KB-5492 free base is a potent and selective inhibitor of sigma receptor , inhibits specific [ 3 H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC 50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent
In Vitro
KB-5492 (0.001-100 μM) free base inhibits specific [ 3 H]DTG binding in a concentration-dependent manner. KB-5492 (0.1-1 mM) free base significantly and concentration-dependently prevents the ethanol- and acidified aspirin-induced increases in 51 Cr release from gastric epithelial cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
KB-5492 (200 mg/kg; p.o.) free base prevents macroscopic lesions in the gastric mucosa. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats weighing 210-240 g are induced gastric mucosal damageDosage: 200 mg/kg Administration: Oral gavage Result: Reduced the lesion length as compared with the control. Prevented the deep mucosal lesions and exfoliation of surface epithelial cells.