Leander J D
Pharmacol Biochem Behav. 1987 Apr;26(4):705-7. doi: 10.1016/0091-3057(87)90600-9.
The effects of cyclazocine (SC) were studied under a variety of test conditions to determine its various activities on urinary output. Cyclazocine antagonized the morphine-induced (20 mg/kg) antidiuretic effect in water-loaded (3 ml/100 g b.wt.) rats at low doses (0.08, 0.16 and 0.32 mg/kg). At higher doses (1.25, 5 and 20 mg/kg), cyclazocine caused diuresis in normally hydrated rats. The diuresis produced by 1.25 and 5, but not 20 mg/kg, was antagonized by naloxone (10 mg/kg). In water-deprived rats and in normally hydrated rats, cyclazocine, in a dose-related fashion, antagonized the diuretic effects of 0.08 mg/kg of bremazocine. These results are compatible with the interpretation that cyclazocine has mu-antagonist activity at low doses, then partial kappa-agonist activity at intermediate doses, followed by non-opioid agonist activities at the higher doses.
在各种试验条件下研究了环唑辛（皮下注射）对尿量的影响，以确定其对尿量的多种作用。在低剂量（0.08、0.16和0.32mg/kg）时，环唑辛可拮抗吗啡（20mg/kg）对水负荷（3ml/100g体重）大鼠诱导的抗利尿作用。在较高剂量（1.25、5和20mg/kg）时，环唑辛可使正常水合大鼠产生利尿作用。1.25和5mg/kg而非20mg/kg产生的利尿作用可被纳洛酮（10mg/kg）拮抗。在缺水大鼠和正常水合大鼠中，环唑辛以剂量相关方式拮抗0.08mg/kg布马佐辛的利尿作用。这些结果符合以下解释：环唑辛在低剂量时具有μ-拮抗活性，在中等剂量时具有部分κ-激动活性，在高剂量时具有非阿片类激动活性。
