lumateperone Tosylate (ITI-007) is a 5-HT2A receptor antagonist (Ki: 0.54 nM), a SERT blocker (Ki: 61 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki: 32 nM).

SERT:61 nM (Ki), 5-HT2A receptor:0.54 nM (Ki)

Lumateperone also possesses an affinity for the D1 receptor (Ki: 52 nM) and weak affinity for the α1A- and α1B-adrenergic receptors (Ki: 173 nM at α1) and D4 receptor. Lumateperone does not significantly bind to the 5-HT2B, 5-HT2C, H1, or mACh receptors. Lumateperone shows a 60-fold difference in its affinities for the 5-HT2A and D2 receptors, which is far greater than that of most or all existing atypical antipsychotics, such as risperidone (12-fold), olanzapine (12.4-fold), and aripiprazole (0.18-fold).