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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。
The 125I-IPIN probe was prepared by chloramine-T oxidation method, and its interaction with β-adrenergic receptor (β-AR) in mouse brain and lung tissue Binding characteristics. The results of equilibrium binding assay, dissociation kinetics assay and competitive inhibition assay showed that the binding of 125Ⅰ-IPIN to the above tissue β-AR was saturable, reversible and specific. The equilibrium dissociation constant (KD) was 0.143 ± 0.042nM (brain, n = 14), 0.180 ± 0.072nM (lung, n = 13) and the maximum binding capacity (Bmax) was 37.04 ± 6.68 fmol / , 370.05 ± 86.36 fmol / mg protein (lung), and the Hill coefficient was close to 1. When the ligand concentration was in the range of 0.01 ~ 0.3 nM. Scatchard analysis is in line.