DOV-102,677

DOV-102,677 is an oral small-molecule triple monoamine reuptake inhibitor that selectively blocks the dopamine transporter (DAT), norepinephrine transporter (NET), and serotonin transporter (SERT) with similar potency, thereby increasing extracellular dopamine, norepinephrine, and serotonin levels in brain regions such as the prefrontal cortex and nucleus accumbens.[4][3][10] Chemically, it is the (1S,5R) enantiomer of the azabicyclohexane DOV-216,303, and it also shows appreciable affinity at several monoaminergic receptors, including adrenergic, dopaminergic, histamine H1, muscarinic cholinergic, serotonin, and sigma sites at higher concentrations.[4][8] The compound was originally developed by DOV Pharmaceutical and later by Euthymics Bioscience, and entered phase 1 clinical development primarily for major depressive disorder and for alcohol abuse/dependence, where preclinical studies demonstrated robust antidepressant‑like effects and prolonged, selective reductions in alcohol-motivated behaviors in alcohol-preferring rats.[9][13][5]

Other names

(1S,5R)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane