Lesogaberan napadisylate T40572

Product Introduction
Bioactivity


英文名: Lesogaberan napadisylate

描述: Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, as determined by its displacement of [3H]GABA binding in brain membranes. Notably, Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.

体外活性: Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro[2]. Cell Proliferation Assay[2]Cell Line: Human islet cells Concentration: 3, 10, and 30 nM Incubation Time: 4 days Result: Had a small but nonsignificant promitotic effect at 3?nM, while treatment at higher dosages (10 and 30?nM) led to a 2-3-fold increase in proliferation relative to that of islets cultured in medium alone.

体内活性: Lesogaberan (AZD3355) potently stimulates recombinant human GABA B receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1]. Oral Lesogaberan (0.08?mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice[2]. Lesogaberan (7 μmol/kg) shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1]. Animal Model: Diabetic NOD/scid mice were implanted with human islets[2]Dosage: 0.08?mg/mL Administration: Oral feeding; 48 hours Result: Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin + β-cells in human islet grafts. Animal Model: Female Sprague Dawley rats[1]Dosage: 7 μmol/kg (Pharmacokinetic Analysis) Administration: Oral Result: High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Lesogaberan napadisylate

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途