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Sarizotan

产品编号 T40439 CAS 351862-32-3

别名: EMD 128130

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 .

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Sarizotan, CAS 351862-32-3

规格	价格/CNY	货期
2 mg	￥ 1,220	5日内发货
5 mg	￥ 2,270	5日内发货
25 mg	￥ 7,690	6-8周
50 mg	￥ 9,990	6-8周
1 mL * 10 mM (in DMSO)	￥ 2,280	5日内发货

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Sarizotan 的其他形式现货产品:

Sarizotan HCl

其他形式的 Sarizotan:

Sarizotan HCl
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 .
靶点活性	5-HT2A receptor:587 nM (IC50, human, antagonist site), 5-HT2A receptor:960 nM (IC50, rat, agonist site), 5-HT2C receptor:800 nM (IC50, pig), 5-HT6 receptor:3300 nM (IC50, human), 5-HT7 receptor:10 nM (IC50, human), 5-HT3 receptor:3500 nM (IC50, NG 108 cells), D3 receptor:6.8 nM (IC50, human), 5-HT2B receptor:108 nM (IC50, human), 5-HT1A receptor:0.1 nM (IC50, human), 5-HT1A receptor:6.5 nM (IC50, rat), 5-HT1B receptor:600 nM (IC50, rat), 5-HT5A receptor:313 nM (IC50, human), D 4.2:2.4 nM (IC50, human), D2 receptor:15.1 nM (IC50, rat), D2 receptor:17 nM (IC50, human), 5-HT1D receptor:500 nM (IC50, calf)
体外活性	Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC 50 value of 150 nM (E max 40% at 1 mM)[1].
体内活性	Sarizotan (3, 10 mg/kg, po) at the higher dose slightly decreases 5-HT in the striatum and its metabolite 5-HIAA in frontal cortex and hippocampus. Sarizotan (10 mg/kg, po) substantially increases the DA metabolites DOPAC and HVA in the striatum and frontal cortex[1]. Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease[1]. Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats[2]. Animal Model: Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response)[2]. Dosage: 1 ng, 10 ng and 1 μg in 0.3 μL solution. Administration: Administered via an injection cannula inserted to the guide cannula through the STN (V -8.4 mm from skull) with the injection cannula connected to a 10-μL syringe and mounted on a microinfusion pump for 22 consecutive days. Result: On day 23, the subthalamic administration of Sarizotan at the higher doses tested (10 ng and 1 μg) significantly decreased the total dyskinesia score in levodopa-treated rats in comparison with the rats treated only with levodopa (p<0.05, p<0.01, respectively).

别名	EMD 128130
分子量	348.421
分子式	C22H21FN2O
CAS No.	351862-32-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. G D Bartoszyk, et al. Sarizotan, a Serotonin 5-HT1A Receptor Agonist and Dopamine Receptor Ligand. J Neural Transm (Vienna). 2004 Feb;111(2):113-26. 2. C Marin, et al. Local Administration of Sarizotan Into the Subthalamic Nucleus Attenuates Levodopa-Induced Dyskinesias in 6-OHDA-lesioned Rats. Psychopharmacology (Berl). 2009 Jun;204(2):241-50.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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