Lesogaberan

Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan 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 inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action[1].

Product Specifications

CAS Number

[344413-67-8]

Product Name Alternative

AZD-3355

UNSPSC

12352211

Hazard Statement

H302-H412

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.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C3H9FNO2P

Molecular Weight

141.08

Precautions

P264-P270-P273-P330-P501

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.