Mizuchi A, Kitagawa N, Saruta S, Tokuda H, Miyachi Y
Arch Int Pharmacodyn Ther. 1984 Feb;267(2):232-40.
Oral administration of sultopride caused a significant and dose-related increase in serum prolactin levels in the rat. Sultopride was 4-6 times as potent as sulpiride in stimulating prolactin secretion. Both drugs produced much greater stimulations of prolactin release in female rats than in male rats, suggesting the sex difference in response to drugs. CB-154, a dopamine agonist, inhibited the sultopride-induced prolactin release. Stereoselective activity of sultopride-isomers was observed in increasing rat prolactin secretion. Sultopride had no significant effects on LH and FSH basal levels in female rats. In a successive study, basal prolactin levels in the male rat were higher at 2-3 days, but lower at 6 and 14 days. Prolactin response 1 hr after sultopride administration was observed throughout the experiments. Sultopride neutralized the dopamine-mediated inhibition of prolactin secretion from the anterior pituitary in vitro. These results suggest that sultopride, like sulpiride, stimulates prolactin secretion by blocking the dopamine receptor in the pituitary.
口服舒托必利可使大鼠血清催乳素水平显著升高，且呈剂量依赖性。在刺激催乳素分泌方面，舒托必利的效力是舒必利的4至6倍。两种药物对雌性大鼠催乳素释放的刺激作用均远大于雄性大鼠，表明对药物的反应存在性别差异。多巴胺激动剂CB - 154可抑制舒托必利诱导的催乳素释放。在增加大鼠催乳素分泌方面观察到了舒托必利异构体的立体选择性活性。舒托必利对雌性大鼠促黄体生成素（LH）和促卵泡生成素（FSH）的基础水平无显著影响。在一项后续研究中，雄性大鼠的基础催乳素水平在第2至3天较高，但在第6天和第14天较低。在整个实验过程中均观察到了舒托必利给药后1小时的催乳素反应。在体外，舒托必利可中和多巴胺介导的对垂体前叶催乳素分泌的抑制作用。这些结果表明，舒托必利与舒必利一样，通过阻断垂体中的多巴胺受体来刺激催乳素分泌。
