Driver A G, Mustafa S J
Department of Medicine, East Carolina University, School of Medicine, Greenville, NC 27858.
Eur J Pharmacol. 1987 Jul 23;139(3):287-95. doi: 10.1016/0014-2999(87)90586-3.
In order to validate the use of [3H]mepyramine as a radioligand to label airway histamine H1 receptors, the results of radioligand binding experiments using porcine tracheal tissue membranes were compared with the results of physiologic studies measuring histamine-induced trachealis muscle contraction. Close agreement was found between histamine-induced [3H]mepyramine binding inhibition and histamine concentration-contraction-response curves. Close agreement was also found between the KD of mepyramine-induced [3H]mepyramine binding inhibition and the K beta of mepyramine antagonism of muscle contractions stimulated by 10(-4) M histamine. [3H]Mepyramine binding was found to be rapid, reversible, saturable and stereospecific. Only H1 agonists and antagonists displayed potent [3H]mepyramine binding inhibition in competition binding studies. The results fulfill criteria for histamine H1 receptor identification by radioligand binding with [3H]mepyramine.
为了验证[3H]美吡拉敏作为放射性配体标记气道组胺H1受体的用途，将使用猪气管组织膜进行的放射性配体结合实验结果与测量组胺诱导的气管平滑肌收缩的生理学研究结果进行了比较。在组胺诱导的[3H]美吡拉敏结合抑制与组胺浓度-收缩反应曲线之间发现了密切的一致性。在美吡拉敏诱导的[3H]美吡拉敏结合抑制的KD与美吡拉敏对10(-4)M组胺刺激的肌肉收缩的拮抗作用的Kβ之间也发现了密切的一致性。发现[3H]美吡拉敏结合是快速、可逆、可饱和和立体特异性的。在竞争结合研究中，只有H1激动剂和拮抗剂表现出有效的[3H]美吡拉敏结合抑制。这些结果符合通过[3H]美吡拉敏放射性配体结合鉴定组胺H1受体的标准。
