Effect of two non tricyclic antidepressant drugs on [14C]5-hydroxytryptamine uptake by rat platelets

M. Wielosz, A. Dall'Olio, G. De Gaetano, S. Garattini

Research output: Contribution to journalArticle

Abstract

The uptake of 14C-5-HT by rat blood platelets was examined in vitro in experimental conditions which allowed measurement of the initial velocity and excluded other passive processes across the cell membrane. In these conditions, the effect of two non tricyclic antidepressant drugs (Lilly 110140 and trazodone) was investigated. Lilly 110140 was as active as chlorimipramine and several times more active than imipramine as an inhibitor of 14C-5-HT uptake. Like chlorimipramine, Lilly 110140 appeared to be either a non-competitive or an uncompetitive inhibitor, according to the concentration of drug used. Trazodone also inhibited 14C-5-HT uptake by platelets but to a lesser extent than chlorimipramine, imipramine or Lilly 110140. m-Chlorophenylpiperazine, a possible metabolite of trazodone, was about 3 times more potent an inhibitor than the parent molecule. Both compounds acted noncompetitively. Compared with published data on the effect of Lilly 110140 and trazodone on brain 5-HT, the present results support the suggestion that rat platelets are a useful pharmacological model of serotoninergic nerve endings.

Original languageEnglish
Pages (from-to)546-549
Number of pages4
JournalJournal of Pharmacy and Pharmacology
Volume29
Issue number9
Publication statusPublished - 1977

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Tricyclic Antidepressive Agents
Fluoxetine
Trazodone
Serotonin
Blood Platelets
Clomipramine
Imipramine
Nerve Endings
Serotonin Uptake Inhibitors
Cell Membrane
Pharmacology
Brain
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Pharmacology

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Effect of two non tricyclic antidepressant drugs on [14C]5-hydroxytryptamine uptake by rat platelets. / Wielosz, M.; Dall'Olio, A.; De Gaetano, G.; Garattini, S.

In: Journal of Pharmacy and Pharmacology, Vol. 29, No. 9, 1977, p. 546-549.

Research output: Contribution to journalArticle

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