Lumateperone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Lumateperone (ITI-007) 是一种有效的 5-HT2A 拮抗剂 (Ki=0.54 nM)、突触后 D2 拮抗剂 (Ki=32 nM) 和 SERT 阻滞剂 (Ki= 61 nM)。

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.

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.

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.

ITI-007

GPCR/G Protein

5-HT Receptor

5-HT Receptor

Neurological Disease

Schizophrenia

313368-91-1

393.496

C24H28FN3O

>98% (HPLC)

——

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

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

(-20℃)

With Ice Pack

≥ 2 years