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85068-56-0

英文名稱(chēng) calcium (±)-bis[4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate]
CAS 85068-56-0
分子式 C36H50CaN4O8
分子量 706.882
MOL 文件 85068-56-0.mol
85068-56-0 結(jié)構(gòu)式 85068-56-0 結(jié)構(gòu)式

基本信息

英文別名
Einecs 285-313-2
Proglumide hemicalcium
Calcium (1)-bis(4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate)
calcium (±)-bis[4-(benzoylamino)-5-(dipropylamino)-5-oxovalerate]

常見(jiàn)問(wèn)題列表

生物活性
Proglumide hemicalcium 是一種非肽和口服活性膽囊收縮素 (CCK)-A/B 受體拮抗劑。Proglumide hemicalcium 選擇性阻斷 CCK 在中樞神經(jīng)系統(tǒng)中的作用。Proglumide hemicalcium 具有抑制胃分泌和保護(hù)胃十二指腸粘膜的能力,還具有抗癲癇和抗氧化活性。
靶點(diǎn)

Cholecystokinin (CCK)-A/B receptors

體外研究

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%.

體內(nèi)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.
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