Lumateperone

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Lumateperone

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

313368-91-1

ITI-007

Lumateperone (ITI-007) 是一种5-HT2A受体拮抗剂 (Ki = 0.54 nM)、突触前 D2 受体的部分激动剂和突触后 D2 受体的拮抗剂 (Ki = 32 nM)、多巴胺 D1 受体调节剂。Lumateperone 具有抗癌活性, 可用于精神分裂症等相关精神病的研究。

生物活性

Lumateperone (ITI-007) is a5-HT2Areceptor 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].

体外研究
(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 IC₅₀value of 17.30 μM.

体内研究
(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.

Clinical Trial

分子量

393.50

Formula

C₂₄H₂₈FN₃O

CAS 号

313368-91-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.