Johnston B M, Owen D A
Eur J Pharmacol. 1977 Aug 15;44(4):355-63. doi: 10.1016/0014-2999(77)90310-7.
The effects of mepyramine, a selective histamine H1-receptor antagonist, and metiamide, a selective histamine H2-receptor antagonist, have been determined on the cardiovascular response to intravenous infusions of a large dose of histamine, 1 X 10(-7) mol/kg/min. Pretreatment with either mepyramine, 2.5 X 10(-6) mol/kg, or metiamide, 2 X 10(-6) mol/kg/min, had no significant effect on the fall in blood pressure or fall in total peripheral resistance during histamine infusion. Pretreatment with mepyramine, 2.5 X 10(-6) mol/kg, and metiamide, 2 X 10(-6) mol/kg/min, abolished the fall in blood pressure and total peripheral resistance during infusion of histamine. Histamine-induced vasodilatation in the stomach was unaltered by pretreatment with mepyramine but abolished by pretreatment with metiamide. Histamine-induced coronary vasodilation was reduced slightly by pretreatment with mepyramine and substantially by pretreatment with metiamide. Coronary vasodilatation was abolished by treatment with mepyramine and metiamide.
已确定选择性组胺H1受体拮抗剂美吡拉敏和选择性组胺H2受体拮抗剂甲硫米特对静脉输注大剂量组胺(1×10⁻⁷摩尔/千克/分钟)时心血管反应的影响。用2.5×10⁻⁶摩尔/千克的美吡拉敏或2×10⁻⁶摩尔/千克/分钟的甲硫米特预处理,对组胺输注期间的血压下降或总外周阻力下降均无显著影响。用2.5×10⁻⁶摩尔/千克的美吡拉敏和2×10⁻⁶摩尔/千克/分钟的甲硫米特预处理,可消除组胺输注期间的血压下降和总外周阻力下降。美吡拉敏预处理不改变组胺诱导的胃血管舒张,但甲硫米特预处理可消除该作用。美吡拉敏预处理使组胺诱导的冠状动脉血管舒张略有降低,而甲硫米特预处理则使其显著降低。美吡拉敏和甲硫米特联合处理可消除冠状动脉血管舒张。