4-苯酰胺-5-二丙氨基-5-氧戊酸钠盐

生物活性靶点体外研究体内研究 4-苯酰胺-5-二丙氨基-5-氧戊酸钠盐试剂级价格

CAS号:99247-33-3
英文名:PROGLUMIDE, SODIUM SALT
中文名:4-苯酰胺-5-二丙氨基-5-氧戊酸钠盐
CBNumber:CB3125814
分子式:C18H27N2NaO4
分子量:358.41
MOL File:99247-33-3.mol

4-苯酰胺-5-二丙氨基-5-氧戊酸钠盐化学性质

储存条件 :Desiccate at RT
溶解度 :H₂O: soluble
形态 :solid
颜色 :white
水溶解性 :Soluble to 100 mM in water

安全信息

WGK Germany :3

4-苯酰胺-5-二丙氨基-5-氧戊酸钠盐性质、用途与生产工艺

生物活性 Proglumide sodium 是一种非肽和口服活性胆囊收缩素 (CCK)-A/B 受体拮抗剂。Proglumide sodium 选择性阻断 CCK 在中枢神经系统中的作用。Proglumide sodium 具有抑制胃分泌和保护胃十二指肠粘膜的能力，还具有抗癫痫和抗氧化活性。
靶点

Cholecystokinin (CCK)-A/B receptors
体外研究

In an in vitro study, Proglumide at concentrations between 0.3-10 mM inhibits CCK-stimulated amylase release dose-dependently, while Proglumide does not influence the basal amylase release at concentrations between 0-3 mM. Dose-response curves to CCK for amylase release shifted to the right with increase in Proglumide concentration. This inhibition by Proglumide is reversible. In addition, the effect of Proglumide is selective for CCK and its related peptide.
The incubation of HT29 cells with Proglumide significantly reduces the [ ³ H]-thymidine incorporation to HT29 cells in a dose-dependent manner, with an IC ₅₀ of 6.5 mM. Proglumide reduces in a dose-dependent manner the percentage of necrosis with a parallel increase of apoptosis up to 70%.

体内研究

Proglumide (250-750 mg/kg; intraperitoneal injection; adult male Sprague Dawley rats) treatment is significantly effective in ameliorating the seizure activities, cognitive dysfunctions, and cerebral oxidative stress.

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.