Pointon S E, Banerjee S P
Biochim Biophys Acta. 1979 May 1;584(2):231-41. doi: 10.1016/0304-4165(79)90267-8.
Binding of [3H]dihydroergokryptine and [3H]dihydroalprenolol to membrane preparations from rat submaxillary gland was measured to characterize the alpha- and beta-adrenergic receptors, respectively. Kinetic analysis of the data revealed a high affinity binding site for each radioligand. Inhibition of binding at each site was stereospecific for the active isomer of the catecholamine used. The greater ability of a beta1 than beta2 specific beta-adrenergic antagonist to displace [3H]dihydroalprenolol binding indicated that this binding site was of the beta1 type. Chemical sympathectomy with reserpine or 6-hydroxydopamine resulted in a significant increase in both [3H]dihydroalprenolol and [3H]dihydroergokryptine binding in the rat submaxillary gland. 3scatchard analysis of the data indicated that these increases in binding were due to a change in total number of binding sites for [3H]dihydroergokryptine and [3H]dihydroalprenolol with little change in apparent affinities. This suggests that changes in alpha- and beta-adrenergic receptor density may be important in the development of supersensitivity in salivary glands after reserpine and 6-hydroxydopamine treatment.
分别测定了[3H]二氢麦角隐亭和[3H]二氢阿普洛尔与大鼠颌下腺膜制剂的结合,以分别表征α-和β-肾上腺素能受体。对数据的动力学分析显示,每种放射性配体都有一个高亲和力结合位点。每个位点的结合抑制对所用儿茶酚胺的活性异构体具有立体特异性。β1特异性β-肾上腺素能拮抗剂比β2特异性β-肾上腺素能拮抗剂更能置换[3H]二氢阿普洛尔的结合,这表明该结合位点是β1型的。用利血平或6-羟基多巴胺进行化学交感神经切除术导致大鼠颌下腺中[3H]二氢阿普洛尔和[3H]二氢麦角隐亭的结合均显著增加。对数据的Scatchard分析表明,这些结合的增加是由于[3H]二氢麦角隐亭和[3H]二氢阿普洛尔结合位点总数的变化,而表观亲和力变化很小。这表明,α-和β-肾上腺素能受体密度的变化可能在利血平和6-羟基多巴胺治疗后唾液腺超敏反应的发展中起重要作用。