Snell P H, Snell C R
MRC Neuroendocrinology Unit, Newcastle General Hospital, Westgate Road, Newcastle upon Tyne NE4 6BE, U.K.
Neurochem Int. 1983;5(2):245-9. doi: 10.1016/0197-0186(83)90121-3.
Adenosine binding sites on 108CC15 neuroblastoma x glioma hybrid cells and rat brain membranes were investigated using [(3)H]adenosine as labelled ligand. Both the hybrid cells and brain membranes were found to have a high affinity binding site, K(d) 0.8 and 3 nM respectively. The same ligand was used to demonstrate two lower affinity binding sites on brain membranes, K(d)s 1.4 and 29.1 ?M and a single low affinity site on the hybrid cells, K(d) 2.6 ?M. Structure activity studies of the low affinity binding site on hybrid cells showed this to be an 'R' adenosine receptor of the A(2) subtype. It is concluded that [(3)H]adenosine can be used to demonstrate both high and low affinity binding sites and that 108CC15 hybrid cells provide a valuable system for studying adenosine receptors.
使用[³H]腺苷作为标记配体,研究了108CC15神经母细胞瘤x胶质瘤杂交细胞和大鼠脑膜上的腺苷结合位点。发现杂交细胞和脑膜均具有高亲和力结合位点,解离常数(K(d))分别为0.8和3 nM。使用相同的配体证明脑膜上有两个低亲和力结合位点,解离常数分别为1.4和29.1 μM,杂交细胞上有一个低亲和力位点,解离常数为2.6 μM。对杂交细胞上低亲和力结合位点的构效关系研究表明,该位点是A(2)亚型的“R”腺苷受体。得出的结论是,[³H]腺苷可用于证明高亲和力和低亲和力结合位点,并且108CC15杂交细胞为研究腺苷受体提供了一个有价值的系统。