Sakamoto H, Yokoyama N, Kohno S, Ohata K
Jpn J Pharmacol. 1984 Dec;36(4):455-60. doi: 10.1254/jjp.36.455.
The receptor binding profile, composed of the Ki-values measured in eight different receptor binding models using rat brain membranes, is reported for the new tricyclic antidepressant quinupramine, 10,11-dihydro-5-(3-quinuclidinyl)-5H-dibenz[b, f]azepine, and three reference compounds with a tertiaryamine side chain. Quinupramine was found to possess high affinity for muscarinic cholinergic and histamine H1 receptor binding sites in rat brain, whereas its affinity for imipramine binding sites was only one seventieth that of imipramine. Receptor binding profiles of the reference compounds were almost similar to that of quinupramine, except in the case of imipramine binding sites.
报道了新型三环抗抑郁药喹纽普明(10,11-二氢-5-(3-喹啉基)-5H-二苯并[b,f]氮杂䓬)以及三种带有叔胺侧链的参考化合物,在使用大鼠脑膜的八种不同受体结合模型中测得的Ki值所构成的受体结合谱。发现喹纽普明对大鼠脑中的毒蕈碱胆碱能和组胺H1受体结合位点具有高亲和力,而其对丙咪嗪结合位点的亲和力仅为丙咪嗪的七十分之一。除了丙咪嗪结合位点的情况外,参考化合物的受体结合谱与喹纽普明的几乎相似。