螺旋多林（U-62066E）——一种κ阿片受体激动剂在人体中的利尿作用机制
Mechanism of diuretic action of spiradoline (U-62066E)--a kappa opioid receptor agonist in the human.
作者信息
Rimoy G H, Bhaskar N K, Wright D M, Rubin P C
机构信息
Department of Therapeutics, Queen's Medical Centre, Nottingham.
出版信息
Br J Clin Pharmacol. 1991 Nov;32(5):611-5. doi: 10.1111/j.1365-2125.1991.tb03960.x.
Abstract
- The mechanism of the diuretic effect of the kappa opioid receptor agonist spiradoline was investigated in 10 healthy male subjects in a placebo-controlled, double-blind cross-over study. 2. Urine volume and osmolality, plasma vasopressin and Doppler renal blood velocity indices were recorded for 1.25 h before and 6 h following injection. 3. Spiradoline caused a significant increase in urine output which was antagonized by high but not low dose naloxone. The urine increase was accompanied by a significant decrease in osmolality which was also antagonised by high but not low dose naloxone. 4. Spiradoline had no effect on plasma vasopressin concentration or on renal blood velocity indices. 5. We conclude that kappa agonists induce diuresis in humans by a mechanism not involving suppression of vasopressin or changes in renal blood velocity indices.
摘要
- 在一项安慰剂对照、双盲交叉研究中，对10名健康男性受试者研究了κ阿片受体激动剂spiradoline的利尿作用机制。2. 在注射前1.25小时和注射后6小时记录尿量和渗透压、血浆血管加压素和多普勒肾血流速度指标。3. Spiradoline导致尿量显著增加，高剂量而非低剂量纳洛酮可拮抗此作用。尿量增加伴随渗透压显著降低，高剂量而非低剂量纳洛酮也可拮抗此作用。4. Spiradoline对血浆血管加压素浓度或肾血流速度指标无影响。5. 我们得出结论，κ激动剂通过不涉及抑制血管加压素或肾血流速度指标变化的机制诱导人体利尿。
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