Lumateperone( ITI-007 )

Catalog No. M14006 CAS No. 313368-91-1

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HNMR

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Product Name

Lumateperone
Note

Research use only, not for human use.
Brief Description

Lumateperone (ITI-007) is a potent 5-HT2A antagonist (Ki=0.54 nM), postsynaptic D2 antagonist(Ki=32 nM), and SERT blocker (Ki= 61 nM).
Description

Lumateperone (ITI-007) is a potent 5-HT2A antagonist (Ki=0.54 nM), postsynaptic D2 antagonist(Ki=32 nM), and SERT blocker (Ki= 61 nM); also shows affinity for D1; orally bioavailable and exhibits good antipsychotic efficacy in vivo.Schizophrenia Phase 3 Clinical.
In Vitro

Lumateperone (2-30 μM) has anti-tumor activity and can inhibit cell proliferation in a dose-dependent manner. Cell Proliferation Assay 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. Animal Model:Adult male Sprague-Dawley rats Dosage:1-10mg/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.
Synonyms

ITI-007
Pathway

GPCR/G Protein
Target

5-HT Receptor
Recptor

5-HT Receptor
Research Area

Neurological Disease
Indication

Schizophrenia

CAS Number

313368-91-1
Formula Weight

393.496
Molecular Formula

C24H28FN3O
Purity

>98% (HPLC)
Solubility

——
SMILES

O=C(C1=CC=C(F)C=C1)CCCN2CC[C@@](N3CCN(C)C4=C3C5=CC=C4)([H])[C@@]5([H])C2
Chemical Name

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

1. Li P, et al. J Med Chem. 2014 Mar 27;57(6):2670-82. 2. Snyder GL, et al. Psychopharmacology (Berl). 2015 Feb;232(3):605-21.

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