Blosser J C, Barrantes M, Parker R B
Eur J Pharmacol. 1987 Jan 28;134(1):97-103. doi: 10.1016/0014-2999(87)90136-1.
The potencies of a number of phenylethylamines and related compounds to inhibit food intake were compared with their relative affinities for hypothalamic (+)-amphetamine binding sites in vitro. There was a positive correlation (r = 0.78, P less than 0.001, n = 19) between potencies of these compounds to inhibit food intake and their potencies to inhibit 3H-amphetamine binding. Individual enantiomers of amphetamine, ephedrine, norephedrine, pseudoephedrine and norpseudoephedrine all inhibited food intake with a two- to five-fold greater potency than that of their respective optical isomers. However, they did not exhibit a comparable stereospecificity to inhibit 3H-amphetamine binding. Further, several compounds including imipramine and propranolol, without known anorectic properties were among the most potent agents to inhibit 3H-amphetamine binding. Thus, although a positive correlation exists between relative binding affinity and potencies to inhibit food intake, the functional interrelationship is uncertain.
将多种苯乙胺及其相关化合物抑制食物摄取的效能与其在体外对下丘脑（+）-苯丙胺结合位点的相对亲和力进行了比较。这些化合物抑制食物摄取的效能与其抑制[3H]（+）-苯丙胺结合的效能之间存在正相关（r = 0.78，P < 0.001，n = 19）。苯丙胺、麻黄碱、去甲麻黄碱、伪麻黄碱和去甲伪麻黄碱的各个对映体抑制食物摄取的效能均比其各自的旋光异构体高2至5倍。然而，它们在抑制[3H]（+）-苯丙胺结合方面未表现出类似的立体特异性。此外，包括丙咪嗪和普萘洛尔在内的几种没有已知食欲抑制特性的化合物是抑制[3H]（+）-苯丙胺结合的最有效药物之一。因此，尽管相对结合亲和力与抑制食物摄取的效能之间存在正相关，但功能上的相互关系尚不确定。
