Upregulation of opioid receptor subtypes correlates with potency changes of morphine and DADLE.
Upregulation of opioid receptor subtypes correlates with potency changes of morphine and DADLE.
复制标题
阿片受体亚型的上调与吗啡和 DADLE 的效力变化相关。
DOI：
10.1016/0024-3205(88)90587-5
复制
发表时间：
1988
期刊：
影响因子：
6.1
通讯作者：
Inturrisi,CE
中科院分区：
文献类型：
--
作者：
Yoburn,BC;Luke,MC;Pasternak,GW;Inturrisi,CE
阿片拮抗剂的长期治疗增加了阿片激动剂的效力，并增加了脑阿片结合位点。在本研究中，用纳洛酮治疗8天在整个治疗期间阻断吗啡和DADLE镇痛，并增加小鼠脑中μ1，μ 2和δ阿片受体结合位点。μ 1和μ 2结合分别增加了81%和67%，而δ结合增加了31%。与这些结合变化一致，ICV吗啡产生镇痛的效力增加了3倍以上，而ICV DADLE的效力仅增加了1.7倍。这些结果表明，阿片受体亚型的相对增加与阿片受体激动剂效力变化的药效学研究一致。
Chronic treatment with opioid antagonists increases the potency of opioid agonists and produces an increase in brain opioid binding sites. In the present study, 8 day treatment with naltrexone blocked morphine and DADLE analgesia for the entire treatment period and increased μ1, μ2and δ opioid receptor binding sites in mouse brain. μ1and μ2binding were increased by 81 and 67%, respectively, while δ binding was increased by 31%. Consistent with these binding changes, the potency of ICV morphine to produce analgesia was increased by over 3-fold, while the potency of ICV DADLE was increased by only 1.7. These findings indicate that relative increases in opioid receptor subtypes agree with pharmacodynamic studies on potency changes of opioid agonists.