PK 11195, an antagonist of peripheral type benzodiazepine receptors, modulates Bay K8644 sensitive but not beta- or H2-receptor sensitive voltage operated calcium channels in the guinea pig heart.

Abstract:

:In a partially depolarized guinea pig papillary muscle preparation, BAY K8644 stimulated voltage-operated calcium channels, promoting slow action potentials; this effect was dose-dependent over a concentration range of 3 X 10(-7) M to 3 X 10(-6) M. Isoproterenol and histamine also induced slow action potentials by stimulating beta or H2 receptors, respectively. PK 11195, the antagonist of peripheral type benzodiazepine receptors, inhibited the effect of BAY K8644, but not those of histamine or isoproterenol. Moreover, PK 11195 "dose-dependently" antagonized the ability of RO5-4864 to inhibit the slow action potentials elicited by barium chloride. Thus, in the heart, PK 11195, an antagonist of peripheral type benzodiazepine receptors, can modulate voltage-operated calcium channels when they are activated directly, but not when they are activated by stimulation of neurotransmitter receptors.

journal_name

Life Sci

journal_title

Life sciences

authors

Mestre M,Carriot T,Néliat G,Uzan A,Renault C,Dubroeucq MC,Guérémy C,Doble A,Le Fur G

doi

10.1016/0024-3205(86)90651-x

subject

Has Abstract

pub_date

1986-07-28 00:00:00

pages

329-39

issue

4

eissn

0024-3205

issn

1879-0631

pii

0024-3205(86)90651-X

journal_volume

39

pub_type

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