Lesogaberan (hydrochloride)

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].

Product Specifications

CAS Number

[2925644-17-1]

Product Name Alternative

AZD-3355 (hydrochloride)

UNSPSC

12352211

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/lesogaberan-hydrochloride.html

Purity

98.0

Solubility

DMSO : 240 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

O=P(C[C@H](F)CN)O.[H]Cl

Molecular Formula

C3H10ClFNO2P

Molecular Weight

177.54

References & Citations

[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.