3-甲基芬太尼——一个高选择性的μ阿片受体激动剂

3-Methylfentanyl——A Potent Selective μ Opioid Receptor Agonist

芬太尼、３－甲基芬太尼和羟甲芬太尼都是强镇痛剂。本文主要观察了３－甲基芬太尼，芬太尼和羟甲芬太尼和镇痛和对阿片受体的选择性。结果表明，芬太尼、３－甲基芬太尼和羟甲芬太尼的镇冯强度分别是吗啡的３００、１５００和６３００倍。

Fentanyl, 3-methylfentanyl and ohmefentanyl are potent analgesics. Fentanyl and ohme-fentanyl are μ. opioid receptor selective agonists. 3-methylfentanyl may be also a μ opioid receptor agonist. However, the analgesia activities and selectivity for opioid receptors of 3-methylfentanyl were also observed. These results showed 3-methylfentanyl is a potent analgesic and selective μ opioid receptor agonist. 3-methylfentanyl analgesia activity is 1500 times as potent as morphine. In isolated organs, the inhibitory action of 3-methylfentanyl is potent on guinea pig ileum and mice vas deferens. The guinea pig ileum contained mainly μ and K opioid receptors, but the mice vas deferens contained mainly S and ft opioid receptors ,so 3-methylfentanyl may be a μ opioid receptor agonist. In binding assay,the inhibitory action of 3-methylfentanyl on [3H]DAGO is significantly higher than on [3H]DPDPE. DAGO is a μ opioid receptor selectiv agonist,but DPDPE is a S opioid receptor selective agonist. These results suggested that 3-methylfentanyl might be a potent analgesic and selective ft opioid receptor agonist. The ft opioid receptor is involved in mediating the analgesia effect of 3-methylfentanyl.