A 2H-NMR study on the interactions of the local anesthetic tetracaine with membranes containing phosphatidylserine.
A 2H-NMR study on the interactions of the local anesthetic tetracaine with membranes containing phosphatidylserine.
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关于局麻药丁卡因与含有磷脂酰丝氨酸的膜相互作用的 2H-NMR 研究。
DOI：
10.1016/0005-2736(86)90013-1
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发表时间：
1986
期刊：
影响因子：
--
通讯作者：
Ian C.P. Smith
中科院分区：
文献类型：
--
作者：
E. C. Kelusky;Yvan Boulanger;Shirley Schreier;Ian C.P. Smith
本文用~ 2 H-NMR研究了局部麻醉药丁卡因与含磷脂酰丝氨酸的模型膜的相互作用。带电丁卡因表现出异常大的分配系数到磷脂酰丝氨酸的多层分散体。2 H-NMR谱由Pake双峰和窄线组成，前者对应于双层中的丁卡因，后者对应于溶液中的丁卡因。一个强大的pH依赖性的四极分裂表示不同的膜位置带电和不带电的丁卡因。在磷脂酰丝氨酸和磷脂酰胆碱的等摩尔混合物中，分配系数和2 H-NMR谱更像在纯磷脂酰胆碱中观察到的那些。在pH 5.5的稀释研究表明，在磷脂酰丝氨酸/磷脂酰胆碱混合物丁卡因的经验，类似于早期发现的丁卡因在磷脂酰胆碱的三个网站交换。丁卡因在与膜弱结合的位点和溶液中游离的位点之间快速交换，并且与膜中强结合的位点缓慢交换。
The interaction of the local anesthetic tetracaine with phosphatidylserine-containing model membranes has been studied by2H-NMR. Charged tetracaine exhibited an unusually large partition coefficient into multilamellar dispersions of phosphatidylserine. The2H-NMR spectra consisted of a Pake doublet and a narrow line, with the former corresponding to tetracaine in the bilayer and the latter to tetracaine free in solution. A strong pH dependence of the quadrupole splittings indicated different membrane locations for charged and uncharged tetracaine. In equimolar mixtures of phosphatidylserine and phosphatidylcholine the partition coefficients and2H-NMR spectra were much more like those observed in neat phosphatidylcholine than in neat phosphatidylserine. Dilution studies at pH 5.5 indicated that in phosphatidylserine/phosphatidylcholine mixtures tetracaine experiences a three-site exchange similar to that found earlier for tetracaine in phosphatidylcholine. Tetracaine is in fast exchange between sites weakly bound to membrane and free in solution, and in slow exchange with a strongly bound site in the membrane.
麻醉电荷对麻醉剂-磷脂相互作用的影响。
DOI：
10.1016/0005-2736(81)90371-0
发表时间：
1981
期刊：
Biochimica et biophysica acta
影响因子：
--
作者：
Davio,SR;Low,PS
通讯作者：
Low,PS