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各种氯丙嗪衍生物对阿扑吗啡引起的突触体酪氨酸羟化酶活性抑制的影响。

The effect of various chlorpromazine derivatives on the apomorphine-elicited inhibition of synaptosomal tyrosine hydroxylase activity.

作者信息

Bronaugh R L, Goldstein M

出版信息

Psychopharmacol Commun. 1975;1(2):201-8.

PMID:4859
Abstract

The effects of chlorpromazine and of some metabolites of chlorpromazine on the apomorphine-elicited inhibition of synaptosomal tyrosine hydroxylase activity were investigated. Chlorpromazine, nor1-chlorpromazine and 7-hydroxychlorpromazine reverse the apomorphine-elicited inhibition of tyrosine hydroxylase activity while nor1-chlorpromazine sulfoxide and nor2-chlorpromazine sulfoxide have no effect on this inhibition. 6-Hydroxychlorpromazine and promethazine also reverse the enzyme inhibition by apomorphine but are less potent than chlorpromazine or 7-hydroxychlorpromazine. These results show that chlorpromazine and its metabolites with antipsychotic activity are more effective in reversing the apomorphine-elicited inhibition of tyrosine hydroxylase than those metabolites which are devoid of antipsychotic activity.

摘要

研究了氯丙嗪及其一些代谢产物对阿扑吗啡引起的突触体酪氨酸羟化酶活性抑制的影响。氯丙嗪、去甲-1-氯丙嗪和7-羟基氯丙嗪可逆转阿扑吗啡引起的酪氨酸羟化酶活性抑制,而去甲-1-氯丙嗪亚砜和去甲-2-氯丙嗪亚砜对这种抑制没有影响。6-羟基氯丙嗪和异丙嗪也可逆转阿扑吗啡对酶的抑制作用,但效力低于氯丙嗪或7-羟基氯丙嗪。这些结果表明,具有抗精神病活性的氯丙嗪及其代谢产物在逆转阿扑吗啡引起的酪氨酸羟化酶抑制方面比那些没有抗精神病活性的代谢产物更有效。

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