Oishi R, Takemori A E
Neuropharmacology. 1982 Jan;21(1):57-61. doi: 10.1016/0028-3908(82)90211-8.
Stereospecific accumulation of [3H]dihydromorphine and [3H]naltrexone by striatal slices from morphine-dependent mice was examined in Krebs-Ringer bicarbonate medium. Striatal slices showed a saturable and stereospecific accumulation of both [3H]ligands. The accumulation constant of naltrexone, determined by Wilkinson's analysis, was significantly decreased in both morphine-dependent mice and dependent mice abruptly withdrawn for 6 hr. The maximal accumulation of naltrexone was not changed in withdrawn mice, but decreased in dependent mice. This could be due to the high concentration of residual morphine in the slices. There were no significant differences in the accumulation constant or maximal accumulation of dihydromorphine among the striatal slices from control, dependent and withdrawn mice. These data indicate that in morphine-dependent mice, there is an increased affinity of the opioid receptors for the narcotic antagonist, naltrexone but not for the agonist, dihydromorphine.
在碳酸氢盐缓冲的 Krebs-Ringer 培养基中,检测了吗啡依赖小鼠纹状体切片对 [³H] 二氢吗啡和 [³H] 纳曲酮的立体特异性摄取。纹状体切片对两种 [³H] 配体均表现出可饱和的立体特异性摄取。通过威尔金森分析确定的纳曲酮摄取常数,在吗啡依赖小鼠和突然戒断 6 小时的依赖小鼠中均显著降低。纳曲酮的最大摄取量在戒断小鼠中未改变,但在依赖小鼠中降低。这可能是由于切片中残留吗啡的浓度较高。对照、依赖和戒断小鼠的纹状体切片中二氢吗啡的摄取常数或最大摄取量无显著差异。这些数据表明,在吗啡依赖小鼠中,阿片受体对麻醉拮抗剂纳曲酮的亲和力增加,但对激动剂二氢吗啡的亲和力未增加。