SPECIFIC AFFINITY LABELING OF MU-OPIOID RECEPTORS IN RAT-BRAIN BY S-ACTIVATED SULFHYDRYLDIHYDROMORPHINE ANALOGS

被引：8

作者：

SAGARA, T

OKAMURA, M

SHIMOHIGASHI, Y

OHNO, M

KANEMATSU, K

机构：

[1] KYUSHU UNIV 62,FAC PHARMACEUT SCI,INST SYNTHET ORGAN CHEM,HIGASHI KU,FUKUOKA 81282,JAPAN

[2] KYUSHU UNIV 33,FAC SCI,DEPT CHEM,BIOCHEM LAB,HIGASHI KU,FUKUOKA 81282,JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 15期

关键词：

D O I：

10.1016/0960-894X(95)00263-S

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

S-Activated sulfhydryldihydromorphine analogs 1 and 2 were synthesized. In the rat brain receptor binding assays, both 1 and 2 exhibited considerably high affinities for mu opioid receptors (IC50; 1 = 31.1 nM, 2 = 10.7 nM). However, when each analog was incubated with membranes for the purpose of getting disulfide bridgings, 1 (EC(50) = 58 nM) was found to affinity-label the mu receptors about 30 times more effectively than 2 (EC(50) = 1700 nM).

引用

页码：1609 / 1614

页数：6

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