SERT-IN-2 is a potent SERT inhibitor ( IC 50 =0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier In Vivo SERT-IN-2 (DH4) (2.5 mg/kg, 5 mg/kg; p.o.; single dose) shows high plasma exposure and oral bioavailability in dogs and rats . SERT-IN-2 (10 mg/kg; i.p.; single dose) can cross the blood brain barrier in SD rats . SERT-IN-2 (1-10 mg/kg; i.p.; single dose) inhibited serotonin uptake and potently antagonizes the p-chloroamphetamine (PCA)-induced depletion of 5-HT in the rat hypothalamus . SERT-IN-2 (1-10 mg/kg; i.v.; 3 times before the test) exerts antidepressant effect in rat, reduces the immobility times in the forced swimming test (FST) in a dose-dependent manner . Pharmacokinetic Analysis Route Dose (mg/kg) C max (ng/mL) AUC (0-t) (ng·h/mL) T 1/2 (h) V ss (L/kg) Cl (L/h/kg) F (%) Rat IV 1 193 1340 7.53 6.41 11.6 / PO 2.5 180 2790 7.28 / / 83.28 Dog IV 1 520 2820 4.39 3.4 5.14 / PO 5 794 7540 16.4 / / 53.5 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 0.58 nM (SERT)