PMID

Data

Article Title

Organization

Synthesis and alpha 2-adrenoceptor effects of substituted catecholimidazoline and catecholimidazole analogues in human platelets.

Ohio State University

Structure-activity relationships in potentially hallucinogenic N,N-dialkyltryptamines substituted in the benzene moiety.

TBA

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

Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket.

Abbott Healthcare Products

Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1 F receptor agonists: Evolution from bicyclic to monocyclic cores.

Eli Lilly

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

Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.

Wyeth Research

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

Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.

Glaxosmithkline

Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.

Theravance

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

Beijing Normal University

Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists.

Eli Lilly

Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT

Sunshine Lake Pharma

Substituted furo[3,2-b]pyridines: novel bioisosteres of 5-HT 1F receptor agonists.

Eli Lilly

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

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

Glaxosmithkline

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

Merck Sharp & Dohme Research Laboratories

Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.

Glaxosmithkline

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

Merck Sharp & Dohme Research Laboratories

Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.

Merck Sharp and Dohme Research Laboratories

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

Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.

Glaxowellcome

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

Northwestern University

Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.

Tehran University of Medical Sciences

Structure and Inhibition of Microbiome ß-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity.

University of North Carolina At Chapel Hill