecham Pharmaceuticals

BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex.

Boehringer Ingelheim Italia

Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.

Vrije Universiteit

Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo.

Syntex Discovery Research

Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain.

Glaxo Group Research

Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.

Synaptic Pharmaceutical

Molecular biology of 5-HT receptors.

University of Alberta

The 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants.

Synaptic Pharmaceutical

RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist.

Syntex Discovery Research

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