Harvey C A, Owen D A
Br J Pharmacol. 1984 Oct;83(2):427-32. doi: 10.1111/j.1476-5381.1984.tb16503.x.
Cardiovascular studies have been made in anaesthetized cats with SK&F 93319, an antagonist of histamine at both H1- and H2-receptors. SK&F 93319, 8 X 10(-8) and 4 X 10(-7) mol kg-1 min-1 antagonized depressor responses to injections of histamine and the maximum displacement of histamine dose-response curves exceeded that which can be obtained with either an H1-receptor antagonist or an H2-receptor antagonist alone. SK&F 93319, 8 X 10(-8) and 4 X 10(-7) mol kg-1 min-1, also caused dose-dependent antagonism of histamine-induced falls in blood pressure and total peripheral resistance during intravenous infusions of histamine. SK&F 93319 inhibited depressor responses to intravenous injections of 2-(2-aminoethyl)pyridine, dimaprit and impromidine. The displacement of the 2-(2-aminoethyl)pyridine dose-response curve was similar to the displacement of histamine dose-response curves. SK&F 93319 caused greater displacement of dimaprit or impromidine dose-response curves than of histamine or 2-(2-aminoethyl)pyridine dose-response curves. SK&F 93319 was an effective antagonist of histamine, 2-(2-aminoethyl)pyridine or dimaprit-induced vasodilatation in femoral and gastric vasculature. SK&F 93319 has been shown to be an effective antagonist of vascular responses to histamine in anaesthetized cats. SK&F 93319 appeared to be more effective as an H2-receptor antagonist than as an H1-receptor antagonist in these vascular studies.
已使用SK&F 93319（一种H1和H2受体的组胺拮抗剂）对麻醉猫进行了心血管研究。SK&F 93319，8×10(-8)和4×10(-7)摩尔/千克·分钟-1拮抗了注射组胺后的降压反应，组胺剂量-反应曲线的最大位移超过了单独使用H1受体拮抗剂或H2受体拮抗剂所能获得的位移。SK&F 93319，8×10(-8)和4×10(-7)摩尔/千克·分钟-1，在静脉输注组胺期间也引起了组胺诱导的血压下降和总外周阻力下降的剂量依赖性拮抗作用。SK&F 93319抑制了对静脉注射2-(2-氨基乙基)吡啶、二甲双胍和英普咪定的降压反应。2-(2-氨基乙基)吡啶剂量-反应曲线的位移与组胺剂量-反应曲线的位移相似。SK&F 93319引起的二甲双胍或英普咪定剂量-反应曲线的位移大于组胺或2-(2-氨基乙基)吡啶剂量-反应曲线的位移。SK&F 93319是组胺、2-(2-氨基乙基)吡啶或二甲双胍诱导的股动脉和胃血管舒张的有效拮抗剂。已证明SK&F 93319是麻醉猫血管对组胺反应的有效拮抗剂。在这些血管研究中，SK&F 93319作为H2受体拮抗剂似乎比作为H1受体拮抗剂更有效。
