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PubMed · 6090832

Histidine modification with diethylpyrocarbonate induces a decrease in the binding of an antagonist, PK 11195, but not of an agonist, RO5-4864, of the peripheral benzodiazepine receptors.

J Bénavidès·F Begassat·T Phan·C Tur·A Uzan·C Renault·M C Dubroeucq·C Guérémy·G Le Fur
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Abstract

[3H]PK 11195 binding to peripheral type benzodiazepine binding sites in kidney membranes is inhibited by the histidine blocking agent diethylpyrocarbonate. This reagent irreversibly decreases the Bmax for [3H]PK 11195 without affecting the affinity. By contrast binding of [3H]RO5-4864 is not affected by diethylpyrocarbonate treatment. However RO5-4864 can protect in a concentration dependent manner the [3H]PK 11195 binding site from diethylpyrocarbonate whereas clonazepam and RO15-1788 are not active. These results suggest that PK 11195 and RO5-4864 interact with different conformational states of the receptors that RO5-4864. This is in agreement with our previous hypothesis that PK 11195 is an antagonist and RO5-4864 an agonist at the "peripheral type" benzodiazepine receptors.

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AnimalsBenzodiazepinonesCell MembraneDiethyl PyrocarbonateFormatesHistidineIsoquinolinesKidneyMaleRatsRats, Inbred StrainsReceptors, GABA-AJournal Article

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J Bénavidès, F Begassat, T Phan, C Tur, A Uzan, C Renault, M C Dubroeucq, C Guérémy, G Le Fur. 1984-09-17. Histidine modification with diethylpyrocarbonate induces a decrease in the binding of an antagonist, PK 11195, but not of an agonist, RO5-4864, of the peripheral benzodiazepine receptors.. https://doi.org/10.1016/0024-3205(84)90095-x

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