Fernández A G, Massingham R, Roberts D J
Department of Pharmacology, Research Institute, Laboratorios Almirall, Barcelona, Spain.
Methods Find Exp Clin Pharmacol. 1988 May;10(5):285-93.
The substituted benzamide, clebopride, at doses (0.03-3 mg kg-1 i.p.) that were without effect per se on the secretion of gastric acid in pylorus ligated (Shay) rats, potentiated the antisecretory effects of the histamine H2 receptor antagonists cimetidine and ranitidine in this model but not those of the muscarine receptor antagonist pirenzepine nor those of the proton pump inhibitor omeprazole. By contrast, clebopride was without influence on the inhibitory effects of cimetidine on pentagastrin-induced secretion in perfused stomach (Ghosh and Schild) preparations in anaesthetized rats. The significance of these findings is discussed in relation to the previously described potentiating effects of clebopride on the anti-ulcer activity of cimetidine in various experimental models, and the potential beneficial effects of such combined therapy in the clinic.
取代苯甲酰胺类药物氯波必利,在剂量为0.03 - 3毫克/千克腹腔注射时,本身对幽门结扎( Shay )大鼠的胃酸分泌无影响,但在该模型中可增强组胺H2受体拮抗剂西咪替丁和雷尼替丁的抗分泌作用,而对毒蕈碱受体拮抗剂哌仑西平及质子泵抑制剂奥美拉唑的抗分泌作用则无增强作用。相比之下,氯波必利对西咪替丁在麻醉大鼠灌流胃( Ghosh和Schild )制备物中抑制五肽胃泌素诱导的分泌的作用没有影响。结合先前描述的氯波必利在各种实验模型中对西咪替丁抗溃疡活性的增强作用以及这种联合疗法在临床上的潜在有益作用,对这些发现的意义进行了讨论。