Specific Affinity Labeling of μ Opioid Receptors by S-Activated Enkephalin Analog Containing p-Nitrophenylalanine
Specific Affinity Labeling of μ Opioid Receptors by S-Activated Enkephalin Analog Containing p-Nitrophenylalanine
复制标题
含有对硝基苯丙氨酸的 S-激活脑啡肽类似物对 μ 阿片受体的特异性亲和力标记
DOI：
10.1246/bcsj.67.296
复制
发表时间：
1994
期刊：
影响因子：
--
通讯作者：
M. Kondo
中科院分区：
文献类型：
--
作者：
T. Yasunaga;Y. Shimohigashi;H. Kodama;M. Miyazaki;M. Nagaishi;M. Ohno;M. Kondo
对硝基苯丙氨酸（Phe（p-NO2））取代[D-Ala 2，Leu（CH 2S-Npys）5]脑啡肽的Phe 4。在大鼠脑受体结合试验中，含Npys的Phe（p-NO2）4-和Phe 4-脑啡肽对μ受体的亲和力几乎没有变化（IC 50 = 16-21 nM）。然而，当膜与每种类似物孵育时，Phe（p-NO2）4-脑啡肽（EC 50 = 6.90 nM）可以比Phe 4-脑啡肽更有效地标记μ受体约三倍。
p-Nitrophenylalanine (Phe(p-NO2)) was incorporated in place of Phe4 of [D-Ala2, Leu(CH2S-Npys)5]enkephalin. In the rat brain receptor binding assay, Npys-containing Phe(p-NO2)4- and Phe4-enkephalins exhibited almost unchanged affinities for μ receptors (IC50 = 16—21 nM). However, when the membrane was incubated with each analog, Phe(p-NO2)4-enkephalin (EC50 = 6.90 nM) could label the μ receptors about three times more effectively than Phe4-enkephalin.