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

Caroline J Goodacre; Steven M Bromidge; David Clapham; Frank D King; Peter J Lovell; Mike Allen; Lorraine P Campbell; Vicky Holland; Graham J Riley; Kathryn R Starr; Brenda K Trail; Martyn D Wood

doi:10.1016/j.bmcl.2005.08.004

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

Bioorg Med Chem Lett. 2005 Nov 15;15(22):4989-93. doi: 10.1016/j.bmcl.2005.08.004.

Authors

Caroline J Goodacre¹, Steven M Bromidge, David Clapham, Frank D King, Peter J Lovell, Mike Allen, Lorraine P Campbell, Vicky Holland, Graham J Riley, Kathryn R Starr, Brenda K Trail, Martyn D Wood

Affiliation

¹ Psychiatry Centre of Excellence in Drug Discovery, GlaxoSmithkline Pharmaceuticals, Third Avenue, Harlow, Essex CM19 5AW, UK. Caroline_Goodacre@GSK.com

PMID: 16168649
DOI: 10.1016/j.bmcl.2005.08.004

Abstract

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.

MeSH terms

Administration, Oral
Animals
Cell Line
Humans
Imidazolidines / administration & dosage*
Imidazolidines / chemical synthesis
Imidazolidines / chemistry
Imidazolidines / pharmacology*
Molecular Structure
Rats
Receptor, Serotonin, 5-HT2A / metabolism
Receptor, Serotonin, 5-HT2B / metabolism
Receptor, Serotonin, 5-HT2C / metabolism
Sensitivity and Specificity
Serotonin 5-HT2 Receptor Antagonists*
Structure-Activity Relationship
Substrate Specificity

Substances

Imidazolidines
Receptor, Serotonin, 5-HT2A
Receptor, Serotonin, 5-HT2B
Receptor, Serotonin, 5-HT2C
Serotonin 5-HT2 Receptor Antagonists