The two prototypical μ opioid agonists morphine and alfentanil were tested in a warm-water tail withdrawal antinociception assay performed at 45 o C, 50 o C and 55 o C in rhesus monkeys before and after administration of the irreversible opioid antagonist clocinnamox (0.1 mg/kg s.c.). Clocinnamox acutely decreased the available opioid receptors by up to 90%. Receptor numbers returned to control levels with a half-life of approximately one week. The affinity, efficacy, the maximum effect, and the stimulus-response transduction factor did not change significantly over time. The efficacy of alfentanil was always 2-3-fold higher than that for morphine, the efficacies of both agonists being higher at lower temperatures. The affinity of alfentanil was 29-fold higher than that of morphine
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