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S44819 is a potent and selective small molecule antagonist of the GABA-A α5 receptor, developed to enhance functional recovery after acute ischemic stroke. By competitively inhibiting the GABA-A α5 receptor, S44819 reduces excessive GABAergic inhibition in the peri-infarct cortex, thereby promoting neuroplasticity and improving motor and cognitive outcomes post-stroke. The drug has been evaluated in phase II clinical trials (RESTORE BRAIN study) for its efficacy and safety in patients recovering from recent ischemic cerebral events[1][2][3][4]. Preclinical studies have shown that S44819 can increase cortico-spinal excitability by reducing GABA-A α5-mediated inhibition, supporting its mechanism of action as a neurorestorative agent[1][6].
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