Endomorphin-1 and endomorphin-2 are partial agonists at the human μ-opioid receptor
Endomorphin-1 and endomorphin-2 are partial agonists at the human μ-opioid receptor
复制标题
DOI：
10.1016/s0014-2999(98)00117-4
复制
发表时间：
1998-04-03
影响因子：
5
通讯作者：
Yamamura, HI
中科院分区：
文献类型：
--
作者：
Hosohata, K;Burkey, TH;Yamamura, HI
最近，鉴定出优先与μ阿片受体结合的两种四肽配体，并将其命名为内吗啡-1和内吗啡-2。我们检查了这些肽刺激人 CL-阿片受体转染的 B82 成纤维细胞中 G 蛋白活化的能力，通过 [S-35]GTP gamma S 与细胞膜的结合来测量。与 mu 选择性激动剂 [D-Ala(2),N-Me-Phe(4), Gly-ol(5)]脑啡肽 (DAMGO) 相比，内吗啡肽-1 和 -2 在此检测系统中均充当部分激动剂。此外，内吗啡的功效与吗啡相似。这些发现表明，内吗啡肽对 mu-阿片受体具有与吗啡相似的活性，并表明这些肽具有调节体内神经元活动的潜力。 (C) 1998 Elsevier Science B.V.
Recently two tetrapeptide ligands that bind preferentially to the mu-opioid receptor were identified and named endomorphin-1 and endomorphin-2. We examined the ability of these peptides to stimulate G protein activation in human CL-opioid receptor transfected B82 fibroblasts as measured by [S-35]GTP gamma S binding to cell membranes. Both endomorphin-1 and -2 act as partial agonists in this assay system compared with the mu-selective agonist [D-Ala(2),N-Me-Phe(4), Gly-ol(5)]enkephalin (DAMGO). In addition, endomorphins demonstrate efficacy similar to morphine. These findings demonstrate that endomorphin peptides have similar activity at the mu-opioid receptor as morphine and suggest that these peptides have the potential to modulate neuronal activity in vivo. (C) 1998 Elsevier Science B.V.