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 journalArticle

Abstract

(Chemical Equation Presented) Treating neurological conditions: Optimization of a previously identified lead 5-HT2C agonist (left) led to the discovery of a highly selective 5-HT2C agonist (right). Importantly, this compound is a 5-HT2B receptor antagonist. Because of its selective 5-HT2C 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 languageEnglish (US)
Pages (from-to)1221-1225
Number of pages5
JournalChemMedChem
Volume5
Issue number8
DOIs
StatePublished - Aug 2 2010

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Keywords

  • 5-HT
  • CNS
  • Drug discovery
  • Medicinal chemistry
  • Schizophrenia

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

Cite this

Kozikowski, A. P., Cho, S. J., Jensen, N. H., Allen, J. A., Svennebring, A. M., & Roth, B. L. (2010). HTS and rational drug design to generate a class of 5-HT 2C-selective ligands for possible use in schizophrenia. ChemMedChem, 5(8), 1221-1225. https://doi.org/10.1002/cmdc.201000186