Pharmacological profile of neuroleptics at human monoamine transporters

Masahiko Tatsumi, Karen Jansen, Randy D. Blakely, Elliott Richelson

Research output: Contribution to journalArticle

95 Scopus citations

Abstract

Using radioligand binding techniques, we determined the equilibrium dissociation constants (K(D)) for 37 neuroleptics and one metabolite of a neuroleptic (haloperidol metabolite) for the human serotonin, norepinephrine, and dopamine transporters with [3H]imipramine, [3H]nisoxetine, and [3H]WIN35428, respectively. Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM). At the human dopamine transporter, only pimozide (K(D)=69±3) ziprasidone (K(D)=76±5) had notable potency. These data may be useful in predicting therapeutic and adverse effects, including drug interactions of neuroleptics. Copyright (C) 1999 Elsevier Science B.V.

Original languageEnglish (US)
Pages (from-to)277-283
Number of pages7
JournalEuropean Journal of Pharmacology
Volume368
Issue number2-3
DOIs
StatePublished - Mar 5 1999

Keywords

  • 5-HT (5-hydroxy-hyptamine, serotonin), human
  • Dopamine transporter, human
  • Neuroleptic
  • Norepinephrine transporter, human
  • Radioligand binding assay

ASJC Scopus subject areas

  • Pharmacology

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