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D-舒必利在人体多巴胺受体水平可能具有的混合激动剂-拮抗剂活性。

Possible mixed agonist--antagonist activity of D-sulpiride at dopamine receptor level in man.

作者信息

Benfenati F, Bernardi P, Cortelli P, Capelli M, Adani C, Calzà L, Agnati L F

出版信息

Neurosci Lett. 1981 Nov 4;26(3):289-95. doi: 10.1016/0304-3940(81)90147-6.

Abstract

The effects of different doses of D-sulpiride (1, 6, 12 and 25 mg, i.v.) on arterial blood pressure (ABP), heart rate (HR) and prolactin (PRL), growth hormone (GH), insulin and gastrin secretions have been studied in 8 normal men. D-Sulpiride increased systolic ABP with a maximum effect rather 12 mg i.v., while it had only slight effects on diastolic ABP and HR. PRL secretion was increased by D-sulpiride in a dose-dependent way, while insulin secretion was lowered and GH secretion slightly enhanced only in a restricted range of doses (6 mg and 12 mg i.v., respectively). Gastrin secretion seemed to be unaffected by D-sulpiride at any of the tested doses. These results are discussed in view of a possible mixed agonist--antagonist activity of D-sulpiride at dopamine receptor level in contrast with the relatively pure antagonistic action of the levo isomer.

摘要

研究了不同剂量的D-舒必利(1、6、12和25毫克,静脉注射)对8名正常男性动脉血压(ABP)、心率(HR)以及催乳素(PRL)、生长激素(GH)、胰岛素和胃泌素分泌的影响。D-舒必利可使收缩压升高,静脉注射12毫克时作用最强,而对舒张压和心率仅有轻微影响。D-舒必利可剂量依赖性地增加PRL分泌,而胰岛素分泌降低,GH分泌仅在有限的剂量范围内(分别为静脉注射6毫克和12毫克)略有增强。在任何测试剂量下,胃泌素分泌似乎均不受D-舒必利影响。鉴于D-舒必利在多巴胺受体水平可能具有混合激动剂 - 拮抗剂活性,与左旋异构体相对纯粹的拮抗作用形成对比,对这些结果进行了讨论。

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