Tesofensine

Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC₅₀=6.5 nM), norepinephrine (NE;IC₅₀=1.7 nM), and serotonin (5-HT;IC₅₀=11 nM), and with potentials as an anti-obesity agent^[1]. Tesofensine is a CNS acting anti-obesity agent^[2]. IC50 & Target: DA/NE/5-HT^[1] In Vivo: Tesofensine (a single dose of 0.1-3? mg/kg, s.c.) induces hypophagia in the DIO rat. A single dose of Tesofensine (0. 1-3?mg/kg, s.c.) robustly and dose dependently inhibits food intake in DIO rats over the 12?h nocturnal observation period. Daily administration of a moderate dose of Tesofensine (2.0?mg/kg, s.c.) over 16 days triggers a significant reduction in body weight after 4 days of administration relative to vehicle-treated controls^[3].