Gushchin I S, Deriugin I L, Kaminka M E
Biull Eksp Biol Med. 1978 Mar;85(3):329-32.
Research Allergological Laboratory of the USSR Academy of Medical Sciences and Laboratory of Pharmacology, S. Ordzhonikidze Research Chemico-Pharmaceutical Institute, Moscow. Among the tested new antihistaminic drugs (quinuclidine derivatives) quinuclidyl-3-(O-tolyl) carbinol possessed histamine releasing action (HRA) on the isolated rat mast cells. In used concentrations (up to 0.4 mmol) all phenothiazines (promethazine, phenethazine, chlorpromazine, methylene blue) had HRA. There was no correlation between the HRA and the antihistaminic activity of the tested drugs. Histamine release induced by antihistaminic drugs and a steep dose-response curve, was produced at low temperature and was not inhibited under conditions of inhibition of energy-dependent stage of 48/80-induced histamine release. It was concluded that the tested antihistaminic drugs which had HRA were non-selective histamine releasers.
苏联医学科学院变态反应学研究实验室及药理学实验室,莫斯科S. 奥尔忠尼启则化学制药研究所。在所测试的新型抗组胺药物(奎宁环衍生物)中,奎宁环基-3-(邻甲苯基)甲醇对离体大鼠肥大细胞具有组胺释放作用(HRA)。在所使用的浓度(高达0.4 mmol)下,所有吩噻嗪类药物(异丙嗪、吩乙嗪、氯丙嗪、亚甲蓝)均具有组胺释放作用。所测试药物的组胺释放作用与抗组胺活性之间无相关性。抗组胺药物诱导的组胺释放以及陡峭的剂量反应曲线在低温下产生,并且在抑制48/80诱导的组胺释放的能量依赖阶段的条件下未被抑制。得出的结论是,具有组胺释放作用的所测试抗组胺药物是非选择性组胺释放剂。