Martin L L, Roland D M, Neale R F, Wood P L
Eur J Pharmacol. 1986 Dec 2;132(1):53-5. doi: 10.1016/0014-2999(86)90008-7.
The ability of various phenylalkylamines to inhibit the binding of [3H]tryptamine to rat frontal/parietal cortical membranes was examined in vitro. Affinity for [3H]tryptamine binding sites improved as the alkyl side chain was extended to include four carbons or when a methoxy group was added at the para position of the ring. One compound, p-methoxyphenylpropylamine (IC50 = 3.6 nM), was as potent as unlabelled tryptamine as a displacing agent. Based on the unique structure-activity relationship obtained, it appears that [3H]tryptamine binding sites do not mediate the actions of phenethylamines on serotonin uptake or release.
在体外研究了各种苯烷基胺抑制[3H]色胺与大鼠额叶/顶叶皮质膜结合的能力。随着烷基侧链延长至包含四个碳原子或在环的对位添加甲氧基，对[3H]色胺结合位点的亲和力增强。一种化合物，对甲氧基苯丙胺（IC50 = 3.6 nM），作为置换剂与未标记的色胺一样有效。基于所获得的独特构效关系，[3H]色胺结合位点似乎并不介导苯乙胺对5-羟色胺摄取或释放的作用。
