Alvarez F J, Galindo A, Velasco A
Department of Pharmacology and Therapeutics, Faculty of Medicine, University of Valladolid, Spain.
Methods Find Exp Clin Pharmacol. 1992 Jul-Aug;14(6):431-5.
The effects of the monoamine oxidase inhibitors iproniazid, nialamide and phenelzine, the neuroleptics haloperidol and thioridazine, and the benzodiazepines diazepam and clonazepam on histamine H2-receptors were assessed on rat isolated uterus. The monoamine oxidase inhibitors showed a slight non-competitive antihistamine H2 activity, while diazepam and clonazepam were devoid of any action. Haloperidol and thioridazine inhibited in a dose-dependent manner the tonic component of KCl induced contraction, while thioridazine under the same conditions exhibited a slight antihistamine H2 activity. These data show that the drugs tested are devoid of or elicited only a slight antihistamine H2 activity at high non-therapeutic concentrations.
在大鼠离体子宫上评估了单胺氧化酶抑制剂异烟肼、尼亚酰胺和苯乙肼、抗精神病药物氟哌啶醇和硫利达嗪以及苯二氮䓬类药物地西泮和氯硝西泮对组胺H2受体的作用。单胺氧化酶抑制剂表现出轻微的非竞争性抗组胺H2活性,而地西泮和氯硝西泮则无任何作用。氟哌啶醇和硫利达嗪以剂量依赖性方式抑制氯化钾诱导收缩的张力成分,而硫利达嗪在相同条件下表现出轻微的抗组胺H2活性。这些数据表明,所测试的药物在高非治疗浓度下没有或仅引起轻微的抗组胺H2活性。