ENANTIOSELECTIVE KAPPA OPIOID BINDING-SITES ON THE MACROPHAGE CELL-LINE, P388D

被引：25

作者：

CARR, DJJ ^{[1
]}

DECOSTA, BR ^{[1
]}

JACOBSON, AE ^{[1
]}

RICE, KC ^{[1
]}

BLALOCK, JE ^{[1
]}

机构：

[1] NIDDK,MED CHEM LAB,BETHESDA,MD 20892

来源：

LIFE SCIENCES | 1991年 / 49卷 / 01期

关键词：

D O I：

10.1016/0024-3205(91)90578-Y

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

A kappa (kappa) opioid binding site has been characterized on the macrophage cell line, P388d1, using the kappa selective affinity ligand, [H-3](1S,2S)-(-)-trans-2-isothiocyanato-N-methyl-N-[2-(1-pyrrolidinyl) cyclohexyl] benzeneacetamide (-)BD166). The kappa site has a relative molecular mass (Mr) of 38,000 under nonreducing conditions and 42,000 under reducing conditions. Moreover, it exhibits enantioselectivity in that 1S,2S-(-)-trans-3,4-dichloro-N-methyl-N-[2-1-pyrrolidinyl)cyclohexyl] benzeneacetamide ((-)U-50,488) blocks [H-3](5-alpha,7-alpha,8-beta)-(-)-N-methyl-N-[7-(1- pyrrolidinyl)-1-oxaspiro-(4,5)-dec-8-yl]benzeneacetamide (U-69,593) binding to P388d1 cells with an IC50 = 7.0 nM whereas 1R,2R-(+)-trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide ((+)U-50,488) blocks [H-3]U-69,593 binding to P388d1 cells with an IC50 = 700 nM.

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页码：45 / 51

页数：7

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