2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. Sarizotan

Sarizotan  (Synonyms: EMD 128130)

目录号: HY-100820 纯度: 98.74%
COA 产品使用指南

摩尔计算器

Sarizotan (EMD 128130) 是具有口服活性的 5-HT1A 受体 和多巴胺受体的激动剂，其 IC50 值分别为 6.5 nM (rat 5-HT1A)、 0.1 nM (human 5-HT1A)、15.1 nM (rat D2)、17 nM (human D2)、6.8 nM (human D3) 和 2.4 nM (human D4.2)。

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Sarizotan Chemical Structure

Sarizotan Chemical Structure

CAS No. : 351862-32-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2750
In-stock
5 mg ￥2500
In-stock
10 mg ￥3800
In-stock
25 mg ￥7500
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Sarizotan 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

查看 Dopamine Receptor 亚型特异性产品:

查看所有亚型
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively[1].

IC50 & Target[1]

5-HT1A Receptor

6.5 nM (IC50, rat)

5-HT1A Receptor

0.1 nM (IC50, human)

rD2 Receptor

15.1 nM (IC50, rat)

D3 Receptor

6.8 nM (IC50, human)

5-HT1B Receptor

600 nM (IC50, rat)

5-HT1D Receptor

500 nM (IC50, calf)

5-HT2A Receptor

960 nM (IC50, rat, agonist site)

5-HT2A Receptor

587 nM (IC50, human, antagonist site)

5-HT2B Receptor

108 nM (IC50, human)

5-HT2C Receptor

800 nM (IC50, pig)

5-HT3 Receptor

3500 nM (IC50, NG 108 cells)

5-HT5A Receptor

313 nM (IC50, human)

5-HT6 Receptor

3300 nM (IC50, human)

5-HT7 Receptor

10 nM (IC50, human)

hD4.2 Receptor

2.4 nM (IC50)

hD2 Receptor

17 nM (IC50)

体外研究
(In Vitro)

Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC50 value of 150 nM (Emax 40% at 1 mM) [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Sarizotan 相关抗体:
体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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).
Clinical Trial
分子量

348.41

Formula

C22H21FN2O
CAS 号
性状

粘稠液体

颜色

Colorless to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (287.02 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8702 mL 14.3509 mL 28.7018 mL
5 mM 0.5740 mL 2.8702 mL 5.7404 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Sarizotan 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8702 mL 14.3509 mL 28.7018 mL 71.7545 mL
5 mM 0.5740 mL 2.8702 mL 5.7404 mL 14.3509 mL
10 mM 0.2870 mL 1.4351 mL 2.8702 mL 7.1755 mL
15 mM 0.1913 mL 0.9567 mL 1.9135 mL 4.7836 mL
20 mM 0.1435 mL 0.7175 mL 1.4351 mL 3.5877 mL
25 mM 0.1148 mL 0.5740 mL 1.1481 mL 2.8702 mL
30 mM 0.0957 mL 0.4784 mL 0.9567 mL 2.3918 mL
40 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7939 mL
50 mM 0.0574 mL 0.2870 mL 0.5740 mL 1.4351 mL
60 mM 0.0478 mL 0.2392 mL 0.4784 mL 1.1959 mL
80 mM 0.0359 mL 0.1794 mL 0.3588 mL 0.8969 mL
100 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7175 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sarizotan351862-32-3EMD 128130EMD128130EMD-1281305-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorParkinson’sdiseaseDOPAdyskinesiaInhibitorinhibitorinhibit

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