Meltzer H Y, Fang V S, Simonovich M, Paul S M
Eur J Pharmacol. 1977 Feb 21;41(4):431-6. doi: 10.1016/0014-2999(77)90263-1.
Since prolactin secretion is under vigorous dopaminergic inhibition, neuroleptic drugs can, because of their capacity to block dopamine receptors, produce large increases in plasma prolactin levels in man and laboratory animals. The capacity of intramuscular (i.m.) chlorpromazine and 6 of its metabolites to increase plasma prolactin levels in male rats was compared. 7-Hydroxychlorpromazine produced increases in plasma prolactin equivalent to those produced by chlorpromazine. The following metabolites had no effect on plasma prolactin levels after i.m. injections of 5 mg/kg: 8-hydroxychlorpromazine; 7,8-dihydroxychlorpromazine; 8-hydroxy-7-methoxychlorpromazine; 7-methoxychlorpromazine; and chlorpromazine sulfoxide. 8-Hydroxychlorpromazine, 7-methoxychlorpromazine, 7,8-dihydroxychlorpromazine and chlorpromazine sulfoxide had no effect even after 25 mg/kg i.m. The capacity to increase rat plasma prolactin correlates highly with other methods of determining potential antipsychotic activity of chlorpromazine and its derivatives.
由于催乳素的分泌受到强大的多巴胺能抑制作用，抗精神病药物因其阻断多巴胺受体的能力，可使人类和实验动物的血浆催乳素水平大幅升高。比较了肌肉注射氯丙嗪及其6种代谢产物使雄性大鼠血浆催乳素水平升高的能力。7-羟基氯丙嗪使血浆催乳素升高的程度与氯丙嗪相当。肌肉注射5mg/kg后，以下代谢产物对血浆催乳素水平无影响：8-羟基氯丙嗪、7,8-二羟基氯丙嗪、8-羟基-7-甲氧基氯丙嗪、7-甲氧基氯丙嗪和氯丙嗪亚砜。即使肌肉注射25mg/kg，8-羟基氯丙嗪、7-甲氧基氯丙嗪、7,8-二羟基氯丙嗪和氯丙嗪亚砜也无影响。使大鼠血浆催乳素升高的能力与测定氯丙嗪及其衍生物潜在抗精神病活性的其他方法高度相关。
