Ukai M, Kameyama T
Brain Res. 1985 Jul 1;337(2):352-6. doi: 10.1016/0006-8993(85)90074-5.
The effects of U-50, 488H (trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl ]-benzeneacetamide, methane sulfonate, hydrate), a purported selective kappa (non-mu) opioid agonist on spontaneous locomotor activity were investigated using a multi-dimensional behavioral analyzer (Animex II). U-50,488H (1 mg/kg) failed to affect behavior in mice, however, 3 mg/kg significantly reduced rearing and grooming. In addition, 10 mg/kg markedly reduced linear locomotion, rearing and grooming. The behavioral depression induced by U-50,488H (10 mg/kg) was reversible by the opioid antagonist Mr2266 (10 mg/kg). These results suggest that the selective activation of the kappa (non-mu) opioid receptor by U-50,488H decreases linear locomotion, rearing and grooming in mice.
使用多维度行为分析仪(Animex II)研究了U-50,488H(反式-3,4-二氯-N-甲基-N-[2-(1-吡咯烷基)-环己基]-苯乙酰胺甲磺酸盐一水合物),一种据称的选择性κ(非μ)阿片受体激动剂对自发运动活性的影响。U-50,488H(1毫克/千克)对小鼠行为没有影响,然而,3毫克/千克显著减少了竖毛和理毛行为。此外,10毫克/千克显著减少了直线运动、竖毛和理毛行为。U-50,488H(10毫克/千克)诱导的行为抑制可被阿片受体拮抗剂Mr2266(10毫克/千克)逆转。这些结果表明,U-50,488H对κ(非μ)阿片受体的选择性激活会降低小鼠的直线运动、竖毛和理毛行为。