Honoré T, Nielsen M, Braestrup C
Life Sci. 1984 Nov 26;35(22):2257-67. doi: 10.1016/0024-3205(84)90467-3.
Specific binding of the BZ-receptor ligand 3H-DMCM to rat cortical membranes was dramatically enhanced by preincubation of the homogenate with 0.1 mM silver (Ag+) nitrate. The binding was completely inhibited by midazolam. Nevertheless, the pharmacological specificity of the Ag+-enhanced 3H-DMCM binding was different from that of BZ-receptors. Furthermore, the Bmax value, the regional distribution and the molecular target size determined by radiation inactivation analysis of the Ag+-enhanced binding site were different from those of BZ-receptors. The results indicate that Ag+-enhanced 3H-DMCM binding represent a high affinity metal complex formation between 3H-DMCM and an unknown brain specific protein of approximately 100,000 daltons molecular weight.
通过将匀浆与0.1 mM硝酸银(Ag+)预孵育,BZ受体配体3H-DMCM与大鼠皮质膜的特异性结合显著增强。该结合被咪达唑仑完全抑制。然而,Ag+增强的3H-DMCM结合的药理学特异性与BZ受体不同。此外,通过对Ag+增强的结合位点进行辐射失活分析确定的Bmax值、区域分布和分子靶标大小与BZ受体不同。结果表明,Ag+增强的3H-DMCM结合代表了3H-DMCM与一种分子量约为100,000道尔顿的未知脑特异性蛋白之间形成的高亲和力金属复合物。