Sloviter R S, Connor J D, Damiano B P, Drust E G
Pharmacol Biochem Behav. 1980 Aug;13(2):283-6. doi: 10.1016/0091-3057(80)90084-2.
The serotonin (5-HT) behavioral syndrome in rats served as a model to test for possible acute serotonergic effects of para-halogenated phenethylamines. p-Chloro-, p-chloro-beta-methyl-, p-fluoro-, p-bromo-, and p-iodophenethylamine produced the same 5-HT behavioral syndrome as did p-chloroamphetamine, but unlike the latter did not deplete brain 5-HT 3 days after injection. Pretreatment of rats with the 5-HT depletor p-chlorophenylalanine (pCPA)( prevented the serotonergic effects of both chloro-derivatives, and partially prevented the effects of bromo- and iodophenethylamine. 5-hydroxytryptophan restored the behavioral responses to these compounds in pCPA-pretreated rats. pCPA treatment did not prevent the behavioral effects of p-fluorophenethylamine. Similarly, zimelidine, a 5-HT uptake inhibitor, prevented the serotonergic behavioral effects of all compounds tested except p-fluorophenethylamine. Taken as a group, para-halogenated phenethylamines are short-acting serotonergic compounds which, unlike p-chloroamphetamine, do not produce long-lasting depletion of brain 5-HT. p-Chlorophenethylamine and its beta-methyl analog apparently activate central 5-HT receptors indirectly, i.e., by 5-HT release; p-fluorophenethylamine is a direct 5-HT agonist. The p-bromo- and p-iodo-derivatives apparently possess both properties.
大鼠血清素（5-羟色胺，5-HT）行为综合征被用作模型，以测试对卤代苯乙胺可能的急性血清素能效应。对氯、对氯-β-甲基、对氟、对溴和对碘苯乙胺产生了与对氯苯丙胺相同的5-HT行为综合征，但与后者不同的是，注射后3天它们不会耗尽脑内5-HT。用5-HT耗竭剂对氯苯丙氨酸（pCPA）预处理大鼠可预防两种氯衍生物的血清素能效应，并部分预防溴和碘苯乙胺的效应。5-羟色氨酸可恢复pCPA预处理大鼠对这些化合物的行为反应。pCPA处理不能预防对氟苯乙胺的行为效应。同样，5-HT摄取抑制剂齐美利定可预防除对氟苯乙胺外所有测试化合物的血清素能行为效应。总的来说，卤代苯乙胺是短效血清素能化合物，与对氯苯丙胺不同，它们不会导致脑内5-HT的长期耗竭。对氯苯乙胺及其β-甲基类似物显然通过5-HT释放间接激活中枢5-HT受体；对氟苯乙胺是一种直接的5-HT激动剂。对溴和对碘衍生物显然兼具这两种特性。
