Saviprazole (HOE-731) is a H +,K + -ATPase inhibitor. Saviprazole inhibits gastric acid secretion. Saviprazole inhibits histamine- and dbcAMP-stimulated [ 14 C]aminopyrine uptake, dbcAMP-induced oxygen consumption. Saviprazole can be used in research related to gastrointestinal diseases, such as gastric ulcers and acid reflux [1] [2].
In Vivo, Saviprazole (0.03-1 mg/kg; i.v., i.d.; single dose) causes dose-dependent, state-of-stimulation-dependent inhibition of histamine-stimulated gastric acid secretion in Heidenhain pouch dogs, with an ID50 of 0.16 mg/kg i.v. and 0.31 mg/kg i.d.[2]. Saviprazole (0.1-30 mg/kg; i.d.; single dose) causes dose-dependent inhibition of basal and secretagogue-stimulated gastric acid secretion in pylorus-ligated rats, with ID50 values ranging from 0.9 to 2.5 mg/kg[2]. Saviprazole (0.1-1 mg/kg; i.v.; single dose) causes dose-dependent inhibition of receptor- and postreceptor-stimulated gastric acid secretion in anesthetized stomach-lumen-perfused rats, with 0.5 mg/kg reducing IBMX + Forskolin -stimulated secretion by ~70%[2].
In Vitro, Saviprazole (0.1-30 μM; 20 min pre-stimulation) non-competitively inhibits histamine- and dbcAMP-stimulated [14C] aminopyrine uptake in isolated rabbit gastric glands with IC50 values of 0.8 μM and 1.3 μM, respectively, and this inhibition is reversible with Dithioerythritol [1]. Saviprazole (100 μM; 45 min) inhibits dbcAMP-stimulated oxygen consumption in isolated rabbit gastric glands down to basal levels, and this effect is dependent on an acidic parietal cell compartment, as it is fully prevented by 10 mM Imidazole [1]. Saviprazole potently inhibits gastric H+,K+-ATPase and proton transport in gastric vesicles[2].
References:
[1]. Herling AW, et al. The inhibitory effect of HOE 731 in isolated rabbit gastric glands. Biochem Pharmacol. 1990;40(8):1809-1814.
[2]. Herling AW, et al. Gastric acid inhibitory profile of saviprazole (HOE 731) compared to omeprazole. Pharmacology. 1991;43(6):293-303.
In Vivo, Saviprazole (0.03-1 mg/kg; i.v., i.d.; single dose) causes dose-dependent, state-of-stimulation-dependent inhibition of histamine-stimulated gastric acid secretion in Heidenhain pouch dogs, with an ID50 of 0.16 mg/kg i.v. and 0.31 mg/kg i.d.[2]. Saviprazole (0.1-30 mg/kg; i.d.; single dose) causes dose-dependent inhibition of basal and secretagogue-stimulated gastric acid secretion in pylorus-ligated rats, with ID50 values ranging from 0.9 to 2.5 mg/kg[2]. Saviprazole (0.1-1 mg/kg; i.v.; single dose) causes dose-dependent inhibition of receptor- and postreceptor-stimulated gastric acid secretion in anesthetized stomach-lumen-perfused rats, with 0.5 mg/kg reducing IBMX + Forskolin -stimulated secretion by ~70%[2].
In Vitro, Saviprazole (0.1-30 μM; 20 min pre-stimulation) non-competitively inhibits histamine- and dbcAMP-stimulated [14C] aminopyrine uptake in isolated rabbit gastric glands with IC50 values of 0.8 μM and 1.3 μM, respectively, and this inhibition is reversible with Dithioerythritol [1]. Saviprazole (100 μM; 45 min) inhibits dbcAMP-stimulated oxygen consumption in isolated rabbit gastric glands down to basal levels, and this effect is dependent on an acidic parietal cell compartment, as it is fully prevented by 10 mM Imidazole [1]. Saviprazole potently inhibits gastric H+,K+-ATPase and proton transport in gastric vesicles[2].
References:
[1]. Herling AW, et al. The inhibitory effect of HOE 731 in isolated rabbit gastric glands. Biochem Pharmacol. 1990;40(8):1809-1814.
[2]. Herling AW, et al. Gastric acid inhibitory profile of saviprazole (HOE 731) compared to omeprazole. Pharmacology. 1991;43(6):293-303.