Ary T E, Frank G B
Can J Physiol Pharmacol. 1983 Nov;61(11):1361-7. doi: 10.1139/y83-195.
Intracellular microelectrode studies were conducted to investigate the actions of the partial agonist-antagonist nalorphine at an opiate receptor on functional frog skeletal muscle fiber membranes. In high bath concentrations (greater than or equal to 10(-4) M), nalorphine alone produces agonist actions similar to the "full" opiate agonists. These actions were (i) to depress both the sodium and potassium (gNa and gK) conductance increases due to electrical stimulation by a nonspecific local anestheticlike mechanism and (ii) to depress gNa by a specific opiate receptor mediated mechanism. In a much lower bath concentration (1 X 10(-8) M) nalorphine acts to antagonize the specific opiate receptor mediated depression of gNa produced by the "full" agonist meperidine. Thus in this preparation nalorphine, "the partial antagonist," has the same actions as naloxone, which is often considered to be a full antagonist. The quantitative differences observed in the effects of these two opiate antagonists are discussed.
进行了细胞内微电极研究，以探究部分激动剂-拮抗剂烯丙吗啡在阿片受体上对功能性青蛙骨骼肌纤维膜的作用。在高浴槽浓度（大于或等于10⁻⁴ M）下，单独的烯丙吗啡产生类似于“完全”阿片激动剂的激动剂作用。这些作用包括：（i）通过非特异性局部麻醉样机制抑制由于电刺激引起的钠和钾（gNa和gK）电导增加；（ii）通过特定的阿片受体介导机制抑制gNa。在低得多的浴槽浓度（1×10⁻⁸ M）下，烯丙吗啡起到拮抗“完全”激动剂哌替啶产生的gNa特异性阿片受体介导的抑制作用。因此，在该制剂中，“部分拮抗剂”烯丙吗啡与通常被认为是完全拮抗剂的纳洛酮具有相同的作用。讨论了在这两种阿片拮抗剂作用中观察到的定量差异。
