β-内啡肽。双头及相关类似物的合成与性质
Beta-Endorphin. Synthesis and properties of double-headed and related analogs.
作者信息
Yamashiro D, Li C H, Nicolas P, Hammonds R G
出版信息
Int J Pept Protein Res. 1982 Apr;19(4):348-53.
PMID:6288593
Abstract
A double-headed analog of human beta-endorphin (betah-EP), N,N'-bis (beta-endorphinyl)-cystine (II), has been synthesized by the solid-phase method, along with betah-EP-Cys(CH2CONH2)-OH (I) and [Tyr31]-betah-EP (III). Their relative potencies in a radioreceptor-binding assay were: betah-EP, 100; II, 235; I, 170; and III, 204. In the tail-flick test for analgesic activity their relative potencies were: betah-EP, 100; II, 86; I, 93; and III, 116.
摘要
通过固相法合成了人β-内啡肽（β-EP）的双头类似物N，N'-双（β-内啡肽基）-胱氨酸（II），以及β-EP-Cys(CH2CONH2)-OH（I）和[酪氨酸31]-β-EP（III）。它们在放射受体结合试验中的相对效力为：β-EP，100；II，235；I，170；III，204。在甩尾试验中它们的镇痛活性相对效力为：β-EP，100；II，86；I，93；III，116。
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