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Binding of hypoglycaemic sulphonylureas to an artificial phospholipid bilayer

机译:低血糖磺酰脲与人工磷脂双层的结合

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摘要

Hypoglycaemic sulphonylureas bind to multilamellar liposomes formed of egg yolk phosphatidylcholine. In this artificial model, both specific and non-specific components of the binding phenomenon can be characterized by the same criteria as those used in studies performed with natural membranes. The relative ability of distinct sulphonylureas to inhibit the binding of 3H-glibenclamide or 3H-gliquidone to the liposomes parallels their relative potency as insulin secretagogues. It is proposed that the insertion of hypoglycaemic sulphonylureas into the phospholipid domain of the B cell membrane could represent a primary event in the mechanism by which these agents stimulate insulin release. © 1984 Springer-Verlag.
机译:降血糖的磺酰脲结合由蛋黄磷脂酰胆碱形成的多层脂质体。在这种人工模型中,结合现象的特异性和非特异性成分均可通过与天然膜研究中所用的相同标准来表征。独特的磺酰脲类抑制3H-格列本脲或3H-甘露酮与脂质体结合的相对能力与其作为胰岛素促泌剂的相对效力平行。建议将降血糖的磺酰脲类插入B细胞膜的磷脂结构域中,可能代表这些药物刺激胰岛素释放的机制中的主要事件。 ©1984 Springer-Verlag。

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