Leander J D, Hynes M D
Eur J Pharmacol. 1983 Mar 4;87(4):481-4. doi: 10.1016/0014-2999(83)90089-4.
Diprenorphine, naloxone, MR-2266-BS and WIN-44,441-3 were compared for their ability to antagonize morphine analgesia and to decrease deprivation-induced drinking in rats. Diprenorphine and naloxone were markedly more potent (32x) than MR-2266-BS and WIN-44,441-3 in antagonizing the analgesic effects of morphine. In contrast, diprenorphine, naloxone and MR-2266-BS decreased deprivation-induced drinking over a similar dose range. The doses required to reduce fluid consumption were higher than those necessary to antagonize morphine. WIN-44,441-3 was ineffective in decreasing drinking. The relatively similar potencies of diprenorphine, naloxone and MR-2266-BS for decreasing deprivation-induced drinking suggest that the effect on drinking involves antagonist activity at a kappa-opioid receptor.
比较了二丙诺啡、纳洛酮、MR-2266-BS和WIN-44,441-3拮抗吗啡镇痛以及减少大鼠剥夺诱导饮水的能力。在拮抗吗啡的镇痛作用方面,二丙诺啡和纳洛酮的效力明显比MR-2266-BS和WIN-44,441-3强(32倍)。相比之下,二丙诺啡、纳洛酮和MR-2266-BS在相似的剂量范围内减少剥夺诱导的饮水。减少液体消耗所需的剂量高于拮抗吗啡所需的剂量。WIN-44,441-3在减少饮水方面无效。二丙诺啡、纳洛酮和MR-2266-BS减少剥夺诱导饮水的效力相对相似,这表明对饮水的影响涉及κ-阿片受体的拮抗活性。