清醒大鼠静脉注射 SCH 23390 和 SKF 38393 后血浆催乳素浓度的升高。

Elevation of plasma prolactin concentrations by intravenous SCH 23390 and SKF 38393 in conscious rats.

作者信息

Tanimoto K, Tamminga C A, Chase T N

机构信息

Experimental Therapeutics Branch, National Institute of Neurological and Communicative Disorders and Stroke, Bethesda, MD 20205.

出版信息

Eur J Pharmacol. 1987 Dec 1;144(2):147-51. doi: 10.1016/0014-2999(87)90513-9.

DOI:10.1016/0014-2999(87)90513-9

PMID:3325296

Abstract

The effect of the selective dopamine-1 (D-1) antagonist, SCH 23390 and the selective D-1 agonist, SKF 38393 on plasma prolactin levels was investigated in conscious, freely moving male rats. Plasma prolactin was markedly increased by the intravenous injection of either SCH 23390 or SKF 38393 in a dose-related fashion. The maximal prolactin response was observed 15 min after drug injection. The d-isomer of SKF 38393 was significantly more potent than the l-isomer. In urethane-anesthetized rats, the two drugs produced similar effects on prolactin as those in the conscious animal preparation. Both SCH 23390 and SKF 38393 potentiated the sulpiride-induced prolactin elevation. These observations suggest that pharmacologic stimulation, or blockade of D-1 receptors in the living animal, can mimic the action of a D2 antagonist at the anterior pituitary lactotroph. We have speculated on the possible mechanisms in pituitary and higher in the central nervous system which might be responsible for the prolactin changes caused by either SCH 23390 or SKF 38393.

摘要

在清醒、自由活动的雄性大鼠中，研究了选择性多巴胺-1（D-1）拮抗剂SCH 23390和选择性D-1激动剂SKF 38393对血浆催乳素水平的影响。静脉注射SCH 23390或SKF 38393均可使血浆催乳素呈剂量依赖性显著升高。给药后15分钟观察到催乳素的最大反应。SKF 38393的d-异构体比l-异构体的效力明显更强。在氨基甲酸乙酯麻醉的大鼠中，这两种药物对催乳素产生的作用与清醒动物实验中的作用相似。SCH 23390和SKF 38393均增强了舒必利诱导的催乳素升高。这些观察结果表明，在活体动物中，药理学刺激或阻断D-1受体可以模拟D2拮抗剂对垂体前叶催乳细胞的作用。我们推测了垂体及中枢神经系统更高部位可能导致SCH 23390或SKF 38393引起催乳素变化的机制。