lesogaberan hydrochloride

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 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 .

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 (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC50 of 8.6 nM for human recombinant GABA B receptors. It has an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, determined by displacement of [3H]GABA binding in brain membranes. Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.