局部麻醉药对磷脂酶的影响。
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据Traynor Kunze H -纳哈斯N, JR, Wurl M
局部麻醉药对磷脂酶的影响。
Biochim Biophys学报。1976年7月20日,441 (1):93 - 102。
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952985年(在PubMed]
- 文摘
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1。六个局部麻醉药的影响一直在研究可溶性磷脂酶A2的活动(EC 3.1.1.4)和溶血磷脂酶(EC 3.1.1.5)。2。磷脂酶A2活性在人类精浆对用放射性同位素对磷脂酰乙醇胺略低刺激和抑制化合物在高浓度的麻醉工作。递减的顺序效力是氯丙嗪、dibucaine丁卡因、利多卡因、可卡因和普鲁卡因。符合之前的发现,抑制模式被认为是竞争对Ca2 +。3所示。磷脂酶A2活性的粗毒液Crotalus adamanteus并不影响或轻微刺激局部麻醉药10(2)浓度,当蛋黄作为衬底。然而,用放射性同位素对磷脂酰胆碱、磷脂酰乙醇胺作为底物,刺激磷脂酶活性与所有局部麻醉药10 (2)M,递减的顺序力量再次被氯丙嗪,dibucaine,盐酸丁卡因、利多卡因、可卡因和普鲁卡因。刺激的模式被认为是un-competitive衬底和可能独立于任何Ca2 +的参与。 4. As in seminal plasma phospholipase A2, the activity in crude Naja naja venom towards sonicated radioactively labelled phosphatidylcholine was stimulated at low and inhibited at high concentrations of dibucaine and chloropromazine, for example. The mode of inhibition was seen to be competitive with respect to Ca2+, whereas stimulation by the anaesthetic drugs was independent of Ca2+. Binding between drug and enzyme was demonstrated by equilibration filtration of purified phospholipase A2 of Naja naja venom through a Sephadex G 25-fine column, previously equilibrated with 0.5 mM radioactively labelled chlorpromazine. 5. Lysophospholipase activity in rat liver cytosol towards radioactively labelled lysophosphatidylcholine was inhibited by all local anaesthetics used; the order of decreasing potency was chlorpromazine, dibucaine, tetracaine, cocaine, lidocaine and procaine. The inhibition was un-competitive with respect to substrate. 6. The inhibitory and stimulatory potencies of the local anaesthetics employed closely parallel their lipid solubilities and anaesthetic potencies.