Proglumide hemicalcium

立即咨询

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

85068-56-0

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。

生物活性

Proglumide hemicalcium is a nonpeptide and orally activecholecystokinin (CCK)-A/B receptorsantagonist. Proglumide hemicalcium selective blocksCCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities^[1]^[2]^[3]^[4]^[5].

IC₅₀& Target

Cholecystokinin (CCK)-A/B receptors^[1]^[2]

体外研究
(In Vitro)

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^[2].
The incubation of HT29 cells with Proglumide significantly reduces the [³H]-thymidine incorporation to HT29 cells in a dose-dependent manner, with an IC₅₀of 6.5 mM. Proglumide reduces in a dose-dependent manner the percentage of necrosis with a parallel increase of apoptosis up to 70%^[3].

体内研究
(In Vivo)

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^[1].

Animal Model:	Adult male Sprague Dawley rats (200-250 g; 2 months old) are induced status epilepticus (SE)^[1]
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.

Clinical Trial

分子量

353.44

Formula

C₁₈H₂₆N₂O_4.1/2Ca

CAS 号

85068-56-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.