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 [ 3 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.
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