[Effect of trazodone (KB-831) and its metabolites on brain monoamines in rat].

摘要: The effects of trazodone (KB-831) and its metabolites on the uptake, turnover contents monoamines in rats were studied comparison with those imipramine mianserin. Trazodone exhibited a more potent inhibitory effect uptake [3H] 5-hydroxytryptamine (5-HT) into brain synaptosomes than [3H]norepinephrine (NE). at 10-30 mg/kg, p.o., also inhibited p-chloramphetamine-induced depletion 5-HT rat brain, but not 6-hydroxydopamine-induced NE heart. was most selective inhibitor among drugs tested vitro. Its metabolite, m-chlorophenyl-piperazine (m-CPP), vitro, vivo. (100 mg/kg) (30-100 induced by alpha-methyl-p-tyrosine, whereas mianserin facilitated it. At 1 hr after single administration each drug, an increase content decrease 5-hydroxyindole-3-acetic acid (5-HIAA) observed when 30 mg/kg used. 100 increased levels dihydroxyphenylacetic (DOPAC) homovanillic (HVA) decreased content. m-CPP (10-30 produced similar monoamine to trazodone. Imipramine had no even dose mg/kg. After 3 weeks successive administration, 5-HIAA hr, 17 final administration. 5-HIAA, lasted for hr. These results suggest that is neurochemical profile different from