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本项研究探素了用氚标的β-受体拮抗剂~3H-双氢心得舒与大鼠中脑上丘平面冰冻切片进行结合实验的条件。实验得出配体与脑切片的最大特异性结合量为17.3±4.5 fmol/mg,组织干重,表观平衡解离常数为5.8±0.6nM,Hill系数为0.93±0.3,结合速率常数为0.112±0.025nM~(-1)·min~(-1),解离速率常数为0.69±0.07min~(-1),心得安与配体竞争结合的IC_(50)为1.00±0.15×10~(-8)M,心得宁的IC~(50)为167±0.22×10~(-8)M,异丙肾上慷素的IC_(50)为1.32±0.3×10~(-6)M。这些结果与用组织匀浆进行结合实验所得结果近似,表明在合适的条件下用冰冻组织切片进行β-受体结合实验是可行的。
This study explored the tritiated β -receptor antagonist ~ 3H-dihydrochlorothiazide and rat midbrain plane freezing section of the conditions for binding experiments. The maximal specific binding capacity between the ligand and the brain slices was 17.3 ± 4.5 fmol / mg, the dry weight of the tissue, the apparent equilibrium dissociation constant was 5.8 ± 0.6nM, the Hill coefficient was 0.93 ± 0.3 and the binding rate constant was 0.112 ± 0.025nM -1 min -1 and the rate constant of dissociation was 0.69 ± 0.07min -1. The IC 50 of the combination of propranolol and ligand was 1.00 ± 0.15 × 10 ~ (8) M, and the IC50 value of dextromethorphan was 167 ± 0.22 × 10 ~ (-8) M. The IC50 of isoprenaline was 1.32 ± 0.3 × 10 ~ (-6) M . These results are similar to the results obtained with the binding experiments with tissue homogenization, indicating that it is feasible to perform beta-receptor binding experiments with frozen tissue sections under appropriate conditions.