CONFORMATIONALLY RESTRICTED ANALOGS OF SOMATOSTATIN WITH HIGH MU-OPIATE RECEPTOR SPECIFICITY
CONFORMATIONALLY RESTRICTED ANALOGS OF SOMATOSTATIN WITH HIGH MU-OPIATE RECEPTOR SPECIFICITY
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DOI：
10.1073/pnas.82.1.236
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发表时间：
1985-01-01
影响因子：
11.1
通讯作者：
YAMAMURA, HI
中科院分区：
文献类型：
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作者：
PELTON, JT;GULYA, K;YAMAMURA, HI
制备了一系列环状构象受限的生长抑素类似物，并测试了它们抑制[~3H]纳洛酮和[D-丙氨酸，D-亮氨酸][~3H]脑啡肽与大鼠脑膜结合的能力。给出了最强的类似物；它对阿片受体有很高的亲和力([~3H]纳洛酮的IC50=3.5 nM)，是生长抑素的7800倍。环八肽也表现出很高的阿片受体选择性，其IC50([D-丙氨酸，D-亮氨酸]脑啡肽)/IC50(纳洛酮)为271。生长抑素类似物对阿片受体的高亲和力和选择性可用于研究阿片受体的生理作用(S)。
A series of cyclic, conformationally restricted analogs of somatostatin were prepared and tested for their ability to inhibited the binding of [3H]naloxone and [D-Ala2, D-Leu5][3H]enkephalin to rat brain membranes. The most potent analog is given; it exhibited high affinity for .mu.-opiate receptors (IC50 [mean inhibitory concentration] value of [3H]naloxone = 3.5 nM), being 7800 times more petent than somatostatin. The cyclic octapeptide also displayed high .mu.-opiate receptor selectivity with an IC50 ([D-Ala2, D-Leu5]enkephalin)/IC50 (naloxone) ratio of 271. The high affinity and selectively of the somatostatin analog for .mu.g-opiate receptors may be of use in examining the physiological role(s) of the .mu.-opiate receptor.