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最近几年,对内啡肽和脑啡肽虽做了大量研究,但仍有些错误概念未予澄清。第一、内啡肽和脑啡肽在血中或组织中受氨基肽酶迅速作用,立刻转变为无活性的去酪化合物。实验证明,这一概念有两方面错误:(1)去酪~1—甲啡肽和去酪~1—内啡肽并不是无活性化合物,它们不作用于阿片受体,但却有强烈的行为效应。(2)β-内啡肽能在血液中循环而不被立即破坏。大鼠注射~3H标记的人β-内啡肽后45分钟,血浆中50%的放射性仍来自于完整的β-内啡肽。据认为,β-内啡肽N-端的裂解是产生行为活性衍生物的一个选择性代谢途径的开始。
In recent years, a large number of studies have been done on endorphins and enkephalin, but some erroneous concepts remain unclear. First, endorphins and enkephalin are rapidly acted by aminopeptidase in the blood or tissues and are immediately converted to inactive chelating compounds. Experiments show that this concept has two mistakes: (1) to the cheese ~ 1-methamorphin and cheese ~ 1 ~ endorphin is not inactive compounds, they do not act on opioid receptors, but there is a strong Behavioral effects. (2) β-endorphin in the blood circulation without being destroyed immediately. Forty-five minutes after the ~ 3H-labeled human beta-endorphin was injected into the rat, 50% of the radioactivity in the plasma still came from the intact beta-endorphin. It is believed that the cleavage of the N-terminal of the [beta] -endorphin is the beginning of a selective metabolic pathway that produces a viable derivative.