Li C H, Yamashiro D, Tseng L F, Loh H H
Int J Pept Protein Res. 1978 Feb;11(2):154-8. doi: 10.1111/j.1399-3011.1978.tb02834.x.
Three analogs of beta-endorphin have been synthesized by the solid-phase method: betac-endorphin-(1--5)-(28--31), betac-endorphin-(6--31) and betah-endorphin-(1--5)-(16--31). The analgesic activities of these synthetic peptides relative to that of the parent molecule are reported. All three peptides at high doses exhibit either no or much weaker analgesic activity than beta-endorphin. These data suggest that the entire beta-endorphin molecule is necessary for full in vivo analgesic activity.
通过固相法合成了三种β-内啡肽类似物:βc-内啡肽-(1--5)-(28--31)、βc-内啡肽-(6--31)和βh-内啡肽-(1--5)-(16--31)。报道了这些合成肽相对于母体分子的镇痛活性。所有这三种肽在高剂量时均表现出与β-内啡肽相比无镇痛活性或镇痛活性弱得多的情况。这些数据表明,完整的β-内啡肽分子对于体内充分的镇痛活性是必需的。