多巴胺的纯摄取阻滞剂可降低催乳素分泌：双氯芬辛的研究。

Pure uptake blockers of dopamine can reduce prolactin secretion: studies with diclofensine.

作者信息

Di Renzo G, Amoroso S, Taglialatela M, Canzoniero L M, Maida P, Lombardi G, Annunziato L

机构信息

Department of Pharmacology, 2nd School of Medicine, University of Naples, Italy.

出版信息

Life Sci. 1988;42(21):2161-9. doi: 10.1016/0024-3205(88)90131-2.

DOI:10.1016/0024-3205(88)90131-2

PMID:2968488

Abstract

The effects of diclofensine, a pure dopamine (DA) uptake inhibitor on 1) 3H-DA uptake in rat arcuate-periventricular nucleus-median eminence synaptosomes, 2) basal and K+-evoked endogenous DA release from tuberoinfundibular dopaminergic (TIDA) neurons and 3) in vivo prolactin (PRL) secretion were studied. Diclofensine, in concentrations of 0.01, 0.1 and 1 microM caused a marked decrease of 3H-DA uptake. In addition, it was unable to stimulate basal endogenous DA release which, on the contrary, was elicited by d-amphetamine in the same concentration (50 microM). On the other hand, diclofensine (50 microM) caused a 3 fold enhancement of K+-evoked DA release. Finally, the compound, when administered in vivo to male rats, significantly reduced basal serum PRL levels. The results of the present study seem to indicate that the pharmacological blockade of DA uptake in TIDA neurons is a condition sufficient to cause a reduction of PRL release.

摘要

研究了纯多巴胺（DA）摄取抑制剂双氯芬辛对以下方面的影响：1）大鼠弓状-室周核-正中隆起突触体对³H-DA的摄取；2）来自结节漏斗多巴胺能（TIDA）神经元的基础及钾离子诱发的内源性DA释放；3）体内催乳素（PRL）分泌。双氯芬辛浓度为0.01、0.1和1微摩尔时，可显著降低³H-DA摄取。此外，它无法刺激基础内源性DA释放，相反，相同浓度（50微摩尔）的右旋苯丙胺可引发这种释放。另一方面，双氯芬辛（50微摩尔）可使钾离子诱发的DA释放增强3倍。最后，该化合物对雄性大鼠进行体内给药时，可显著降低基础血清PRL水平。本研究结果似乎表明，TIDA神经元中DA摄取的药理学阻断足以导致PRL释放减少。