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前列腺素(A1、A2和B2)对苯二氮䓬结合的中枢特异性且对γ-氨基丁酸不敏感的抑制作用。

Centrally specific and GABA-insensitive inhibition of benzodiazepine binding by prostaglandins (A1, A2 and B2).

作者信息

Matsumoto K, Saito K, Fukuda H

出版信息

J Pharmacobiodyn. 1983 Oct;6(10):784-6. doi: 10.1248/bpb1978.6.784.

Abstract

Prostaglandins A1, A2 and B2 (PG A1, A2 and B2) dose-dependently inhibited specific [3H]diazepam binding to rat brain membranes but did not affect specific [3H]Ro 5-4864 binding to kidney membranes. The inhibition of [3H]diazepam binding to brain membranes by benzodiazepine agonists (diazepam and flurazepam) was potentiated by 30 microM GABA, whereas those of prostaglandins were not modified by the same concentration of GABA. These results suggest that PG A1, A2 and B2 specifically interact with central type-benzodiazepine receptors in a manner different from interactions seen with benzodiazepine agonists.

摘要

前列腺素A1、A2和B2(PGA1、A2和B2)对大鼠脑膜上特异性[3H]地西泮结合呈剂量依赖性抑制,但不影响[3H]Ro 5-4864与肾膜的特异性结合。苯二氮䓬类激动剂(地西泮和氟西泮)对脑膜上[3H]地西泮结合的抑制作用在30微摩尔γ-氨基丁酸(GABA)存在时增强,而前列腺素的抑制作用不受相同浓度GABA的影响。这些结果表明,PGA1、A2和B2与中枢型苯二氮䓬受体特异性相互作用的方式不同于苯二氮䓬类激动剂。

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