A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists

Caroline J. Goodacre,Steven Mark Bromidge,David E. Clapham,Frank D. King,Peter J. Lovell,Michael J. Allen,Lorraine Campbell,Vicky Holland,Graham J. Riley,Kathryn R. Starr,Brenda Trail,Martyn D. Wood

A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists

2005

Caroline J. Goodacre
Steven Mark Bromidge
David E. Clapham
Frank D. King
Peter J. Lovell
Michael J. Allen
Lorraine Campbell
Vicky Holland
Graham J. Riley
Kathryn R. Starr
Brenda Trail
Martyn D. Wood

Abstract Bisaryl cyclic ureas have been identified as high affinity 5-HT 2C receptor antagonists with selectivity over 5-HT 2A and 5-HT 2B . Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT 2C function in rodents.

Keywords:

5-HT2C receptor
Organic chemistry
5-HT receptor
SB-243213
Biochemistry
Inverse agonist
Stereochemistry
Receptor
Chemistry
Oral administration
Chemical synthesis
Antagonist

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