Knoll J, Gyires K, Hermecz I
Department of Pharmacology, Semmelweis University of Medicine, Budapest, Hungary.
Drugs Exp Clin Res. 1987;13(5):253-8.
1,6-Dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrido 1,2-a pyrimidine-3-carboxamide (Ch-127) significantly inhibited the intestinal ulceration induced by a single dose of indomethacin (15 mg/kg p.o.). Moreover, indomethacin produced 75% lethality in the dose of 3.5 mg/kg p.o. administered daily for 2 weeks. The concurrent daily administration of Ch-127 (50 mg/kg p.o. +25 mg/kg s.c.) with indomethacin prevented the gastrointestinal mucosa from histologically detectable changes, and none of the animals died. The 80% lethality following the daily administration of naproxen (60 mg/kg p.o.) for two weeks was also significantly decreased by combining it with Ch-127 (50 mg/kg p.o.).
1,6 - 二甲基 - 4 - 氧代 - 1,6,7,8,9,9a - 六氢 - 4H - 吡啶并[1,2 - a]嘧啶 - 3 - 甲酰胺（Ch - 127）显著抑制单次口服吲哚美辛（15毫克/千克）诱导的肠道溃疡。此外，每日口服3.5毫克/千克剂量的吲哚美辛，连续给药2周会导致75%的致死率。Ch - 127（口服50毫克/千克 + 皮下注射25毫克/千克）与吲哚美辛同时每日给药可防止胃肠道黏膜出现组织学可检测到的变化，且无动物死亡。每日口服萘普生（60毫克/千克），连续给药两周后80%的致死率，在与Ch - 127（口服50毫克/千克）联合使用时也显著降低。
