Nakamura S, Yamamura H, Kohno S, Ohata K, Yoshimi A, Nishimura K, Kakeya N
Department of Pharmacology, Kyoto Pharmaceutical University.
Arerugi. 1990 Dec;39(12):1621-8.
The oral anti-allergic effect of 1,3-bis-(2- ethoxycarbonylchromon-5-yloxy)-2-((S)-lysyloxy)propane dihydrochloride (N-556, KY-556) was investigated. 1) N-556 (10-100 mg/kg, p.o.) inhibited dose-dependently the 48-hr homologous PCA in rats, and the duration of action was longer than that of intravenous DSCG. 2) N-556 (20 and 100 mg/kg once a day for 20 consecutive days, p.o.) tended to inhibit the histamine release from actively sensitized rat lung fragments. 3) N-556 (100 mg/kg, p.o.) showed the prolongation of survival time in the rat systemic anaphylaxis. 4) N-556 (100 mg/kg, p.o.) significantly inhibited the increased airway resistance in experimental asthma in rats. These results suggest that N-556 is a promising and orally-active pro-drug of disodium cromoglycate (DSCG) against allergic diseases.
研究了1,3-双-(2-乙氧羰基色酮-5-基氧基)-2-((S)-赖氨酰氧基)丙烷二盐酸盐(N-556,KY-556)的口服抗过敏作用。1)N-556(10 - 100毫克/千克,口服)剂量依赖性地抑制大鼠48小时同源被动皮肤过敏反应(PCA),且作用持续时间长于静脉注射色甘酸钠(DSCG)。2)N-556(20和100毫克/千克,每天一次,连续20天,口服)倾向于抑制主动致敏大鼠肺组织碎片中组胺的释放。3)N-556(100毫克/千克,口服)可延长大鼠全身性过敏反应的存活时间。4)N-556(100毫克/千克,口服)显著抑制大鼠实验性哮喘中气道阻力的增加。这些结果表明,N-556是一种有前景的、口服活性的色甘酸钠(DSCG)前药,可用于治疗过敏性疾病。