DSP-6745 is a potent inhibitor of 5-HT transporter (human SERT, Ki=0.653 nM), and 5-HT2A, 5-HT2C, and 5-HT7 receptors with Ki of 0.331, 1.34, and 31.7 nM, respectively.
DSP-6745 shows potent binding affinity for human 5-HT2B receptor and moderate binding affinity for human adrenergic α1A, 5-HT6, and sigma-1 receptors, low affinity for human dopamine D2L, histamine H1, and muscarinic M1 receptors.
DSP-6745 inhibits the calcium response mediated by human 5-HT2A, 5-HT2C, and 5-HT7 receptors in CHO-K1 cells with Kb values of 0.566, 1.37, and 2.12  nM, respectively.
DSP-6745 inhibits [3H]5-HT uptake in CHO cells expressing human SERT with an IC50 value of 0.753 nM.
DSP-6745 (6.4 and 19.1 mg/kg, p.o.) shows rapid antidepressant-like efficacy in the rat forced swim test, even at 24 h post-dosing, and anxiolytic activity in the rat social interaction test.
DSP-6745 (12.7 mg/kg, p.o.) led to an improvement in the apomorphine-induced prepulse inhibition deficit in rats.