Bemesetron

Bemesetron is a selective antagonist of 5-HT3 (IC50 = 0.33 nM) with neuroprotective effects. (In Vitro) :In primary cortical neuronal cells, Bemesetron (1 μM) significantly blocks the H2O2-induced increase of caspase-3 immunoreactivity. Bemesetron (0.01, 0.1 and 1 μM) and Y25130 (0.05, 0.5 and 5 μM) concentration-dependently reduce the H2O2-induced decrease showing inhibition of 74.9 and 79.0% with 1 μM and 5 μM, respectively. (In Vivo) :In male adult albino mice, Bemesetron (1 mg/kg; i.p.) causes a significant reduction of catalepsy, while Bemesetron (10 mg/kg; i.p.) significantly potentiates the phenomenon. The maximum inhibition of catalepsy (about 75%) occurs at 120 min, and the maximum potentiation (about 4.5-times the control value) occurs at 60 min after Haloperidol.