Goodall J, Hughes I E, Mackay D
Br J Pharmacol. 1986 Jul;88(3):645-51. doi: 10.1111/j.1476-5381.1986.tb10246.x.
The effects of the opioid receptor agonist RX783006 and of the opioid receptor partial agonist (+)-meptazinol have been examined on electrically induced twitch responses of the guinea-pig isolated ileum and of the mouse isolated vas deferens. Log10 concentration-tissue state curves were determined for (+)-meptazinol and RX783006, alone, in combination and in the presence of naloxone (30 nM). Analysis of these log10 concentration-tissue state curves using the null equations derived and tested in the preceding paper indicates that the opioid agonist action of (+)-meptazinol on mouse vas deferens is quantitatively similar to that on guinea-pig ileum. The results also suggest that (+)-meptazinol acts as a functional antagonist on the guinea-pig ileum as well as on the mouse vas deferens. The potency of (+)-meptazinol relative to RX783006 has been measured by an indirect method which should eliminate any functional antagonistic action of (+)-meptazinol. This method gives a relative potency of (+)-meptazinol in both tissues which is three to six times greater than that measured directly on guinea-pig ileum. This discrepancy may be due to experimental error but it may also indicate that direct measurements on guinea-pig ileum underestimate the agonist potency of this compound on opioid receptors.
已研究了阿片受体激动剂RX783006和阿片受体部分激动剂(+)-美普他酚对豚鼠离体回肠和小鼠离体输精管电诱导抽搐反应的影响。测定了(+)-美普他酚和RX783006单独、联合以及在纳洛酮(30 nM)存在时的log10浓度-组织状态曲线。使用前文推导和测试的无效方程对这些log10浓度-组织状态曲线进行分析表明,(+)-美普他酚对小鼠输精管的阿片激动剂作用在数量上与对豚鼠回肠的作用相似。结果还表明,(+)-美普他酚在豚鼠回肠和小鼠输精管上均作为功能性拮抗剂起作用。已通过一种间接方法测量了(+)-美普他酚相对于RX783006的效价,该方法应消除(+)-美普他酚的任何功能性拮抗作用。该方法得出(+)-美普他酚在两种组织中的相对效价,比直接在豚鼠回肠上测量的效价高3至6倍。这种差异可能是由于实验误差,但也可能表明对豚鼠回肠的直接测量低估了该化合物对阿片受体的激动剂效价。