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 [1].
In Vivo, F3288-0031 (3-50 mg/kg, i.p., once) has an antidepressant-like activity without confounding locomotor effects in C57BL/6J mice[1].
References:
[1]. Tang M, er al. Reversing the Warburg effect: Discovery of potent pyruvate dehydrogenase kinase inhibitors for inhibiting tumor growth. Bioorg Chem. 2025 Dec;167:109224.
In Vivo, F3288-0031 (3-50 mg/kg, i.p., once) has an antidepressant-like activity without confounding locomotor effects in C57BL/6J mice[1].
References:
[1]. Tang M, er al. Reversing the Warburg effect: Discovery of potent pyruvate dehydrogenase kinase inhibitors for inhibiting tumor growth. Bioorg Chem. 2025 Dec;167:109224.