ChemMedChem

Cover image for Vol. 12 Issue 8

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 77/255 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

June 15, 2010

VIP: HTS and Rational Drug Design to Generate a Class of 5-HT2C-Selective Ligands for Possible Use in Schizophrenia

VIP: HTS and Rational Drug Design to Generate a Class of 5-HT2C-Selective Ligands for Possible Use in SchizophreniaAlan P. Kozikowski,* Sung Jin Cho, Niels H. Jensen, John A. Allen, Andreas M. Svennebring, and Bryan L. Roth

The 5-HT2C receptor is distributed widely in the central nervous system (CNS), and 5-HT2C agonists have shown efficacy in preclinical models of depression, obesity, addiction, and psychosis. Targeting 5-HT2C would be a promising way to address CNS disorders; however, 5-HT2C is homologous to the two other receptor family members, 5-HT2A and 5-HT2B, and so it is crucial that 5-HT2C agonists have minimal or no activity toward these subtypes.

In an effort to improve specificity, Kozikowski et al. carried out stepwise structural modifications to existing 5-HT2C agonists, and identified a series of compounds with marked improvements: potency toward 5-HT2C on par with reference compounds, but with much greater specificity, and an improved pharmacokinetic profile.

Received April 30, 2010; published online June 10, 2010, DOI: 10.1002/cmdc.201000186.

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