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81 articles for thisTarget

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

Article Title
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.EBI
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.EBI
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.EBI
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.EBI
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.EBI
Discovery and pharmacological profile of new hydrophilic 5-HT(4) receptor antagonists.EBI
University of Oslo
Synthesis and structure-activity relationship studies in serotonin 5-HT4 receptor ligands based on a benzo[de][2,6]naphthridine scaffold.EBI
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.EBI
Smithkline Beecham Pharmaceuticals
A multivalent approach to the design and discovery of orally efficacious 5-HT4 receptor agonists.EBI
Synthesis and preliminary screening of novel indole-3-methanamines as 5-HT4 receptor ligands.EBI
Monash University
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.EBI
First tricyclic oximino derivatives as 5-HT3 ligands.EBI
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).EBI
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.EBI
Discovery and pharmacological profile of new 1H-indazole-3-carboxamide and 2H-pyrrolo[3,4-c]quinoline derivatives as selective serotonin 4 receptor ligands.EBI
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.EBI
Suven Life Sciences
Identification of multiple 5-HT4 partial agonist clinical candidates for the treatment of Alzheimer's disease.EBI
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.EBI
Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749.EBI
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
mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I).EBI
An antidepressant that extends lifespan in adult Caenorhabditis elegans.EBI
Howard Hughes Medical Institute
Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers.EBI
Paris-Sud University
5-HT4 receptor ligands: applications and new prospects.EBI
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.EBI
Alcon Research
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.EBI
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.EBI
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.EBI
Universidad Complutense
Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.EBI
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.EBI
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.EBI
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).EBI
Siena Biotech
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonistsEBI
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.EBI
Washington University
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.EBI
Merck Research Laboratories
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.EBI
Uppsala University
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI
3-arylimino-2-indolones are potent and selective galanin GAL3 receptor antagonists.EBI
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.EBI
Predix Pharmaceuticals
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.EBI
Alcon Research
Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies.EBI
Design, synthesis and evaluation of 2-(2-oxoethyl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors.EBI
Hebei University
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.EBI
Beijing Normal University
Discovery of G Protein-Biased Antagonists against 5-HTEBI
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.EBI
Eli Lilly
Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors.EBI
Umr C8076 (Cnrs)
New arylpiperazine derivatives as antagonists of the human cloned 5-HT(4) receptor isoforms.EBI
Paris-Sud University
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.EBI
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine DEBI
University of North Carolina At Chapel Hill
Advancement of multi-target drug discoveries and promising applications in the field of Alzheimer's disease.EBI
Jining Medical University
Novel multi target-directed ligands targeting 5-HTEBI
Normandie Univ
Novel multitarget-directed ligands targeting acetylcholinesterase and ?EBI
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.EBI
Suven Life Sciences
Synthesis and pharmacological properties of a new hydrophilic and orally bioavailable 5-HT4 antagonist.EBI
Drug Discovery Laboratory
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI
Drug Discovery Laboratory
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.EBI
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.EBI
Glaxo Research and Development
Discovery of ?-Arrestin Biased Ligands of 5-HTEBI
Korea Institute of Science and Technology
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products.EBI
University of The Philippines
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HTEBI
Suven Life Sciences
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.EBI
Northwestern University
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
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University of Leipzig
Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation.BDB
Cedars-Sinai Research Institute
Synthesis and activity of quinolinylmethyl P1' alpha-sulfone piperidine hydroxamate inhibitors of TACE.BDB
Wyeth Research