Giachetti A, Pagani F, Micheletti R, Brambilla A, Cereda E, Donetti A
Agents Actions. 1985 Apr;16(3-4):173-5. doi: 10.1007/BF01983131.
Mifentidine, a representative compound of a novel class of H2-antagonists, has been investigated for its ability to interact with H2-receptors and to inhibit gastric acid secretion. Affinity estimates (KB) of mifentidine obtained from in vitro studies on cardiac and gastric mucosal histamine (H2) receptors were in the 20-50 nM range. Mifentidine appeared to be endowed with strong anti-secretory properties against histamine-stimulated secretion in the anaesthetized rat and in the conscious dog. Distinct features of mifentidine were considerable bioavailability and duration of anti-secretory effect.
米芬替丁是新型H2拮抗剂类的代表性化合物，已对其与H2受体相互作用及抑制胃酸分泌的能力进行了研究。通过对心脏和胃黏膜组胺（H2）受体的体外研究获得的米芬替丁亲和力估计值（KB）在20 - 50 nM范围内。米芬替丁对麻醉大鼠和清醒犬组胺刺激的分泌似乎具有很强的抗分泌特性。米芬替丁的显著特点是生物利用度高和抗分泌作用持续时间长。
