F3288-0031 is a brain-penetrant norepinephrine transporter ( NET ) allosteric inhibitor with inhibitory rates of 73.5% at 20 μM. F3288-0031 binds within the inner vestibule of NET , stabilizing the inward-open state and has a preferential NET / SERT inhibition with pIC 50 = 5.9. F3288-0031 shows no detectable off-target functional activity in vitro. F3288-0031 demonstrates robust antidepressant-like efficacy in vivo without confounding locomotor effects, F3288-0031 can be used for depressive disorder and related neuropsychiatric conditions.
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