title: Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents.
abstract: Potent 5-HT(2A) inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in selective compounds that proved effective in modulating 5HT-induced amplification of ADP-stimulated human platelet aggregation.
authors: Arena Pharmaceuticals Inc., 6166 Nancy Ridge Drive, San Diego, CA 92121, United States. pidosa@umn.edu
authors: Peter I
authors: PI
authors: Dosa
authors: Sonja
authors: S
authors: Strah-Pleynet
authors: Honnappa
authors: H
authors: Jayakumar
authors: Martin
authors: M
authors: Casper
authors: Marc
authors: M
authors: Decaire
authors: Yifeng
authors: Y
authors: Xiong
authors: Juerg
authors: J
authors: Lehmann
authors: Karoline
authors: K
authors: Choi
authors: Katie
authors: K
authors: Elwell
authors: Amy
authors: A
authors: Wong
authors: Robert R
authors: RR
authors: Webb
authors: John W
authors: JW
authors: Adams
authors: Juan
authors: J
authors: Ramirez
authors: Jeremy G
authors: JG
authors: Richman
authors: William
authors: W
authors: Thomsen
authors: Graeme
authors: G
authors: Semple
authors: Bradley R
authors: BR
authors: Teegarden
mesh_terms: D006801:Humans; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D058826:Serotonin 5-HT2 Receptor Agonists; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000494:pharmacology*
chemical_list: D010975:Platelet Aggregation Inhibitors; D011720:Pyrazoles; D044402:Receptor, Serotonin, 5-HT2A; D058826:Serotonin 5-HT2 Receptor Agonists; C031280:pyrazole; D014508:Urea