Histidine modification with diethylpyrocarbonate induces a decrease in the binding of an antagonist, PK 11195, but not of an agonist, R05–4864, of the peripheral benzodiazepine receptors
| Autor: | J. Benavides, G. Le Fur, C. Gueremy, T. Phan, Andre Uzan, C. Tur, Christian Renault, Marie-Christine Dubroeucq, F. Begassat |
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| Rok vydání: | 1984 |
| Předmět: |
Agonist
PK-11195 medicine.drug_class GABAA receptor Antagonist General Medicine Pharmacology General Biochemistry Genetics and Molecular Biology Cell membrane chemistry.chemical_compound medicine.anatomical_structure chemistry medicine General Pharmacology Toxicology and Pharmaceutics Binding site Receptor Histidine |
| Zdroj: | Life Sciences. 35:1249-1256 |
| ISSN: | 0024-3205 |
| DOI: | 10.1016/0024-3205(84)90095-x |
| Popis: | [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. |
| Databáze: | OpenAIRE |
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