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  • Title: Caprolactam-barbiturate interaction at the GABAA receptor complex in the guinea-pig intestine.
    Author: Kerr DI, Ong J, Prager RH, Ward DA.
    Journal: Eur J Pharmacol; 1986 May 13; 124(1-2):203-6. PubMed ID: 3013660.
    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.
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