产品
编 号:F545472
分子式:C18H25N2NaO4
分子量:356.39
产品类型
结构图
CAS No: 99247-33-3
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产品详情
生物活性:
Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.
体内研究:
Proglumide (250-750 mg/kg;腹腔注射;成年雄性 Sprague Dawley 大鼠) 处理可显著改善癫痫发作活动、认知功能障碍和脑氧化应激。Animal Model:Adult male Sprague Dawley rats (200-250?g; 2 months old) are induced status epilepticus (SE)
Dosage:250 mg/kg, 500 mg/kg, and 750?mg/kg
Administration:Intraperitoneal injection
Result:Dose-dependently and significantly increased the latencies to seizure and SE. Significantly and dose-dependently attenuated Li-PC (SE) induced increase in thiobarbituric acid (TBARS) and catalase (CAT), attenuated Li-Pc induced decrease in SOD, and attenuated depletion of GSH and glutathione-S transferase (GST) in the hippocampus and striatum.
体外研究:
在一项体外研究中,浓度在 0.3-10 mM 之间的 Proglumide 会剂量依赖性地抑制 CCK 刺激的淀粉酶释放,而浓度在 0-3 mM 之间的 Proglumide 不会影响基础淀粉酶的释放。随着丙谷胺浓度的增加,淀粉酶释放对 CCK 的剂量反应曲线向右移动。Proglumide 的这种抑制作用是可逆的。此外,Proglumide 对 CCK 及其相关肽具有选择性。HT29 细胞与 Proglumide 一起孵育可显著降低 [3H]-胸苷以剂量依赖性方式掺入 HT29 细胞,IC50 为 6.5 mM。Proglumide 以剂量依赖性方式降低坏死百分比,同时细胞凋亡增加高达 70%。