129200-10-8
129200-10-8 结构式
常见问题列表
生物活性
KB-5492 anhydrous 是一种有效的和选择性的 sigma 受体抑制剂，抑制 [3H]1,3-di(2-tolyl)guanidine (DTG) 与 sigma 受体结合，IC50 值为 3.15 μM。KB-5492 anhydrous 是一种抗溃疡药。靶点
IC50: 3.15 μM (sigma receptor)
体外研究
KB-5492 (0.001-100 μM) inhibits specific [
3
H]DTG binding in a concentration-dependent manner.
KB-5492 (0.1-1 mM) significantly and concentration-dependently prevents the ethanol- and acidified aspirin-induced increases in
51
Cr release from gastric epithelial cells.
体内研究
KB-5492 (200 mg/kg; p.o.) prevents macroscopic lesions in the gastric mucosa.
| Animal Model: | Male Sprague-Dawley rats weighing 210-240 g are induced gastric mucosal damage |
| Dosage: | 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. |