ANALGESIA INDUCED INVIVO BY CENTRAL ADMINISTRATION OF ENKEPHALIN IN RAT
ANALGESIA INDUCED INVIVO BY CENTRAL ADMINISTRATION OF ENKEPHALIN IN RAT
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DOI：
10.1038/260625a0
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发表时间：
1976-01-01
期刊：
影响因子：
64.8
通讯作者：
STEIN, L
中科院分区：
文献类型：
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作者：
BELLUZZI, JD;GRANT, N;STEIN, L
脑啡肽是大脑 1-4 中的天然阿片受体激动剂，已被 Hugheset 等人 5 鉴定为两种五肽的混合物：H–Tyr–Gly–Gly–Phe–Met–OH（甲硫氨酸–脑啡肽）和 H–Tyr–Gly–Gly–Phe–Leu–OH（亮氨酸–脑啡肽）。这两种肽都模仿吗啡阻断小鼠输精管和豚鼠回肠电诱发收缩的能力，并且都抑制脑匀浆中阿片拮抗剂3H-纳洛酮的立体特异性受体结合5。基于这一证据和其他 6-8 证据，有人提出 2,9,10 脑啡肽受体可能是吗啡类药物发挥镇痛作用的位点，并且脑啡肽本身可能是大脑系统中抑制疼痛或镇痛的调节剂或递质。与这一建议一致，我们发现，当通过大鼠侧脑室中永久留置的插管给予蛋氨酸-脑啡肽和亮氨酸-脑啡肽时，会在体内引起深度镇痛，这种镇痛作用可被纳洛酮完全逆转。
ENKEPHALIN, a natural opiate receptor agonist in brain1–4, has been identified by Hugheset al.5as a mixture of two pentapeptides : H–Tyr–Gly–Gly–Phe–Met–OH (methionine–enkephalin) and H–Tyr–Gly–Gly–Phe–Leu–OH (leucine–enkephalin). Both peptides mimic the ability of morphine to block electrically evoked contractions of mouse vas deferens and guinea pig ileum, and both inhibit the stereospecific receptor binding of the opiate antagonist3H-naloxone in brain homogenates5. On the basis of this and other6–8evidence, it has been proposed2,9,10that enkephalin receptors may be sites at which morphine-like drugs exert their analgesic actions, and that the enkephalins themselves may be modulators or transmitters in brain systems for pain suppression or analgesia. Consistently with this suggestion, we find that methionine–enkephalin and leucine–enkephalin, when administered through permanently indwelling cannulae in the lateral ventricles of rats, induce a profound analgesiain vivothat is fully reversible by naloxone.