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GATE-102 is an orally bioavailable small molecule that acts as a positive allosteric modulator (PAM) of the N-methyl-D-aspartate (NMDA) receptor. Originally developed by Allergan (later AbbVie) as AGN-241751 and subsequently acquired by Gate Neurosciences, the compound is designed to enhance synaptic plasticity and restore dendritic spine density, which are often diminished in patients with neuropsychiatric conditions. Unlike NMDA antagonists such as ketamine, GATE-102's mechanism as a PAM aims to provide rapid and sustained antidepressant effects with an improved safety profile, specifically avoiding the dissociative and sedative side effects associated with receptor blockade. It is currently being developed for the treatment of major depressive disorder (MDD).
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