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 Allen, Andreas M. Svennebring, Bryan L. Roth

Research output: Contribution to journalArticle

20 Citations (Scopus)

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
Externally publishedYes

Fingerprint

Serotonin 5-HT2 Receptor Agonists
Drug Design
Serotonin
Schizophrenia
Receptor, Serotonin, 5-HT2B
Receptor, Serotonin, 5-HT2C
Ligands
Serotonin 5-HT2 Receptor Antagonists
Phencyclidine
Serotonin Receptor Agonists
Pharmaceutical Preparations

Keywords

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

ASJC Scopus subject areas

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

Cite this

HTS and rational drug design to generate a class of 5-HT 2C-selective ligands for possible use in schizophrenia. / Kozikowski, Alan P.; Cho, Sung Jin; Jensen, Niels H.; Allen, John; Svennebring, Andreas M.; Roth, Bryan L.

In: ChemMedChem, Vol. 5, No. 8, 02.08.2010, p. 1221-1225.

Research output: Contribution to journalArticle

Kozikowski, Alan P. ; Cho, Sung Jin ; Jensen, Niels H. ; Allen, John ; Svennebring, Andreas M. ; Roth, Bryan L. / HTS and rational drug design to generate a class of 5-HT 2C-selective ligands for possible use in schizophrenia. In: ChemMedChem. 2010 ; Vol. 5, No. 8. pp. 1221-1225.
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