脂质双分子层膜的依赖性：戊巴比妥的缓冲分配系数对pH值和脂质组成的影响
The dependence of the lipid bilayer membrane: buffer partition coefficient of pentobarbitone on pH and lipid composition.
作者信息
Miller K W, Yu S C
出版信息
Br J Pharmacol. 1977 Sep;61(1):57-63. doi: 10.1111/j.1476-5381.1977.tb09739.x.
Abstract
1 The membrane/buffer partition coefficient of [14C]-pentobarbitone has been determined as a function of the lipid composition of bilayer membranes. 2 A new technique based on ultrafiltration gave comparable results to conventional techniques but required less time for equilbration. 3 The membrane/buffer coefficient was independent of pentobarbitone concentration in the range studies. 4 The apparent partition coefficient varied with pH and was a linear function of the degree of dissociation of pentobarbition. 5 Both the charged and uncharged forms of pentobarbitone partitioned into the membrane, the latter to a much greater extent than the former. 6 At low pH the highest partition coefficient observed was in egg phosphatidylcholine bilayer membranes. 7 Incorporation of cholesterol or phosphatidic acid into phosphatidylcholine membranes greatly reduced the partition coefficient. 8 High pressures do not greatly change these partition coefficients.
摘要
已测定[¹⁴C] - 戊巴比妥的膜/缓冲液分配系数与双层膜脂质组成的函数关系。
一种基于超滤的新技术得到的结果与传统技术相当，但达到平衡所需时间更短。
在研究范围内，膜/缓冲液系数与戊巴比妥浓度无关。
表观分配系数随pH值变化，是戊巴比妥解离程度的线性函数。
戊巴比妥的带电和不带电形式都能分配到膜中，后者的分配程度比前者大得多。
在低pH值下，观察到的最高分配系数出现在鸡蛋磷脂酰胆碱双层膜中。
将胆固醇或磷脂酸掺入磷脂酰胆碱膜中会大大降低分配系数。
高压不会显著改变这些分配系数。
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