Synthesis and analgesic activity of human beta-endorphin.
Synthesis and analgesic activity of human beta-endorphin.
复制标题
人β-内啡肽的合成和镇痛活性。
DOI：
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发表时间：
1977
影响因子：
7.3
通讯作者：
H. Loh
中科院分区：
文献类型：
--
作者：
C. Li;D. Yamashiro;L. Tseng;H. Loh
本文报道了人β-内啡肽的固相合成。基于起始树脂，实现32%的产率。合成产物在分配色谱、纸电泳、薄层色谱、圆盘电泳、氨基酸组成和胰蛋白酶图谱中表现为均一肽。合成β h-内啡肽具有抗伤害性，如通过小鼠甩尾、热板和扭体试验所估计的。当集中使用时，β h-内啡肽的效力是吗啡的17-48倍。静脉注射时，它的效力是吗啡的3.4倍。镇痛反应可被特异性阿片拮抗剂纳洛酮阻断。
The solid-phase synthesis of human beta-endorphin is described. A yield of 32% is achieved based on starting resin. The synthetic product behaves as a homogeneous peptide in partition chromatography, paper electrophoresis, thin-layer chromatography, disc electrophoresis, amino acid composition, and a tryptic map. The synthetic beta h-endorphin possesses antinociceptive properties as estimated by the tail-flick, hot-plate, and writhing tests in mice. When applied centrally, beta h-endorphin is 17-48 times more potent than morphine. It is 3.4 times more potent than morphine when injected intravenously. The analgesic responses are blocked by the specific opiate antagonist, naloxone.