Fujii T, Sato T, Tamura A, Kometani M, Nakao K, Fujitani K, Kodama K, Akasu M
Department of Biochemistry, Kyoto Pharmaceutical University, Japan.
Eur J Pharmacol. 1988 Feb 9;146(2-3):285-90. doi: 10.1016/0014-2999(88)90304-4.
4'-O-Substituted 1-benzyl-2-methyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines inhibited the collagen-induced activation (aggregation and ATP secretion) of rabbit platelets and transformed the shape of human erythrocytes in a dose-dependent manner. Both effects increased with increasing number of carbon atoms of the 4'-substituted hydrocarbon moiety. The incorporation of these compounds into the erythrocyte membrane was also dependent on the number of carbon atoms of the 4'-substituted radical. The most potent phenoxy derivative suppressed arachidonic acid release from membrane phospholipids but had no effect on arachidonic acid metabolism in platelets. This indicated that the effects are comparable to those of a natural bisbenzylisoquinoline, cepharanthine. These effects appear to be due to a perturbing action on the membrane lipid bilayer.
4'-O-取代的1-苄基-2-甲基-6,7-二甲氧基-1,2,3,4-四氢异喹啉抑制胶原诱导的兔血小板活化（聚集和ATP分泌），并以剂量依赖方式改变人红细胞的形状。随着4'-取代烃部分碳原子数的增加，这两种作用均增强。这些化合物掺入红细胞膜也取决于4'-取代基团的碳原子数。最有效的苯氧基衍生物抑制花生四烯酸从膜磷脂的释放，但对血小板中花生四烯酸的代谢没有影响。这表明这些作用与天然双苄基异喹啉汉防己甲素的作用相当。这些作用似乎是由于对膜脂双层的干扰作用。
