Correlation of hydrophobic character of opioid peptides with their biological activity measured in various bioassay systems.
Correlation of hydrophobic character of opioid peptides with their biological activity measured in various bioassay systems.
复制标题
阿片肽的疏水特性与其在各种生物测定系统中测量的生物活性的相关性。
DOI：
10.1016/0006-2952(82)90289-1
复制
发表时间：
1982
影响因子：
5.8
通讯作者：
O. N. Chichenkov
中科院分区：
文献类型：
--
作者：
B. Zaslavsky;N. M. Mestechkina;L. Miheeva;S. Rogozhin;G.Ya. Bakalkin;G. G. Rjazhsky;E. V. Chetverina;A. A. Asmuko;J. Bespalova;N. Korobov;O. N. Chichenkov
通过在水性聚合聚蔗糖-葡聚糖双相系统中分配，研究了一系列脑啡肽样肽的相对疏水性。已经检查了豚鼠回肠、小鼠输精管和大鼠脑受体结合测定系统中肽的活性。后两种测定中肽的生物活性与其疏水特性相关。无法建立化合物的相对疏水性与其在豚鼠回肠中的活性之间的相关性。获得的相关性似乎表明两种生物测定中的药物-受体相互作用发生在关于膜处的局部离子组成和/或受体位点的可电离状态的各种条件下。吗啡和许多类似药物的活性所描述的关系与肽所发现的关系不同，这似乎支持多阿片受体假说。
Relative hydrophobicity of a series of enkephalin-like peptides has been studied by partitioning in the aqueous polymeric Ficoll-dextran biphasic system. The activities of the peptides in the guinea pig ileum, mouse vas deferens and rat brain receptor binding assay systems have been examined. The biological activities of the peptides in the two latter assays were correlated with their hydrophobic character. No correlation between the relative hydrophobicity of the compounds and their activity in the guinea pig ileum could be established. The correlations obtained appear to indicate that the drug-receptor interactions in the two bioassays occur under various conditions in regard to the local ionic composition at the membrane and/or the ionizable state of the receptor site. The activities of morphine and a number of similar drugs are described by a relationship different from that found for the peptides, which seems to support the multiple opiate receptor hypothesis.