Dickenson A H, Sullivan A F, Roques B P
Department of Pharmacology, University College London, U.K.
Eur J Pharmacol. 1988 Apr 13;148(3):437-9. doi: 10.1016/0014-2999(88)90123-9.
A selective agonist at the delta subtype of the opioid receptor (Tyr-D-Ser(Otbu)-Gly-Phe-Leu-Thr) (DSTBULET), and kelatorphan, a mixed peptidase inhibitor which can protect endogenous enkephalins were applied together onto to the lumbar spinal cord of the intact anaesthetized rat. The combined administration of these agents produced inhibitions of the responses of dorsal horn neurones activated by peripheral stimulation which were no greater than the inhibitions with either the agonist or peptidase inhibitor alone (50-60% inhibitions). The results indicate that endogenous opioids protected by kelatorphan and delta opioid receptor agonists act on a common receptor site to produce spinal antinociception.
一种阿片受体δ亚型的选择性激动剂(酪氨酰-D-丝氨酸(叔丁氧羰基)-甘氨酰-苯丙氨酰-亮氨酰-苏氨酸)(DSTBULET),以及一种可保护内源性脑啡肽的混合肽酶抑制剂凯拉托芬,被一起应用于完整麻醉大鼠的腰脊髓。这些药物联合给药对由外周刺激激活的背角神经元反应的抑制作用,并不比单独使用激动剂或肽酶抑制剂时的抑制作用更强(抑制率为50 - 60%)。结果表明,受凯拉托芬保护的内源性阿片类物质和δ阿片受体激动剂作用于共同的受体位点以产生脊髓镇痛作用。