|1-(4-氟苯基)-4-((6bR,10aS)-3-甲基2,3,6b,7,10,10a-六氢-1H-吡啶并[3',4' :4,5]吡咯并[1,2,3-de]喹喔啉-8(9H) -基)丁-1-酮 4-甲基苯磺酸盐|CsnPharm

CAS No.: 1187020-80-9

Lumateperone tosylate Catalog No. CSN17035

Synonyms: ITI-007 tosylate;ITI-007;ITI 722

Lumateperone tosylate 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 SERT blocker (Ki = 61 nM).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 5-HT Receptor 2A

Ki:0.54nM
描述Lumateperone tosylate 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 SERT blocker (Ki = 61 nM). Lumateperone uniquely acts as an indirect modulator of glutamatergic phosphoprotein with D1-dependent augmentation of both NMDA and AMPA activity via the mammalian target of rapamycin (mTOR) pathway, mechanisms thought to predict potent and rapid antidepressant effects^[3]. One antipsychotic agent, lumateperone tosylate, is a newer agent that the FDA recently approved. Lumateperone tosylate is an FDA-approved drug that can be given only at the 42mg dose once daily with no titration requirement^[4]. Besides, Lumateperone has demonstrated a favourable safety profile without significant extrapyramidal side effects, hyperprolactinemia or changes in cardiometabolic or endocrine factors versus placebo^[5]. Lumateperone demonstrated efficacy for improving the symptoms of schizophrenia and had a favorable safety profile^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7677 mL
- 8.8386 mL
- 17.6773 mL
- 5 mM
- 0.3535 mL
- 1.7677 mL
- 3.5355 mL
- 10 mM
- 0.1768 mL
- 0.8839 mL
- 1.7677 mL

技术信息

CAS号

1187020-80-9

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H36FN3O4S

运输

蓝冰

分子量

565.70

别名

ITI-007 tosylate;ITI-007;ITI 722;Lumateperone (tosylate);Lumateperone;Caplyta,

溶解度

DMSO	95.0 mg/mL (167.9 mM) warming
Water	Insoluble

动物实验配方

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