SPECIFIC NON-OPIATE RECEPTORS FOR BETA-ENDORPHIN
SPECIFIC NON-OPIATE RECEPTORS FOR BETA-ENDORPHIN
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DOI：
10.1126/science.224457
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发表时间：
1979-01-01
期刊：
影响因子：
56.9
通讯作者：
CUATRECASAS, P
中科院分区：
文献类型：
--
作者：
HAZUM, E;CHANG, KJ;CUATRECASAS, P
碘化 βH-[2-D-丙氨酸]内啡肽与培养的人淋巴细胞具有特异性结合。该结合被低浓度的β-内啡肽及其D-丙氨酸2衍生物抑制，但不受阿片激动剂和拮抗剂、或脑啡肽类似物、β-促脂激素、促肾上腺皮质激素或α-黑素细胞刺激激素的影响；这表明β-内啡肽存在特定的非阿片类药物结合位点（受体）。 β-内啡肽的羧基末端区域对于这种结合活性至关重要，因为 α-内啡肽不具有活性。 β-内啡肽可能是一种具有外周生理效应的循环激素，其主要不是通过与阿片或脑啡肽受体的相互作用介导的。
Iodinated βH-[2-D-alanine]endorphin exhibits specific binding to cultured human lymphocytes. The binding is inhibited by low concentrations of β-endorphin and its D-alanine2derivative, but is not affected by opiate agonists and antagonists, or by enkephalin analogs, β-lipotropin, adrenocorticotrophic hormone, or α-melanocyte-stimulating hormone; this suggests the existence of a specific, nonopiate binding site (receptor) for β-endorphin. The carboxy-terminal region of β-endorphin is essential for this binding activity, since α-endorphin is not active. β-Endorphin may be a circulating hormone with peripheral physiological effects that are not primarily mediated through interactions with opiate or enkephalin receptors.