lumateperone (Tosylate)

Synonym(s):1-(4-Fluorophenyl)-4-[(6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl]butan-1-one 4-methylbenzenesulfonate;4-((6bR,10aS)-3-Methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-1-(4-fluorophenyl)-butan-1-one 4-methylbenzenesulfonate;ITI-007

CAS NO.：1187020-80-9
Empirical Formula: C31H36FN3O4S
Molecular Weight: 565.7
MDL number: MFCD29922434
Update Date: 2025-12-15 16:23:17

What is lumateperone (Tosylate)?

The Uses of lumateperone (Tosylate)

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.

Properties of lumateperone (Tosylate)

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

Safety information for lumateperone (Tosylate)

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07 Health Hazard GHS08
GHS Hazard Statements	H336:Specific target organ toxicity,single exposure; Narcotic effects
Precautionary Statement Codes	P202:Do not handle until all safety precautions have been read and understood. P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. P308+P313:IF exposed or concerned: Get medical advice/attention.

Computed Descriptors for lumateperone (Tosylate)

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\|