苯二氮䓬类似物可抑制花生四烯酸诱导的人血小板聚集和血栓素合成。
Benzodiazepine analogues inhibit arachidonate-induced aggregation and thromboxane synthesis in human platelets.
作者信息
Fonlupt P, Croset M, Lagarde M
机构信息
Unité INSERM 205-Laboratoire de Chimie Biologique, Villeurbanne, France.
出版信息
Br J Pharmacol. 1990 Dec;101(4):920-4. doi: 10.1111/j.1476-5381.1990.tb14181.x.
Abstract
- Benzodiazepine analogues inhibit human platelet aggregation induced by arachidonate with an EC50 value of 0.68 microM for PK 11195, the most potent analogue used. 2. There was a highly significant correlation between the inhibition of arachidonate-induced aggregation and the affinity for the peripheral-type of benzodiazepine binding sites. 3. There was no significant correlation between the inhibition of the platelet activating factor (PAF)-induced aggregation and the binding to the peripheral-type of benzodiazepine binding sites. 4. The inhibition of platelet aggregation seems to result from the inhibition of arachidonic acid cyclo-oxygenation, since the synthesis of thromboxane and 12-hydroxy-heptadecatrienoic acid, both cyclo-oxygenase products, was reduced. 5. Our results suggest that peripheral-type of benzodiazepine binding sites on human platelets could be linked to cyclo-oxygenase.
摘要
- 苯二氮䓬类似物抑制花生四烯酸诱导的人血小板聚集，对于所使用的最有效的类似物PK 11195，其半数有效浓度（EC50）值为0.68微摩尔。2. 花生四烯酸诱导的聚集抑制与对外周型苯二氮䓬结合位点的亲和力之间存在高度显著的相关性。3. 血小板活化因子（PAF）诱导的聚集抑制与对外周型苯二氮䓬结合位点的结合之间无显著相关性。4. 血小板聚集的抑制似乎是由于花生四烯酸环氧化作用的抑制，因为血栓素和12-羟基十七碳三烯酸这两种环氧化酶产物的合成均减少。5. 我们的结果表明，人血小板上的外周型苯二氮䓬结合位点可能与环氧化酶有关。
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