Fromson J M, Illing H P, Ings R M, Johnson K I, Johnson P, Ostrowski J, Schraven E, Steward A
Arzneimittelforschung. 1981;31(2):337-45.
14C-Labelled N-ethoxycarbonyl-3-morpholinosyndnonomine(14C-molsidomine, Corvaton) was administered orally to mouse, rat, rabbit, dog and rhesus monkey, and i.v. to rat and dog, at a dose level of 6 mg/kg-1. The rates and routes of excretion of radioactivity were determined. The oral dose was well-absorbed in all species and most (greater than 75%) of the radioactive dose was excreted in urine. In rat and dog less than 1% of the dose was present as expired 14CO2. In dog and rhesus monkey, small amounts of radioactivity were eliminated relatively slowly. In rat, dog and rhesus monkey, the three species examined in detail, radioactivity was generally distributed throughout the body 4-10 days after dosing. Levels were highest in liver, pelt, blood and the gastrointestinal tract. Whole-body autoradiographic studies in rat and rhesus monkey showed that at 4 days post-dose, radioactivity was highest in stomach wall and was distributed into other tissues in lesser amounts. In view of its mode of action, it was interesting that radioactivity was also associated with the heart muscle and aorta walls.
给小鼠、大鼠、兔子、狗和恒河猴口服14C标记的N - 乙氧羰基 - 3 - 吗啉代辛二胺(14C - 吗多明,可洛巴通),给大鼠和狗静脉注射,剂量为6mg/kg-1。测定放射性的排泄速率和途径。口服剂量在所有物种中吸收良好,大部分(超过75%)放射性剂量经尿液排泄。在大鼠和狗中,不到1%的剂量以呼出的14CO2形式存在。在狗和恒河猴中,少量放射性物质排泄相对缓慢。在大鼠、狗和恒河猴这三种详细研究的物种中,给药后4 - 10天放射性物质通常分布于全身。肝脏、皮毛、血液和胃肠道中的含量最高。对大鼠和恒河猴进行的全身放射自显影研究表明,给药后4天,胃壁中的放射性最高,且以较少的量分布于其他组织。鉴于其作用方式,放射性物质也与心肌和主动脉壁有关这一点很有意思。