Schweri M M, Carr L A
J Neural Transm. 1982;54(1-2):41-50. doi: 10.1007/BF01249277.
Cycloheximide (100 mg/kg) and anisomycin (50 mg/kg) decreased the synthesis of [3H]-dopamine (DA) and [3H]-5-hydroxytryptamine (5-TH) from their labelled amino acid precursors in a brain synaptosomal preparation on hour after drug administration in vivo. Treatment with anisomycin also decreased synthesis of [3H]-norepinephrine (NE). Anisomycin (1mM) decreased the accumulation of newly snythesized monoamines when added to the synaptosomal preparation in vitro, while cycloheximide (1mM) impaired only [3H]-norepinephrine formation. All drug-induced decreases in the accumulation of newly synthesized 5-hydroxytryptamine were associated with concomitant decreases in the accumulation of [3H]-tryptophan (Trp) by the synaptosome fraction, suggesting that the drugs may act in part by decreasing precursor availability. However, the same correlation was not observed between [3H]-catecholamine synthesis and [3H]-tyrosine (try) content of the synaptosomal fraction. Comparison of the results obtained after in vivo and in vitro administration of these drugs indicates that cycloheximide may exert many of its effects on monoamine synthesis via a metabolite, while anisomycin appears to act directly.
在体内给药1小时后，在脑突触体标本中，环己酰亚胺（100毫克/千克）和茴香霉素（50毫克/千克）降低了从其标记的氨基酸前体合成[3H] -多巴胺（DA）和[3H] -5-羟色胺（5-TH）的量。用茴香霉素处理也降低了[3H] -去甲肾上腺素（NE）的合成。当在体外加入突触体标本时，茴香霉素（毫1米）降低了新合成单胺的积累，而环己酰亚胺（1毫1米）仅损害了[3H] -去甲肾上腺素的形成。所有药物诱导的新合成5-羟色胺积累的减少都与突触体部分中[3H] -色氨酸（Trp）积累的相应减少有关，这表明这些药物可能部分通过降低前体的可用性起作用。然而，在[3H] -儿茶酚胺合成与突触体部分的[3H] -酪氨酸（try）含量之间未观察到相同的相关性。对这些药物在体内和体外给药后获得的结果进行比较表明，环己酰亚胺可能通过一种代谢产物对单胺合成发挥其许多作用，而茴香霉素似乎直接起作用。
