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M Mestre T Carriot G Néliat A Uzan C Renault M C Dubroeucq C Guérémy A Doble G Le Fur 《Life sciences》1986,39(4):329-339
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. 相似文献
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M. Mestre T. Carriot C. Belin A. Uzan C. Renault M.C. Dubroeucq C. Guérémy G. Le Fur 《Life sciences》1984,35(9):953-962
R05-4864 decreased in a dose-dependent manner, from 3 × 10?9 M to 3 × 10?6 M, the duration of intracellular action potential and the contractility in a guinea pig preparation. Diazepam was less effective and clonazepam inactive. The effects of R05-4864 were GABA-independent and antagonized by PK 11195 but not by the selective antagonist of the brain type benzodiazepine receptors R015-1788. These results show the pharmacological relevance of peripheral type benzodiazepine binding sites at the cardiac level. 相似文献
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Carriot Nathan Barry-Martinet Raphaëlle Briand Jean-François Ortalo-Magné Annick Culioli Gérald 《Metabolomics : Official journal of the Metabolomic Society》2022,18(3):1-12
Metabolomics - Recent advances in high-throughput methodologies in the ‘omics’ and synthetic biology fields call for rapid and sensitive workflows in the metabolic phenotyping of... 相似文献
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Electrophysiological and pharmacological evidence that peripheral type benzodiazepine receptors are coupled to calcium channels in the heart 总被引:10,自引:0,他引:10
M Mestre T Carriot C Belin A Uzan C Renault M C Dubroeucq C Guérémy A Doble G Le Fur 《Life sciences》1985,36(4):391-400
PK 11195, an antagonist of the peripheral type benzodiazepine receptor, does not affect either the duration of the action potential or the tension of the guinea pig papillary muscle. However, it antagonized the effects of the calcium channel blockers, nitrendipine, verapamil, diltiazem, and of BAY K8644, a calcium channel agonist in this heart preparation. On the other hand, PK 11195 does not change the increase in the action potential duration provoked by the potassium channel blocker tetraethylammonium. RO5-4864, an agonist of the peripheral type benzodiazepine receptor, decreased the tension of the guinea pig papillary muscle. The effect was reversed by increasing extracellular Ca2+ concentrations up to 4 mM. These results suggest that in the heart the peripheral type benzodiazepine receptors are coupled to calcium channels. 相似文献
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