calcium (±)-bis[4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate]

中文名称calcium (±)-bis[4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate]
中文同义词
英文名称calcium (±)-bis[4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate]
英文同义词calcium (±)-bis[4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate];Calcium (1)-bis(4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate);Einecs 285-313-2;Proglumide hemicalcium
CAS号85068-56-0
分子式C36H50CaN4O8
分子量706.8822
EINECS号285-313-2
相关类别
Mol文件85068-56-0.mol
结构式calcium (±)-bis[4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate] 结构式

calcium (±)-bis[4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate] 性质

calcium (±)-bis[4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate] 用途与合成方法

Proglumide hemicalcium 是一种非肽和口服活性胆囊收缩素 (CCK)-A/B 受体拮抗剂。Proglumide hemicalcium 选择性阻断 CCK 在中枢神经系统中的作用。Proglumide hemicalcium 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。

Cholecystokinin (CCK)-A/B receptors

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%.

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.

安全信息

MSDS信息

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