Horii D, Hara Y, Hanazuka M, Nishi H
Nihon Yakurigaku Zasshi. 1986 Apr;87(4):417-26. doi: 10.1254/fpj.87.417.
The effects of MY-5116, isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c]quinoline-2-carboxylate, an anti-allergic drug, and MY-1250, an active metabolite of MY-5116, on the cardiovascular system were studied in dogs, rats and guinea pigs. Orally administered MY-5116 (300 mg/kg) had no effect on the cardiovascular system in anesthetized dogs and conscious rats. In anesthetized dogs, MY-1250 and disodium cromoglycate (DSCG) caused hypotension, bradycardia and reduction of respiration rate from the doses of 3 and 10 micrograms/kg, i.v., respectively. Both drugs showed a tachyphylaxic phenomena which was crossed with each other. MY-1250-induced cardiovascular effects were abolished by bilateral vagotomy. MY-1250 (3-30 micrograms/kg, i.v.) caused a decrease of carotid blood flow, a transient decrease followed by a slight increase of renal blood flow, and a transient increase followed by a slight decrease of femoral blood flow in anesthetized dogs. MY-1250 had no effect on sympathetic ganglion, but increased the contractile force of isolated left atria from guinea pigs at 10(-5) g/ml and increased its rate at 10(-4) g/ml. These positive inotropic and chronotropic effects were not influenced by reserpinization. MY-1250 had no effect on the norepinephrine-induced dose-response curve in isolated rat aorta.
对一种抗过敏药物MY - 5116（5,6 - 二氢 - 7,8 - 二甲基 - 4,5 - 二氧代 - 4H - 吡喃并[3,2 - c]喹啉 - 2 - 羧酸异戊酯）及其活性代谢产物MY - 1250对犬、大鼠和豚鼠心血管系统的影响进行了研究。口服给予MY - 5116（300mg/kg）对麻醉犬和清醒大鼠的心血管系统无影响。在麻醉犬中，MY - 1250和色甘酸钠二钠（DSCG）分别静脉注射剂量为3和10μg/kg时会引起低血压、心动过缓和呼吸频率降低。两种药物均表现出快速耐受性现象，且相互交叉。双侧迷走神经切断可消除MY - 1250引起的心血管效应。在麻醉犬中，MY - 1250（静脉注射3 - 30μg/kg）会导致颈动脉血流量减少，肾血流量短暂减少后略有增加，股动脉血流量短暂增加后略有减少。MY - 1250对交感神经节无影响，但在10^(-5)g/ml时可增加豚鼠离体左心房的收缩力，在10^(-4)g/ml时可增加其心率。这些正性肌力和变时性作用不受利血平化的影响。MY - 1250对离体大鼠主动脉中去甲肾上腺素诱导的剂量 - 反应曲线无影响。
