Ishibe T, Kuno T, Tanaka C
Eur J Pharmacol. 1984 Oct 30;106(1):107-12. doi: 10.1016/0014-2999(84)90683-6.
The alpha 1- and beta-adrenergic and muscarinic cholinergic receptors in guinea-pig nasal mucosa were measured for the first time by direct binding techniques using [3H]prazosin, [3H]dihydroalprenolol ([3H]DHA) and [3H]quinuclidinyl benzilate ([3H]QNB). The maximum binding capacities of [3H]prazosin, [3H]DHA and [3H]QNB in guinea-pig nasal mucosa were 20.1, 42.3, 159 fmol/mg protein, respectively. The dissociation constants of [3H]prazosin, [3H]DHA and [3H]QNB in guinea-pig nasal mucosa were 0.37, 0.77 and 1.5 nM, respectively. After the removal of the superior cervical ganglion in the guinea-pig, the number of alpha 1-adrenergic receptors was increased in the nasal mucosa while the number of beta-adrenergic and muscarinic receptors remained unchanged. Thus, alpha 1-adrenergic receptors are probably postsynaptic receptors in the target cells of sympathetic nerves, while beta receptors relate to the circulating catecholamines.
首次采用直接结合技术,使用[3H]哌唑嗪、[3H]二氢阿普洛尔([3H]DHA)和[3H]喹核醇基苯甲酸酯([3H]QNB)测定了豚鼠鼻黏膜中的α1-、β-肾上腺素能和毒蕈碱胆碱能受体。[3H]哌唑嗪、[3H]DHA和[3H]QNB在豚鼠鼻黏膜中的最大结合容量分别为20.1、42.3、159 fmol/mg蛋白质。[3H]哌唑嗪、[3H]DHA和[3H]QNB在豚鼠鼻黏膜中的解离常数分别为0.37、0.77和1.5 nM。切除豚鼠颈上神经节后,鼻黏膜中α1-肾上腺素能受体数量增加,而β-肾上腺素能和毒蕈碱受体数量保持不变。因此,α1-肾上腺素能受体可能是交感神经靶细胞中的突触后受体,而β受体与循环中的儿茶酚胺有关。