Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively.

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

Lesogaberan effectively stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1]. Lesogaberan (7 μmol/kg) displays high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1]. Lesogaberan (0.08?mg/mL; 48 hours; p.o.) treatment, protects human islet β-cells from apoptosis in islet grafts in mice[2].

344413-67-8

C3H9FNO2P

141.08

AZD-3355;Lesogaberan

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years