HTS and rational drug design to generate a class of 5-HT 2C-selective ligands for possible use in schizophrenia

Alan P. Kozikowski; Sung Jin Cho; Niels H. Jensen; John A. Allen; Andreas M. Svennebring; Bryan L. Roth

doi:10.1002/cmdc.201000186

HTS and rational drug design to generate a class of 5-HT _2C-selective ligands for possible use in schizophrenia

Alan P. Kozikowski, Sung Jin Cho, Niels H. Jensen, John A. Allen, Andreas M. Svennebring, Bryan L. Roth

Research output: Contribution to journal › Article › peer-review

20 Scopus citations

Abstract

(Chemical Equation Presented) Treating neurological conditions: Optimization of a previously identified lead 5-HT_2C agonist (left) led to the discovery of a highly selective 5-HT_2C agonist (right). Importantly, this compound is a 5-HT_2B receptor antagonist. Because of its selective 5-HT_2C receptor activity, the compound was further evaluated in the phencyclidine model of disrupted prepulse inhibition, and found to exhibit normalizing effects comparable to those shown by the 5-HT _2C agonist vabicaserin, a drug currently in phase II clinical studies for schizophrenia.

Original language	English (US)
Pages (from-to)	1221-1225
Number of pages	5
Journal	ChemMedChem
Volume	5
Issue number	8
DOIs	https://doi.org/10.1002/cmdc.201000186
State	Published - Aug 2 2010
Externally published	Yes

Keywords

5-HT
CNS
Drug discovery
Medicinal chemistry
Schizophrenia

ASJC Scopus subject areas

Drug Discovery
General Pharmacology, Toxicology and Pharmaceutics
Molecular Medicine
Biochemistry
Pharmacology
Organic Chemistry

Access to Document

10.1002/cmdc.201000186

Cite this

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AU - Svennebring, Andreas M.

AU - Roth, Bryan L.

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