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Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). IC50 value: 0.54 nM (Ki, for 5-HT2A receptor ) Target: 5-HT2A receptor Lumateperone also possesses 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).[1] in vivo: It is thought that this property may improve the effectiveness and reduce the side effect profile of Lumateperone relative to currently-available antipsychotics, a hypothesis which is supported by the observation of minimal catalepsy in mice treated with Lumateperone. |
