溶解性 | (25°C): Water 28.7 mg/mL |
存贮条件 | 储存温度-20°C |
生化机理 |
Description: IC50 Value: 0.92uM(Ki with glycolaldehyde as the varied substrate for E3) Metiamide is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate compound in the development of the successful anti-ulcer drug cimetidine. in vitro: Metiamide is a competitive with aldehyde substrates and noncompetitive with the Human E3 Aldehyde Dehydrogenase coenzyme, binding to both the free E3 isozyme and the enzyme·coenzyme binary complex withK i values of 0.92 μM glycolaldehyde as the varied substrate[1]. Data was got as percentage change in GTPase activity induced by metiamide compared with the GTPase activity stimulated by HA (100 μM)[2]. in vivo: Metiamide is a histamine H2-receptor antagonist. It reduces basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin. Metiamide inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Metiamide include an increase in gastric bacterial flora such as nitrate-reducing organisms. Clinical trail: |