A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.
Bisaryl cyclic ureas have been identified as high affinity 5-HT2C receptor antagonists with selectivity over 5-HT2A and 5-HT2B. Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function in rodents.
Goodacre
Caroline J
CJ
Psychiatry Centre of Excellence in Drug Discovery, GlaxoSmithkline Pharmaceuticals, Third Avenue, Harlow, Essex CM19 5AW, UK. Caroline_Goodacre@GSK.com
Bromidge
Steven M
SM
Clapham
David
D
King
Frank D
FD
Lovell
Peter J
PJ
Allen
Mike
M
Campbell
Lorraine P
LP
Holland
Vicky
V
Riley
Graham J
GJ
Starr
Kathryn R
KR
Trail
Brenda K
BK
Wood
Martyn D
MD
D000284:Administration, Oral; D000818:Animals; D002460:Cell Line; D006801:Humans; D048289:Imidazolidines / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D051381:Rats; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D044403:Receptor, Serotonin, 5-HT2B / Q000378:metabolism; D044405:Receptor, Serotonin, 5-HT2C / Q000378:metabolism; D012680:Sensitivity and Specificity; D058830:Serotonin 5-HT2 Receptor Antagonists; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D048289:Imidazolidines; D044402:Receptor, Serotonin, 5-HT2A; D044403:Receptor, Serotonin, 5-HT2B; D044405:Receptor, Serotonin, 5-HT2C; D058830:Serotonin 5-HT2 Receptor Antagonists