巨噬细胞系P388d1上的对映选择性κ阿片受体结合位点。
Enantioselective kappa opioid binding sites on the macrophage cell line, P388d1.
作者信息
Carr D J, DeCosta B R, Jacobson A E, Rice K C, Blalock J E
机构信息
Department of Physiology and Biophysics, University of Alabama Birmingham 35294.
出版信息
Life Sci. 1991;49(1):45-51. doi: 10.1016/0024-3205(91)90578-y.
A kappa (kappa) opioid binding site has been characterized on the macrophage cell line, P388d1, using the kappa selective affinity ligand, [3H] (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 [3H](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 [3H]U-69,593 binding to P388d1 cells with an IC50 = 7000 nM.
已使用κ选择性亲和配体3H-(-)-反式-2-异硫氰酸-N-甲基-N-[2-(1-吡咯烷基)环己基]苯乙酰胺(-)BD166对巨噬细胞系P388d1上的κ阿片样物质结合位点进行了表征。在非还原条件下，κ位点的相对分子质量（Mr）为38,000，在还原条件下为42,000。此外，它表现出对映选择性，即1S,2S-(-)-反式-3,4-二氯-N-甲基-N-[2-(1-吡咯烷基)环己基]苯乙酰胺((-)-U-50,488)以IC50 = 7.0 nM阻断3H-(-)-N-甲基-N-[7-(1-吡咯烷基)-1-氧杂螺-(4,5)-癸-8-基]苯乙酰胺(U-69,593)与P388d1细胞的结合，而1R,2R-(+)-反式-3,4-二氯-N-甲基-N-[2-(1-吡咯烷基)环己基]苯乙酰胺((+)U-50,488)以IC50 = 7000 nM阻断[3H]U-69,593与P388d1细胞的结合。
Zotero 插件