Dickenson A H, Sullivan A, Feeney C, Fournie-Zaluski M C, Roques B P
Neurosci Lett. 1986 Dec 12;72(2):179-82. doi: 10.1016/0304-3940(86)90076-5.
Kelatorphan, a full inhibitor of aminopeptidases, enkephalinase and dipeptidylaminopeptidase, enzymes which degrade the enkephalins, produced inhibitions (around 50%) of dorsal horn C fibre evoked responses in the rat, following local application. The inhibitions were reversed by the selective delta-opiate receptor antagonists ICI 174,864. Furthermore the inhibitions produced by two doses of Tyr-D-Ala-Gly-MePhe-Gly-ol (DAGO), a potent selective mu-opiate receptor agonist, were not altered in the presence of kelatorphan, so demonstrating an additive effect of the mu-agonist and the enzyme inhibitor. The inhibitions produced by the enzyme inhibitor would seem due to an increased availability of endogenous opioids, presumably the enkephalins which act via the delta-opiate receptor.
凯拉托芬是一种氨肽酶、脑啡肽酶和二肽基氨肽酶的完全抑制剂，这些酶可降解脑啡肽。在大鼠局部应用后，它对背角C纤维诱发反应产生抑制作用（约50%）。选择性δ-阿片受体拮抗剂ICI 174,864可逆转这种抑制作用。此外，强效选择性μ-阿片受体激动剂 Tyr-D-Ala-Gly-MePhe-Gly-ol（DAGO）的两剂所产生的抑制作用，在有凯拉托芬存在的情况下并未改变，因此证明了μ-激动剂和酶抑制剂的相加作用。酶抑制剂所产生的抑制作用似乎是由于内源性阿片类物质（可能是通过δ-阿片受体起作用的脑啡肽）的可用性增加所致。
