Lesogaberan (AZD-3355) hydrochloride 是一种有效的选择性 GABA_B 受体激动剂，对人重组 GABA_B 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 GABA_B 和 GABA_A 受体的亲和力 (K_is)：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。

Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABA B receptor agonist with an EC 50 of 8.6 nM for human recombinant GABA B receptor. The affinity (K i s) of Lesogaberan hydrochloride for rat GABA B and GABA A receptors, as measured by displacement of [H]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.

Viscous liquid

Ki: 5.1±1.2 nM (rat GABAB), 1.4±0.3 μM (rat GABAA)
EC50: 8.6±0.77 nM (human GABAB receptor)

Lesogaberan hydrochloride (3-30 nM) enhances human islet cell proliferation in vitro. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation AssayCell Line:

Lesogaberan hydrochloride potently stimulates recombinant human GABA B receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve.
Oral Lesogaberan (0.08?mg/mL; 48 hours) hydrochloride protects human islet β-cells from apoptosis in islet grafts in mice.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[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.

In Vitro: DMSO : 240 mg/mL (1351.81 mM; Need ultrasonic)H₂O : 100 mg/mL (563.25 mM; Need ultrasonic)配制储备液