Saksida L M, Galea L A, Kavaliers M
Department of Psychology, University of British Columbia, Vancouver, Canada.
Peptides. 1993 Jul-Aug;14(4):763-5. doi: 10.1016/0196-9781(93)90110-3.
In vertebrates the effects of endogenous opioid peptides are limited by proteolytic enzymes such as endopeptidase 24.11 (enkephalinase), which cleaves the Gly-Phe bonds in both methionine- and leucine-enkephalin. SCH 34826 ((S)-N-[n-[1-[(2,2-dimethyl-1,3-dioxolan-4yl) methoxy]carbonyl]-2-phenylethyl]-L-phenylalanine-B-alanine) is a potent, highly specific, enkephalinase inhibitor that has marked analgesic effects in mammals. The present study examined the effects of SCH 34826 on opioid-mediated aversive thermal (nociceptive) response of an invertebrate, the land snail, Cepaea nemoralis. SCH 34828 had significant, dose-related antinociceptive effects in Cepaea that were reduced by naloxone and completely blocked by the specific data opiate antagonist, ICI-174,864, and only weakly affected by the specific kappa opiate antagonist nor-binaltrophimine. These findings with SCH 34826 suggest that an enkephalinase similar to that in vertebrates is present and involved in the mediation of opioid (enkephalin) activity in the snail, Cepaea.
在脊椎动物中，内源性阿片肽的作用受到蛋白水解酶的限制，比如内肽酶24.11（脑啡肽酶），它能裂解甲硫氨酸脑啡肽和亮氨酸脑啡肽中的甘氨酰-苯丙氨酸键。SCH 34826（(S)-N-[n-[1-[(2,2-二甲基-1,3-二氧戊环-4-基)甲氧基]羰基]-2-苯乙基]-L-苯丙氨酸-β-丙氨酸）是一种强效、高度特异性的脑啡肽酶抑制剂，在哺乳动物中具有显著的镇痛作用。本研究检测了SCH 34826对无脊椎动物——陆地蜗牛（盖罩大蜗牛）中阿片介导的厌恶性热（伤害性）反应的影响。SCH 34828在盖罩大蜗牛中具有显著的、剂量相关的抗伤害感受作用，这种作用可被纳洛酮减弱，并被特异性δ阿片拮抗剂ICI-174,864完全阻断，而仅受到特异性κ阿片拮抗剂去甲双丙吗啡的微弱影响。这些关于SCH 34826的研究结果表明，在盖罩大蜗牛中存在一种与脊椎动物中类似的脑啡肽酶，它参与了阿片（脑啡肽）活性的介导过程。
