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Gepirone is an oral antidepressant of the azapirone class, approved for the treatment of major depressive disorder (MDD) in adults. It acts as a selective partial agonist at the serotonin 5-HT1A receptor, modulating serotonergic activity in the central nervous system. Gepirone and its active metabolite 3’-OH-gepirone bind to 5-HT1A receptors as agonists, while another metabolite (1-PP) acts as an antagonist at alpha2-adrenergic receptors. Unlike some other antidepressants, gepirone has minimal affinity for dopamine D2 receptors and is associated with a lower risk of sexual dysfunction. The drug was developed to address limitations of earlier antidepressants and is available in extended-release tablet form[2][4][5][7][8].
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