Pharmacological profile of neuroleptics at human monoamine transporters

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

Research output: Contribution to journalArticle

95 Citations (Scopus)

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

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Antipsychotic Agents
Pharmacology
Norepinephrine Plasma Membrane Transport Proteins
Serotonin Plasma Membrane Transport Proteins
Dopamine Plasma Membrane Transport Proteins
nisoxetine
Chlorpromazine
Triflupromazine
Chlorprothixene
Promazine
Pimozide
Imipramine
Therapeutic Uses
Haloperidol
Drug Interactions
ziprasidone

Keywords

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

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Pharmacological profile of neuroleptics at human monoamine transporters. / Tatsumi, Masahiko; Jansen, Karen; Blakely, Randy D.; Richelson, Elliott.

In: European Journal of Pharmacology, Vol. 368, No. 2-3, 05.03.1999, p. 277-283.

Research output: Contribution to journalArticle

Tatsumi, Masahiko ; Jansen, Karen ; Blakely, Randy D. ; Richelson, Elliott. / Pharmacological profile of neuroleptics at human monoamine transporters. In: European Journal of Pharmacology. 1999 ; Vol. 368, No. 2-3. pp. 277-283.
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