Raisman R, Briley M, Langer S Z
Naunyn Schmiedebergs Arch Pharmacol. 1979 Jul;307(3):223-6. doi: 10.1007/BF00505937.
The alpha-adrenoceptor ligand, 3H-WB 4101 binds to a single population of independent sites in the rat heart ventricle. These sites are not affected by chemical sympathectomy with 6-hydroxydopamine and thus appear to be located postsynaptically. The relative order of potencies for displacement of 3H-WB 4101 binding:prazosin greater than phentolamine greater than yohimbine, is characteristic of that of the alpha 1 type of adrenoceptors. In heart ventricle 3H WB-4101 thus seems to label specifically postsynaptically located alpha 1-adrenoceptors. The significance of the specificity of this ligand is discussed with relevance to its use in the central nervous system.
α-肾上腺素能受体配体3H-WB 4101与大鼠心室中的单一独立位点群结合。这些位点不受6-羟基多巴胺化学交感神经切除术的影响,因此似乎位于突触后。3H-WB 4101结合置换的效力相对顺序为:哌唑嗪大于酚妥拉明大于育亨宾,这是α1型肾上腺素能受体的特征。因此,在心室中,3H-WB 4101似乎特异性标记突触后定位的α1-肾上腺素能受体。结合其在中枢神经系统中的应用,讨论了该配体特异性的意义。