161 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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.
University of Siena
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.
University of Caen Normandie
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
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.
Smithkline Beecham Pharmaceuticals
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.
University of Caen Normandie
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
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
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.
University of Siena
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
University of Siena
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
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
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists
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 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
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
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£
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
Knoll Pharmaceuticals
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
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
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 β-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
C5-C6-carbocyclic fused iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
TBA
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
Beijing Tide Pharmaceutical
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
Beijing Tide Pharmaceutical
Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as TrkA kinase inhibitors
Array Biopharma
1-sulfonyl piperidine derivatives as modulators of prokineticin receptors
Takeda Pharmaceutical
Aromatic heterocyclic derivatives and pharmaceutical applications thereof
Sunshine Lake Pharma
Metabotropic glutamate receptor negative allosteric modulators (NAMS) and uses thereof
Sanford-Burnham Medical Research Institute
Design and synthesis of new 2-anilinoquinolines bearing N-methylpicolinamide moiety as potential antiproliferative agents.
Korea Institute of Science and Technology
Indolizinone based derivatives as potential phosphodiesterase 3 (PDE3) inhibitors and a process for the preparation thereof
Council of Scientific & Industrial Research
Pseudodipeptides as MMP inhibitors
French Alternative Energies and Atomic Energy Commission
Kinetics Studies on the Inhibition Mechanism of Pancreatic α-Amylase by Glycoconjugated 1H-1,2,3-Triazoles: A New Class of Inhibitors with Hypoglycemiant Activity.
Yonsei University
Methionine aminopeptidase (type 2) is the common target for angiogenesis inhibitors AGM-1470 and ovalicin.
Massachusetts Institute of Technology
Structure-based virtual screening for novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase and their experimental evaluation.
Northern Kentucky University
Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors.
Cnr
Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome-Coronavirus Papain-Like Protease.
Purdue University
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.
Yale University
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.
Human Biomolecular Research Institute
Structure-based discovery of triphenylmethane derivatives as inhibitors of hepatitis C virus helicase.
National Taiwan University
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
Kochi Medical School
Chalcones: a valid scaffold for monoamine oxidases inhibitors.
Sapienza University of Rome
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.
Universita Del Piemonte Orientale
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Wyeth Research
Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.
Absolute Science
A selective matrix metalloprotease 12 inhibitor for potential treatment of chronic obstructive pulmonary disease (COPD): discovery of (S)-2-(8-(methoxycarbonylamino)dibenzo[b,d]furan-3-sulfonamido)-3-methylbutanoic acid (MMP408).
Wyeth Research
Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.
Universita Di Siena
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
Tanabe Research Laboratories Usa
Carbonic anhydrase inhibitors: the membrane-associated isoform XV is highly inhibited by inorganic anions.
Universita Degli Studi Di Firenze