Kaufman J M, Elewaut A, Vermeulen A
Arch Int Pharmacodyn Ther. 1981 Dec;254(2):293-303.
Domperidone, a novel dopamine receptor blocking substance, unable to cross the blood brain barrier, was tested in twenty euthyroid volunteers of both sexes and in seven women with autonomous nodular goiter. Oral administration of 20 mg domperidone was followed by marked increase in serum PRL in all subjects; the response, being significantly greater in women as compared to men, was maintained in patients with autonomous goiter. The PRL response after oral domperidone was significantly greater than after 200 micrograms TRH intravenously. The PRL response obtained with oral domperidone followed by 200 microgram TRH i.v. was similar to the response obtained with domperidone alone before TRH administration. In euthyroid men the TSH response to 200 microgram TRH administered intravenously 120 min after oral domperidone was significantly greater than in a control TRH test. The data of the present study suggest that dopamine blockade at pituitary (or median eminence) level is able to stimulate maximally the lactotrophs and emphasize the important role of the dopaminergic system in the interrelated regulation of TSH and PRL secretion at the pituitary level.
多潘立酮是一种新型多巴胺受体阻断物质,不能穿过血脑屏障,在20名甲状腺功能正常的男女志愿者以及7名患有自主性结节性甲状腺肿的女性中进行了测试。所有受试者口服20毫克多潘立酮后,血清催乳素均显著升高;女性的反应明显大于男性,自主性甲状腺肿患者也保持了这种反应。口服多潘立酮后的催乳素反应明显大于静脉注射200微克促甲状腺激素释放激素(TRH)后的反应。口服多潘立酮后静脉注射200微克TRH所获得的催乳素反应与在TRH给药前单独使用多潘立酮所获得的反应相似。在甲状腺功能正常的男性中,口服多潘立酮120分钟后静脉注射200微克TRH时的促甲状腺激素反应明显大于对照TRH试验。本研究数据表明,垂体(或正中隆起)水平的多巴胺阻断能够最大程度地刺激催乳细胞,并强调多巴胺能系统在垂体水平促甲状腺激素和催乳素分泌的相互关联调节中的重要作用。