Lesogaberan (AZD-3355) hydrochloride 是一种有效的选择性 GABAB 受体激动剂，对人重组 GABAB 受体的 EC50 为 8.6 nM。通过脑膜中 [3H]GABA 结合位移测量，Lesogaberan hydrochloride 对大鼠 GABAB 和 GABAA 受体的亲和力 (Kis):分别为 5.1 nM 和 1.4 μM。Lesogaberan hydrochloride 通过外周作用模式抑制短暂的食管下括约肌松弛。
货号:ajcx34906
CAS:N/A
分子式:C3H10ClFNO2P
分子量：177.54
溶解度:DMSO : 240 mg/mL (1351.81 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action[1].

Lesogaberan hydrochloride (3-30 nM) enhances human islet cell proliferation in vitro[2].

Lesogaberan hydrochloride potently stimulates recombinant human GABAB 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) hydrochloride protects human islet β-cells from apoptosis in islet grafts in mice[2]. Lesogaberan (7 μmol/kg) hydrochloride shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1].

[1]. Lehmann A, et al. (R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABAB receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action. J Pharmacol Exp Ther. 2009 Nov;331(2):504-12.
[2]. Tian J, et al. Repurposing Lesogaberan to Promote Human Islet Cell Survival and β-Cell Replication. J Diabetes Res. 2017;2017:6403539.