Caprolactam-barbiturate interaction at the GABAA receptor complex in the guinea-pig intestine.

Abstract:

:4,6,6-Trimethylcaprolactam antagonised GABAA receptor-mediated contractile responses in guinea-pig isolated ileum, displacing the GABA dose-response curve to the right in a non-parallel manner, and causing a depression of the maximum response. Pentobarbitone not only potentiated the GABAA receptor-mediated contractions but also reversed this non-competitive antagonism by 4,6,6-trimethylcaprolactam, shifting the dose-response curve for GABA to the left and restoring the maximum response. It is conclude that this caprolactam acts at the picrotoxin-barbiturate site on the Cl(-)-ionophore complex.

journal_name

Eur J Pharmacol

authors

Kerr DI,Ong J,Prager RH,Ward DA

doi

10.1016/0014-2999(86)90146-9

subject

Has Abstract

pub_date

1986-05-13 00:00:00

pages

203-6

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(86)90146-9

journal_volume

124

pub_type

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