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Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma[1].

human Norepinephrine transporter: 8.0 (pIC₅₀); human Serotonin transporter: 8.6 (pIC₅₀); rat Norepinephrine transporter: 7.9 (pIC₅₀); rat Serotonin transporter: 8.9 (pIC₅₀)

[1] Smith JA, et al. Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor. Int J Neuropsychopharmacol. 2014 Dec 13;18(2):pyu027. DOI:10.1093/ijnp/pyu027