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鲁拉西酮 /Lurasidone {[allProObj[0].p_purity_real_show]}

货号:A418721 同义名: SM-13496

Lurasidone functions as an antagonist of the dopamine D2 and D3 receptors, the serotonin 5-HT2A and 5-HT7 receptors, the α2C-adrenergic receptor, and as a partial agonist of the serotonin 5-HT1A receptor.

Lurasidone 化学结构 CAS号:367514-87-2
Lurasidone 化学结构
CAS号:367514-87-2
Lurasidone 3D分子结构
CAS号:367514-87-2
Lurasidone 化学结构 CAS号:367514-87-2
Lurasidone 3D分子结构 CAS号:367514-87-2
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Lurasidone 纯度/质量文件 产品仅供科研

货号:A418721 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 D1 receptor D2 receptor D3 receptor D4 receptor D5 receptor DAT Dopamine receptor 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 95%
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

98%
Levosulpiride 99+%
Pridopidine 95%
Metoclopramide 99+%
Molindone HCl 98%
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

98+%
Phenothiazine 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

+++

Dopamine D2 receptor, Ki: 3.0 nM

++++

Dopamine D3 receptor, Ki: 0.83 nM

98%
Rotundine ++

D1 receptor, IC50: 166 nM

+

D2 receptor, IC50: 1.47 μM

+

D3 receptor, IC50: 3.25 μM

98%
Domperidone 99+%
ONC206 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

+++

Dopamine D2 Receptor, pKi: 8.19

++

Dopamine D4.4 Receptor, pKi: 7.54

97%
Loxapine succinate ++

D1 receptor (human), Ki: 26 nM

D2 receptor (Human), Ki: 62 nM

++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 nM

+++

D4 receptor (human), Ki: 7.5 nM

99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

+++

D2 receptor, Ki: 2.96 nM

+++

D3 receptor, Ki: 4.56 nM

+++

D5 receptor, Ki: 9 nM

98%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

++++

D5 dopamine receptor, Ki: 0.3 nM

98%
MPP+ iodide 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

97%
Benztropine mesylate ++

DAT, IC50: 118 nM

98%
Azaperone 98%
Ziprasidone HCl 98+%
Paliperidone 98%
Alizapride HCl 99+%
Amisulpride 98%
Quetiapine hemifumarate Adrenergic Receptor 98%
Clozapine N-oxide 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Lurasidone 生物活性

靶点
  • D2 receptor

    D2 receptor, IC50:1.68 nM

  • D2 receptor

    D2 receptor, Ki:1 nM

描述 Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM. In vitro receptor binding experiments reveal that Lurasidone (SM-13496) demonstrates affinity for dopamine D2 and 5-HT2A receptors higher than other tested antipsychotics. Lurasidone (SM-13496) dose-dependently increases the ratio of DOPAC/dopamine in frontal cortex and striatum, but it shows a preferential effect on the frontal cortex compare with the striatum, especially at higher doses. Lurasidone (SM-13496) (ED50 values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED50 values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED50 9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED50 values 0.44 to 1.7 mg/kg). Lurasidone (SM-13496) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED50 values are 6.3 mg/kg. Lurasidone (SM-13496) dose-dependently inhibits tryptamine (TRY)-induced forepaw clonic seizure and p-chloroamphetamine (p-CAMP)-induced hyperthermia with ED50 values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (SM-13496) (0.3 to 30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the conflict test with MED of 10 mg/kg[1]. 80 mg/d lurasidone, an effective and tolerable dose for non-TRS (treatment-resistant schizophrenia) patients, was also effective in TRS patients but required longer duration of treatment[2]. In the ITT (intention-to-treat) (but not the mITT) population, treatment with lurasidone was associated with significant improvement in the PANSS (Positive and Negative Syndrome Scale) total score in patients with schizophrenia. Lurasidone was generally well tolerated with minimal impact on weight and metabolic parameters[3].

Lurasidone 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02181803 Schizophrenia Phase 1 Completed - -
NCT01431326 - Recruiting February 2020 -
NCT01364818 - Completed - United States, North Carolina ... 展开 >> University of North Carolina Chapel Hill Chapel Hill, North Carolina, United States, 27599 收起 <<

Lurasidone 参考文献

[1]Ishibashi T, Horisawa T, Tokuda K, Ishiyama T, Ogasa M, Tagashira R, Matsumoto K, Nishikawa H, Ueda Y, Toma S, Oki H, Tanno N, Saji I, Ito A, Ohno Y, Nakamura M. Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010 Jul;334(1):171-81

[2]Meltzer HY, Share DB, Jayathilake K, Salomon RM, Lee MA. Lurasidone Improves Psychopathology and Cognition in Treatment-Resistant Schizophrenia. J Clin Psychopharmacol. 2020 May/Jun;40(3):240-249

[3]Higuchi T, Ishigooka J, Iyo M, Yeh CB, Ebenezer EG, Liang KY, Lee JS, Lee SY, Lin SK, Yoon BH, Nakamura M, Hagi K, Sato T. Lurasidone in the treatment of schizophrenia: Results of a double-blind, placebo-controlled trial in Asian patients. Asia Pac Psychiatry. 2019 Jun;11(2):e12352

Lurasidone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.15mL

2.03mL

1.01mL

20.30mL

4.06mL

2.03mL

Lurasidone 技术信息

CAS号367514-87-2
分子式C28H36N4O2S
分子量 492.676
别名 SM-13496
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 20 mg/mL(40.59 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 3 mg/mL(6.09 mM),配合低频超声,并水浴加热至45℃助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方
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