MacDermot J, Barnes P J, Waddell K A, Dollery C T, Blair I A
Eur J Pharmacol. 1981 Oct 22;75(2-3):127-30. doi: 10.1016/0014-2999(81)90071-6.
[3H] Prostacyclin bound to membranes of guinea pig lung. Specific binding was saturable, and the results revealed two receptor classes (Kd =16 nM and 258 nM). The binding capacity of the high affinity site was 105 fmol [3H]prostacyclin per mg of membrane protein, and that of the low affinity site was 1257 fmol per mg membrane protein. A comparison of selected prostaglandins as inhibitors of [3H] prostacyclin binding revealed some of the structural requriements of the ligand for occupation of the high affinity receptor.
[3H]前列环素与豚鼠肺膜结合。特异性结合具有饱和性,结果显示存在两类受体(解离常数分别为16 nM和258 nM)。高亲和力位点的结合容量为每毫克膜蛋白105 fmol [3H]前列环素,低亲和力位点的结合容量为每毫克膜蛋白1257 fmol。对作为[3H]前列环素结合抑制剂的选定前列腺素进行比较,揭示了配体占据高亲和力受体的一些结构要求。