Leander J D
Eur J Pharmacol. 1983 Jan 21;86(3-4):467-70. doi: 10.1016/0014-2999(83)90198-x.
Nalorphine, butorphanol and oxilorphan were compared in their ability to increase urinary output in the normally hydrated rat and to antagonize the increased urinary output produced by the full kappa-agonist, bremazocine. Nalorphine, butorphanol and oxilorphan increased 5-h cumulative urine output compared to controls, but the maximal effect was less than half the amount excreted after injection with 0.08 mg/kg of bremazocine. The effects of bremazocine were antagonized by nalorphine, butorphanol and oxilorphan. These effects of nalorphine, butorphanol and oxilorphan satisfy the criteria for classifying these agents as partial agonists at the kappa-opioid receptor responsible for mediating the effect of increased urinary output.
对纳洛啡、布托啡诺和奥昔吗啡增加正常水合大鼠尿量的能力以及拮抗完全κ-激动剂布瑞马佐辛引起的尿量增加的能力进行了比较。与对照组相比，纳洛啡、布托啡诺和奥昔吗啡增加了5小时累积尿量，但最大效应小于注射0.08mg/kg布瑞马佐辛后排出量的一半。纳洛啡、布托啡诺和奥昔吗啡拮抗了布瑞马佐辛的作用。纳洛啡、布托啡诺和奥昔吗啡的这些作用符合将这些药物归类为负责介导尿量增加效应的κ-阿片受体部分激动剂的标准。
