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Proglumide hemicalcium

CAS No. : 85068-56-0

MCE 站：Proglumide hemicalcium

产品活性：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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Cholecystokinin Receptor

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.
The incubation of HT29 cells with Proglumide significantly reduces the [³H]-thymidine incorporation to HT29 cells in a dose-dependent manner, with an IC₅₀ of 6.5 mM. Proglumide reduces in a dose-dependent manner the percentage of necrosis with a parallel increase of apoptosis up to 70%.

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.

相关产品：Ceruletide  |  Gastrin I, human  |  Pentagastrin  |  Loxiglumide  |  Sograzepide  |  Lorglumide sodium salt  |  Devazepide  |  Nastorazepide  |  CCK-B Receptor Antagonist 2  |  Proglumide  |  SR 146131  |  CCK-B Receptor Antagonist 1  |  Dexloxiglumide  |  Lintitript  |  Mini Gastrin I, human TFA  |  Gastrin I, rat  |  Tarazepide  |  CCK-A receptor inhibitor 1  |  CHEMBL333994  |  Gastrin/CCK antagonist 1  |  GI 181771

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