Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents.
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.
Dosa
Peter I
PI
Arena Pharmaceuticals Inc., 6166 Nancy Ridge Drive, San Diego, CA 92121, United States. pidosa@umn.edu
Strah-Pleynet
Sonja
S
Jayakumar
Honnappa
H
Casper
Martin
M
Decaire
Marc
M
Xiong
Yifeng
Y
Lehmann
Juerg
J
Choi
Karoline
K
Elwell
Katie
K
Wong
Amy
A
Webb
Robert R
RR
Adams
John W
JW
Ramirez
Juan
J
Richman
Jeremy G
JG
Thomsen
William
W
Semple
Graeme
G
Teegarden
Bradley R
BR
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*
D010975:Platelet Aggregation Inhibitors; D011720:Pyrazoles; D044402:Receptor, Serotonin, 5-HT2A; D058826:Serotonin 5-HT2 Receptor Agonists; C031280:pyrazole; D014508:Urea