Shah P M, Boulos P B, Springall R, Vashisht R, Pearce F L
Department of Chemistry, University College London, UK.
Agents Actions. 1994 Jun;41 Spec No:C51-2. doi: 10.1007/BF02007763.
The H2-antagonists famotidine and nizatidine produced a dose-dependent inhibition of histamine release from human colonic mucosal and muscle mast cells stimulated with anti-IgE. The IC30 values were in the range 0.5-10 microM and the maximum inhibition approached 50%. The compounds showed similar efficacy against rat peritoneal mast cells but were more potent. The cytoprotectant misoprostol had a striking effect on the human colonic mast cells, producing more than 50% inhibition at concentrations of 0.1-1 nM, but was much less active against the rat cells.
H2拮抗剂法莫替丁和尼扎替丁对用抗IgE刺激的人结肠黏膜和肌肉肥大细胞释放组胺产生剂量依赖性抑制作用。IC30值在0.5 - 10微摩尔范围内,最大抑制率接近50%。这些化合物对大鼠腹膜肥大细胞显示出相似的效力,但效力更强。细胞保护剂米索前列醇对人结肠肥大细胞有显著作用,在0.1 - 1纳摩尔浓度下产生超过50%的抑制作用,但对大鼠细胞的活性则低得多。