Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group

Paul R. Carlier, M. M C Lo, P. C K Lo, Elliott Richelson, Masahiko Tatsumi, Ian J. Reynolds, Terre A. Sharma

Research output: Contribution to journalArticle

50 Scopus citations

Abstract

A series of gamma-amino alcohols were synthesized and screened for reuptake inhibition and noncompetitive NMDA antagonism. Compound (±)-3f simultaneously and potently inhibits reuptake of 5-HT, NE, and DA, representing a potential wide-spectrum reuptake inhibitor antidepressant. In addition, comparative rat and human studies uncovered a species-selective DA reuptake inhibitor (±)-2e, K(D)(hDAT)/K(D)(rDAT) = 97.

Original languageEnglish (US)
Pages (from-to)487-492
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume8
Issue number5
DOIs
StatePublished - Mar 3 1998

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ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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