Esreboxetine (succinate)

Esreboxetine succinate is a selective norepinephrine transporter (NET) inhibitor, with a pIC₅₀ of 9.6 and a pK_i of 9.2 in rats, and it can cross the blood-brain barrier. Esreboxetine succinate increases urethral closure pressure and urethral resistance in rats. Esreboxetine succinate is applicable to research related to inflammatory pain and stress urinary incontinence^[1][2]. In Vitro:Esreboxetine (10 pM-100 μM; 6 h) succinate exhibits 20,000-fold higher selectivity for the rat norepinephrine transporter over the serotonin transporter in in vitro radioligand binding assays, with a pK_i of 9.2 for rat NET and 5.6 for rat SERT^[1].
Esreboxetine (10 pM-100 μM; 30 min pre-incubation, 6 min incubation) succinate potently and selectively inhibits norepinephrine uptake in rat cortical synaptosomes, with a pIC₅₀ of 9.6 for rat NET and a pIC₅₀ of 5.3 for rat SERT, representing a 20,000-fold selectivity for NET over SERT^[1]. In Vivo:A fixed-dose combination of esreboxetine succinate (10 mg/kg; i.p.; single administration) and Fluoxetine (HY-B0102) (1 mg/kg; i.p.; single administration) enhances the analgesic effect of morphine in the rat formalin model and achieves dual occupancy of NET and SERT^[1].