Krell R D, Chakrin L W
Eur J Pharmacol. 1977 Jul 1;44(1):35-44. doi: 10.1016/0014-2999(77)90113-3.
The histamine H2-receptor antagonist metiamide was evaluated in in vitro and in vivo canine models of immediate-type hypersensitivity reactions. At concentrations of 2 and 4 X 10(-4) M, the antagonist significantly increased the amount of histamine present in the medium surrounding passively sensitized canine lung fragments which had been challenged with ascaris antigen. In contrast, the compound was without effect on the release of a slow reacting substance of anaphylaxis. On the basis of these observations metiamide was investigated in an in vivo canine model of allergic asthma. At doses of 10, 30 and 50 mu moles/kg, the antagonist did not enhance the ascaris antigen-induced pulmonary pathophysiology. Similarly, at 10 and 50 mu moles/kg metiamide did not alter histamine-induced increases in pulmonary resistance or decreases in dynamic lung compliance. Insofar as the canine model of allergic asthma may be predictive of the human disease, it could be anticipated that the use of histamine H2-receptor antagonists may not be deleterious to allergic asthmatics.
在速发型超敏反应的体外和体内犬类模型中对组胺H2受体拮抗剂甲硫米特进行了评估。在浓度为2×10⁻⁴M和4×10⁻⁴M时,该拮抗剂显著增加了用蛔虫抗原攻击的被动致敏犬肺组织碎片周围培养基中组胺的含量。相比之下,该化合物对过敏反应慢反应物质的释放没有影响。基于这些观察结果,在过敏性哮喘的体内犬类模型中对甲硫米特进行了研究。在剂量为10、30和50微摩尔/千克时,该拮抗剂并未增强蛔虫抗原诱导的肺部病理生理变化。同样,在10和50微摩尔/千克时,甲硫米特并未改变组胺诱导的肺阻力增加或动态肺顺应性降低。就过敏性哮喘的犬类模型可能预测人类疾病而言,可以预期组胺H2受体拮抗剂的使用可能对过敏性哮喘患者无害。