血小板活化因子拮抗剂与γ-氨基丁酸A型受体相互作用。
Platelet activating factor antagonists interact with GABAA receptors.
作者信息
Miller L G, Bazan N G, Roy R B, Clostre F, Gaver A, Braquet P
机构信息
Department of Medicine, LSU Medical Center, New Orleans 70112.
出版信息
Res Commun Chem Pathol Pharmacol. 1991 Nov;74(2):253-6.
Platelet activating factor (PAF) is ubiquitous in mammals, and may have multiple functions in the central nervous system. Triazolobenzodiazepine compounds are active both at the GABAA receptor and as PAF antagonists. To investigate whether PAF antagonist activity is involved in the actions of triazolobenzodiazepines, we examined effects of two non-benzodiazepine PAF antagonists on binding and function at the GABAA receptor. The gingkolide terpene, BN 52021 and the dioxolane-based compound BN 52115 had no effect on benzodiazepine binding or chloride channel binding in cortical membrane preparations. However, chloride uptake into cortical synaptoneurosomes was enhanced with 1 microM BN 52021 but not 1 microM BN 52115. The effect of BN 52021 was prevented by 1 microM flumazenil. PAF antagonists appear to augment GABAA receptor function without affecting binding.
血小板活化因子（PAF）在哺乳动物中广泛存在，并且可能在中枢神经系统中具有多种功能。三唑并苯二氮䓬类化合物在GABAA受体上具有活性，同时也是PAF拮抗剂。为了研究PAF拮抗剂活性是否参与三唑并苯二氮䓬类药物的作用，我们检测了两种非苯二氮䓬类PAF拮抗剂对GABAA受体结合和功能的影响。银杏内酯萜类化合物BN 52021和基于二氧戊环的化合物BN 52115对皮质膜制剂中的苯二氮䓬结合或氯离子通道结合没有影响。然而，1微摩尔的BN 52021可增强皮质突触体神经小体对氯离子的摄取，而1微摩尔的BN 52115则无此作用。1微摩尔的氟马西尼可阻止BN 52021的作用。PAF拮抗剂似乎在不影响结合的情况下增强了GABAA受体的功能。
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