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Lumateperone

Cat. No. M29891
Lumateperone Structure
Synonym:

ITI-007

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Biological Activity

Lumateperone (ITI-007) 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 dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.

Chemical Information
Molecular Weight 393.5
Formula C24H28FN3O
CAS Number 313368-91-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. Lumateperone

[2] Amber Edinoff, et al. Psychopharmacol Bull. Lumateperone for the Treatment of Schizophrenia

[3] Jessica Greenwood, et al. Ann Pharmacother. Lumateperone: A Novel Antipsychotic for Schizophrenia

[4] Hannah A Blair. Drugs. Lumateperone: First Approval

[5] Christoph U Correll, et al. JAMA Psychiatry. Efficacy and Safety of Lumateperone for Treatment of Schizophrenia: A Randomized Clinical Trial

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