Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).IC50 & Target: Ki: 7.53 nM (5-HT2A), 8.19 nM (sigma-2)In Vitro: Roluperidone (CYR-101) also shows binding affinity for α1-adrenergic receptors but low or no affinity for muscarinic, cholinergic, and histaminergic receptors. Although Roluperidone (CYR-101) has no affinities for pre- or postsynaptic dopaminergic receptors, it is probable that sigma-2 receptors are implicated in the modulation of dopamine and glutamatergic pathways, as well as in calcium neuronal modulation.