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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
  1. 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。

  2. 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。

  3. 在研究范围内,膜/缓冲液系数与戊巴比妥浓度无关。

  4. 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。

  5. 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。

  6. 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。

  7. 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。

  8. 高压不会显著改变这些分配系数。

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