Rinner I, Porta S, Schauenstein K
Institute of Functional Pathology, University of Graz, Austria.
Endocrinol Exp. 1990 Mar;24(1-2):125-32.
The binding parameters of muscarinic antagonists in intact rat thymocytes were determined from competitive binding experiments with 3H-N-methylscopolamine (3H-NMS). The muscarinic antagonists inhibited binding of 3H-NMS in a dose-dependent manner. Non-linear regression analysis of the displacement curves indicated the presence of two affinity states for the muscarinic compounds. The beta-blocking agents R-propranolol, S-propranolol and alprenolol inhibited the binding of 3H-NMS to one, low affinity binding site on rat thymic lymphocytes. The ganglionic blocking substance hexamethonium did not affect the binding of 3H-NMS. The results indicate the presence of two binding sites for the radioligand on rat thymocytes, of which only one is specific for muscarinic receptor antagonists.
通过与3H-N-甲基东莨菪碱(3H-NMS)进行竞争性结合实验,测定了毒蕈碱拮抗剂在完整大鼠胸腺细胞中的结合参数。毒蕈碱拮抗剂以剂量依赖的方式抑制3H-NMS的结合。对位移曲线进行非线性回归分析表明,毒蕈碱化合物存在两种亲和力状态。β-阻滞剂R-普萘洛尔、S-普萘洛尔和阿普洛尔抑制3H-NMS与大鼠胸腺淋巴细胞上一个低亲和力结合位点的结合。神经节阻断物质六甲铵不影响3H-NMS的结合。结果表明,放射性配体在大鼠胸腺细胞上存在两个结合位点,其中只有一个对毒蕈碱受体拮抗剂具有特异性。