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ITI-722

Names

[ CAS No. ]:
313368-91-1

[ Name ]:
ITI-722

[Synonym ]:
Lumateperone
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]-1-butanone
1-Butanone, 1-(4-fluorophenyl)-4-[(6bR,10aS)-2,3,6b,9,10,10a-hexahydro-3-methyl-1H-pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl]-
UNII:70BSQ12069
ITI-007
ITI-722

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[In Vitro]

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

[References]

[1]. Jinyuan Zhang, et al. Identification of Trovafloxacin, Ozanimod, and Ozenoxacin as Potent c-Myc G-quadruplex Stabilizers to Suppress c-Myc Transcription and Myeloma Growth. Mol Inform. 2022 Mar 30:e2200011.

[2]. J Titulaer, et al. Lumateperone-mediated effects on prefrontal glutamatergic receptor-mediated neurotransmission: A dopamine D1 receptor dependent mechanism. Eur Neuropsychopharmacol. 2022 Jul 22;62:22-35.

[3]. Lumateperone

Chemical & Physical Properties

[ Density]:
1.3±0.0 g/cm3

[ Boiling Point ]:
556.4±0.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H28FN3O

[ Molecular Weight ]:
393.497

[ Flash Point ]:
290.3±0.0 °C

[ Exact Mass ]:
393.221649

[ LogP ]:
3.39

[ Vapour Pressure ]:
0.0±0.0 mmHg at 25°C

[ Index of Refraction ]:
1.646

Related Compounds