影响血脑屏障渗透的因素。

The factors that influence permeation across the blood-brain barrier.

作者信息

Abraham Michael H

机构信息

Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, UK.

出版信息

Eur J Med Chem. 2004 Mar;39(3):235-40. doi: 10.1016/j.ejmech.2003.12.004.

DOI:10.1016/j.ejmech.2003.12.004

PMID:15051171

Abstract

Using data on perfusion from saline at pH 7.4 taken from the literature, it is shown that logarithms of PS-products, log PS, can satisfactorily be correlated with the five Abraham descriptors for 30 neutral compounds. The equation has R(2) = 0.870 and S.D. = 0.52, and shows that molecular size leads to an increase in permeation rate, and dipolarity/polarizability, hydrogen bond acidity and hydrogen bond basicity all decrease the rate of permeation. There are difficulties with acids and bases that are partially ionised at pH 7.4 because it is not possible to assess the rate of permeation of the resulting ionic species with respect to the neutral species. The same problem will arise in the analysis of perfusion from plasma or blood.

摘要

利用从文献中获取的pH值为7.4的盐水灌注数据表明，PS产物的对数log PS与30种中性化合物的五个亚伯拉罕描述符能令人满意地相关。该方程的R(2) = 0.870，标准差 = 0.52，表明分子大小导致渗透速率增加，而偶极矩/极化率、氢键酸度和氢键碱度均降低渗透速率。对于在pH 7.4时部分电离的酸和碱存在困难，因为无法评估生成的离子物种相对于中性物种的渗透速率。在分析来自血浆或血液的灌注时也会出现同样的问题。