2. Lumateperone

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Lumateperone tosylate) usually boasts enhanced water solubility and stability.

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Lumateperone Chemical Structure

Lumateperone Chemical Structure

CAS No. : 313368-91-1

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Lumateperone Related Antibodies

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Description

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[1][2][3].

In Vitro

Lumateperone (2-30 μM) has anti-tumor activity and can inhibit cell proliferation in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lumateperone Related Antibodies

Cell Proliferation Assay[1]

Cell Line: RPMI-8226 cells
Concentration: 2-30 μM
Incubation Time: 48 hours
Result: Inhibited cell growth with the IC50 value of 17.30 μM.
In Vivo

Lumateperone (i.p., 1-10 mg/kg) promotes NMDA and AMPA-induced currents in a dopamine D1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male Sprague-Dawley rats[2]
Dosage: 1-10 mg/kg
Administration: Intraperitoneal injection
Result: Inhibited avoidance response at concentrations of 1, 3 and 10 mg/kg after 20 minutes.
Promoted NMDA and AMPA-sensitive currents, also significantly increased dopamine and glutamate release at 10 mg/kg in mPFC cone cells of rat.
Clinical Trial
Molecular Weight

393.50

Formula

C24H28FN3O
CAS No.
SMILES

CN1C2=C3C([C@@]4([H])[C@@](CCN(C4)CCCC(C5=CC=C(C=C5)F)=O)([H])N3CC1)=CC=C2
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lumateperone313368-91-1ITI-007ITI007ITI 007Inhibitorinhibitorinhibit

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