Ukai M, Nakayama S, Kameyama T
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Meijo University, Nagoya, Japan.
Neuropharmacology. 1988 Oct;27(10):1027-31. doi: 10.1016/0028-3908(88)90063-9.
The effects of the opioid antagonist, Mr2266 [(-)-(1R,5R,9R)-5,9-diethyl-2-(3-furyl-methyl)-2'-hydroxy-6,7-benzomo rph an] on the intake of water and saline (0.9%) were investigated in the mouse, deprived of water for 24 hr. In an attempt to evaluate motor functions, the behavior after treatment with Mr2266 was also examined by using multi-dimensional behavioral analyses. Although smaller doses (1.0, 3.0 and 10.0 mg/kg) of Mr2266 failed to affect significantly the intake of water, a larger dose (30.0 mg/kg) elicited a significant attenuation in the intake of water. During a 30 min observation, Mr2266 (30.0 mg/kg) depressed markedly linear locomotion, while other behavioral responses, such as rearing and grooming, remained unchanged. In contrast, 1.0-30.0 mg/kg doses of the drug produced a significant reduction in the intake of saline. The drug Mr2266 had no significant effects on the latency to start drinking at any doses tested. These results suggest that Mr2266 specifically blocks the intake of saline of the mouse through the mediation of opioid systems.
在剥夺水分24小时的小鼠中，研究了阿片类拮抗剂Mr2266 [(-)-(1R,5R,9R)-5,9-二乙基-2-(3-呋喃基甲基)-2'-羟基-6,7-苯并吗啡烷]对水和生理盐水（0.9%）摄取量的影响。为了评估运动功能，还通过多维行为分析检查了Mr2266治疗后的行为。虽然较小剂量（1.0、3.0和10.0 mg/kg）的Mr2266未能显著影响水的摄取量，但较大剂量（30.0 mg/kg）会导致水摄取量显著减少。在30分钟的观察期内，Mr2266（30.0 mg/kg）显著抑制直线运动，而其他行为反应，如竖毛和梳理毛发，保持不变。相比之下，1.0 - 30.0 mg/kg剂量的该药物会使生理盐水摄取量显著减少。在任何测试剂量下，药物Mr2266对开始饮水的潜伏期均无显著影响。这些结果表明，Mr2266通过阿片系统的介导特异性地阻断小鼠对生理盐水的摄取。
