Drazen J M, Schneider M W, Venugopalan C S
Eur J Pharmacol. 1979 May 1;55(3):233-9. doi: 10.1016/0014-2999(79)90189-4.
The bronchodilator activity of the H2-recptor agonist, dimaprit, was assessed in vitro and in vivo. In vitro dimaprit relaxed guinea pig tracheal spirals and parenchymal strips that were constricted by the H1 receptor agonist, 2-PEA, or by carbachol. The H2-receptor antagonist, metiamide, inhibited this effect of dimaprit in vitro on both tissues constricted by 2-PEA but not on the carbachol constricted tracheal spiral. Intravenous infusion of dimaprit in the intact guinea pig resulted in reversal of bronchoconstriction induced by subcutaneous injection of 2-PEA. In vivo pretreatment with the H2-recptor antagonist, metiamide, resulted in a diminished sensitivity to the bronchodilating effects of intravenous dimaprit.
对H2受体激动剂二甲双胍的支气管扩张活性进行了体外和体内评估。在体外,二甲双胍可使由H1受体激动剂2-苯乙胺或卡巴胆碱引起收缩的豚鼠气管螺旋条和实质条舒张。H2受体拮抗剂甲硫米特可在体外抑制二甲双胍对由2-苯乙胺引起收缩的两种组织的作用,但对由卡巴胆碱引起收缩的气管螺旋条无此作用。在完整豚鼠中静脉输注二甲双胍可逆转皮下注射2-苯乙胺所致的支气管收缩。在体内,用H2受体拮抗剂甲硫米特预处理会导致对静脉注射二甲双胍的支气管扩张作用的敏感性降低。