Comparison of the antagonistic effects of 6 beta-naltrexol and naltrexone against morphine analgesia / 药学学报

ABSTRACT

<p><b>AIM</b>To compare the antagonistic effects of 6 beta-naltrexol and naltrexone against morphine analgesia.</p><p><b>METHODS</b>The effects of 6 beta-naltrexol and naltrexone against morphine analgesia were observed in mouse heat radiant tail-flick assay and in mouse (55 +/- 1) degrees C hot plate test. The displacement of 6 beta-naltrexol and naltrexone on binding to CHO-mu receptor was observed by radioligand binding study.</p><p><b>RESULTS</b>6 beta-naltrexol antagonized morphine analgesia but the potency was (6.1 +/- 1.7)% that of naltrexone. The effective duration of 6 beta-naltrexol was 3-4 times that of naltrexone and the peak time of the response was about 0.5-1 h after s.c. equivalent efficacy dose (ED95) in two models. Like naltrexone, 6 beta-naltrexol was effective by oral administration and the potency ratio of p.o./s.c. was 1/3. As an antagonist to opioid receptor, the displacement of 6 beta-naltrexol was about 12.5% that of naltrexone, which was almost in agreement with the efficacies against morphine analgesia in mouse.</p><p><b>CONCLUSION</b>Compared with naltrexone, 6 beta-naltrexol was less potent but duration was longer.</p>