lumateperone (Tosylate) Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF: 25 mg/ml; DMF:PBS (pH 7.2) (1:7): 0.12 mg/ml; DMSO: 10 mg/ml; Ethanol: 1 mg/ml

form 

A solid

color 

White to gray

InChIKey

LHAPOGAFBLSJJQ-HXLBOWIHNA-N

SMILES

S(C1C=CC(C)=CC=1)(O)(=O)=O.CN1CCN2[C@@]3([H])CCN(CCCC(C4C=CC(F)=CC=4)=O)C[C@@]3([H])C3=CC=CC1=C32 |&1:16,34,r|

lumateperone (Tosylate) Usage And Synthesis

Uses

lumateperone (Tosylate) is a new second-generation antipsychotic indicated for treating schizophrenia that can potentially alleviate positive and negative symptoms. This drug interacts with dopamine, serotonin, and glutamate, making it unique compared to other antipsychotics. Its highly selective nature for D2R receptors in specific brain regions decreases unfavorable adverse effects and makes it a safer drug[1].

Biochem/physiol Actions

Lumateperone tosylate (ITI-007) is an orally active, potent 5-HT2A antagonist, postsynaptic D2 antagonist, and serotonin transporter SERT inhibitor (Ki = 0.5, 32, 62 nM, respectively) with in vivo antipsychotic efficacy and no effect toward receptors associated with cognitive and metabolic side effects of antipsychotic drugs (e.g., H1, 5-HT2C, muscarinic). ITI-007 blocks DOI-induced headtwitch (ID50 = 0.09 mg/kg, po.) and D-AMPH-induced hyperlocomotion in mice (ID50 = 0.95 mg/kg, po.), while also acting as a partial agonist at presynaptic striatal D2 receptors.

References

[1] Kunal Maini. “Lumateperone tosylate, A Selective and Concurrent Modulator of Serotonin, Dopamine, and Glutamate, in the Treatment of Schizophrenia.” Health Psychology Research (2021): 24932.

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