Ampreloxetine (TD-9855) is a potent and orally active norepinephrine (NE) and serotonin 5-HT inhibitor. Ampreloxetine has the potential for the research of neurogenic orthostatic hypotension.
Ampreloxetine (0.3, 1, 5, 10, 30, 60 mg/kg; p.o.; single dose) shows a plasma EC50s of 11.7ng/mL and 50.8ng/mL in rat, respectively[1].
References:
[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.
[2]. Kaufmann H, et al. Safety and efficacy of ampreloxetine in symptomatic neurogenic orthostatic hypotension: a phase 2 trial. Clin Auton Res. 2021 Dec;31(6):699-711.