Lumateperone tosylate 是5-HT 2A受体拮抗剂，Ki为 0.54 nM，突触前D2受体的部分激动剂和突触后D2受体的拮抗剂，Ki为 32 nM。

Lumateperone Tosylate 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).

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).

1187020-80-9

C31H36FN3O4S

565.7

Lumateperone甲苯磺酸盐;ITI-007

DMSO:245 mg/mL (433.09 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years