Goto K, Osuga K, Haga K, Tsumagari T
Nihon Yakurigaku Zasshi. 1983 May;81(5):343-63.
Traxanox at the upper dose of 300 mg/kg, p.o., showed no effect on the somatic and autonomic nervous systems in the various tests. This agent caused some relaxation of the guinea pig tracheal strip in the resting tone at a concentration of 10(-6)M or more; however, its activity was less potent than that of isoproterenol and paraverine. Traxanox had no competitive antagonistic action against chemical mediators. Treatment of rats with this agent (3 mg/kg, i.v., or 10 mg/kg, s.c.) resulted in an inhibition of gastric (acid) secretion. Intravenous injections of traxanox (1-10 mg/kg) in dogs caused an immediate but transient inhibition of gastric and jejunal movement, and after a short time, slight potentiation of the latter; however, pretreatment with atropine prevented this latter potentiation. In the in vitro test, 10(-4)M traxanox caused contraction of the guinea pig ileum, a response which was inhibited by atropine. Traxanox (300 mg/kg, p.o.), however, did not show any effects on gastrointestinal propulsion in mice, nor did it have any effect on the gastrointestinal mucosa, gastric ulcers or bile secretion in rats. Traxanox (300 mg/kg, p.o.) showed a diuretic action in both normal and adrenoectomized rats. This action, however, was not observed in the rats treated with indomethacin (1 mg/kg, i.p.). This agent (10 mg/kg, i.v.) suppressed the spontaneous uterine contractions of pregnant rats in some cases. These findings suggest that traxanox at doses (1-5 mg/kg, p. o.) showing antiallergic activity has little effect on the central, somatic and autonomic nervous systems, digestive system, urinary organs and reproductive organs.
口服剂量为300mg/kg的曲克芦丁在各项试验中对躯体和自主神经系统均无影响。该药物在浓度为10(-6)M或更高时,可使豚鼠气管条在静息张力下有所松弛;然而,其活性比异丙肾上腺素和罂粟碱弱。曲克芦丁对化学介质无竞争性拮抗作用。用该药物(静脉注射3mg/kg或皮下注射10mg/kg)治疗大鼠可抑制胃(酸)分泌。给犬静脉注射曲克芦丁(1 - 10mg/kg)可立即但短暂地抑制胃和空肠运动,短时间后对空肠运动有轻微增强作用;然而,用阿托品预处理可防止这种后期的增强作用。在体外试验中,10(-4)M的曲克芦丁可引起豚鼠回肠收缩,这种反应可被阿托品抑制。然而,口服曲克芦丁(300mg/kg)对小鼠胃肠道推进无任何影响,对大鼠胃肠道黏膜、胃溃疡或胆汁分泌也无任何作用。口服曲克芦丁(300mg/kg)在正常大鼠和肾上腺切除大鼠中均显示出利尿作用。然而,在用吲哚美辛(腹腔注射1mg/kg)治疗的大鼠中未观察到这种作用。该药物(静脉注射10mg/kg)在某些情况下可抑制妊娠大鼠的子宫自发收缩。这些发现表明,显示抗过敏活性的剂量(口服1 - 5mg/kg)的曲克芦丁对中枢、躯体和自主神经系统、消化系统、泌尿器官和生殖器官几乎没有影响。