^(125)I-(±)心得静的制备及其与小鼠肺、脑β受体的结合特性  

The Preparation of ^(125)I-pindolol and Its Binding Characteristics to Beta-adrenoceptors of Mouse Lung and Brain

作　　者：张世德[1] 黎明涛[1] 敖屹 夏宗勤[2] 易宁育[2] 

机构地区：[1]上海第二医科大学细胞调控研究室 [2]上海第二医科大学

出　　处：《上海第二医科大学学报》1990年第4期281-284,共4页Acta Universitatis Medicinalis Secondae Shanghai

摘　　要：用氯胺-T氧化法制备[125Ⅰ]-心得静(125Ⅰ-IPIN)为探针,研究其与小鼠脑、肺组织β-肾上腺素能受体(β-adrenergic receptor,β-AR)的结合特性。平衡结合试验、结合解离动力学试验及竞争抑制试验结果表明:125Ⅰ-IPIN与上述组织β-AR的结合具有可饱和性、可逆性和特异性。其平衡解离常数(KD)为0.143±0.042nM(脑,n=14),0.180±0.072nM(肺,n=13);最大结合容量(Bmax)为37.04±6.68 fmol/mg蛋白(脑),370.05±86.36 fmol/mg蛋白(肺);Hill系数接近1.当配基浓度在0.01～0.3nM的范围内。Scatchard分析呈一直线。In this study, a chloramine-T method was established for the preparation of ^(125)I-iodopindolol, a special radioligand reported to have high affinity to betaadrenergic receptors. The characteristics of the product were examined by saturation experiment, kinetic experiment and competitive binding experiment. The results showed that the binding of the radioligand to the beta adrenoceptors of mouse brain and lung was saturable, reversible and highly specific. Scatchard analysis displayed a straight line and the Hill coefficient was close to 1. Using this product, the densities of beta-adrenoceptors of mouse brain and lung were 37.04±6.68 and 370.05±86.36 fmol/mg protein while the equilibrium dissociation constants were 0.143±±0.042 and 0.180±0.072nM respectively.

关 键 词：碘125 心得静 Β-受体 肺 脑 

分 类 号：R817.1[医药卫生—影像医学与核医学]