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Lipid-protein interactions and effect of local anesthetics in acetylcholine receptor-rich membranes from Torpedo marmorata electric organ

机译:脂质蛋白质相互作用及局部麻醉剂从鱼雷MARMORATA电风箱中致乙酰胆碱受体 - 富含膜的影响

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The selectivity of lipid-protein interaction for spin-labeled phospholipids and gangliosides in nicotinic acetylcholine receptor-rich membranes from Torpedo marmorata has been studied by ESR spectroscopy. The association constants of the spin-labeled lipids (relative to phosphatidylcholine) at pH 8.0 are in the order cardiolipin (5.1) approximate to stearic acid (4.9) approximate to phosphatidylinositol (4.7) > phosphatidylserine, (2.7) > phosphatidylglycerol (1.7) > G(D1b) approximate to G(M1) approximate to G(M2) approximate to G(M3) approximate to phosphatidylcholine (1.0) > phosphatidylethanolamine (0.5). No selectivity for mono- or disialogangliosides is found over that for phosphatidylcholine. Aminated local anesthetics were found to compete with spin-labeled phosphatidylinositol, but to a much lesser extent with spin-labeled stearic acid, for sites on the intramembranous surface of the protein. The relative association constant of phosphatidylinositol was reduced in the presence of the different local anesthetics to the following extents: tetracaine (55%) > procaine (35%) benzocaine (30%). For stearic acid, only tetracaine gave an appreciable reduction (30%) in association constant. These displacements represent an intrinsic difference in affinity of the local anesthetics for the lipid-protein interface because the membrane partition coefficients are in the order benzocaine much greater than tetracaine approximate to procaine. [References: 57]
机译:通过ESR光谱研究了来自鱼雷MARMORATA的烟碱乙酰胆碱受体的富含烟碱乙酰胆碱受体的薄膜中旋染磷脂和神经节苷酸的脂质 - 蛋白质相互作用的选择性。在pH8.0下旋转标记的脂质(相对于磷脂酰胆碱)的关联常数在Cardiolipin(5.1)的顺序中近似与磷脂酰肌醇(4.7)>磷脂酰丝氨酸(2.7)>磷脂酰甘油(1.7)> G(D1B)近似到G(M1)近似到G(M2)近似与磷脂酰胆碱(1.0)>磷脂酰乙醇胺(0.5)的G(M3)。对于磷脂酰胆碱没有发现单颗粒或脱髓鞘无选择性。发现胺化局部麻醉剂与旋转标记的磷脂酰肌醇竞争,但在蛋白质膜上表面上的位点具有更大的旋转硬脂酸的程度。将磷脂酰肌醇的相对缔合常数在不同局部麻醉剂存在下降低到以下延伸率:四鲸(55%)>普林(35%)苯唑(30%)。对于硬脂酸,只有四鲸在结合恒定中得到了明显的减少(30%)。这些位移代表了脂蛋白界面对局部麻醉剂的亲和力的内在差异,因为膜分配系数是苯并催化的顺序大于丙谷蛋白近似。 [参考:57]

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