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5-HT3 receptor blocking properties of the antiparkinsonian agent, talipexole.

Authors
  • Nishio, H
  • Kohno, Y
  • Fujii, A
  • Negishi, Y
  • Inoue, A
  • Nakata, Y
Type
Published Article
Journal
General Pharmacology The Vascular System
Publisher
Elsevier
Publication Date
Jul 01, 1996
Volume
27
Issue
5
Pages
779–785
Identifiers
PMID: 8842679
Source
Medline
License
Unknown

Abstract

1. Talipexole showed moderate displacement activity of 3H-GR 65630 binding to 5-HT3 receptors in both rat cortical and intestinal membrane fractions with Ki values of 0.35 microM and 0.22 microM, respectively. 2. Bromocriptine failed to displace the binding activity in either experimental system even at a concentration of 10 microM. 3. Both talipexole and tropisetron were found to significantly inhibit 5-HT3 receptor-mediated effects of 5-HT in isolated guinea-pig ileum or atrium; however, the effect of talipexole was weaker than that of tropisetron. 4. Bromocriptine, in contrast, had no antagonistic effects on 5-HT3 receptor-mediated activity in guinea-pig ileum or atrium. 5. It was concluded that talipexole might act as an antagonist on 5-HT3 receptors in both brain and intestinal tissues.

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