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

Sarizotan (Synonyms: EMD 128130)

目录号: HY-100820 纯度: 98.74%
产品使用指南

Sarizotan (EMD 128130) 是具有口服活性的 5-HT1A 受体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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Top Publications Citing Use of Products
  • 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

5-HT1A Receptor

6.5 nM (IC50, rat)

5-HT1A Receptor

0.1 nM (IC50, human)

D2 Receptor

15.1 nM (IC50, rat)

D2 Receptor

17 nM (IC50, human)

D3 Receptor

6.8 nM (IC50, human)

D4.2

2.4 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)

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.

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
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 : 100 mg/mL (287.02 mM; Need ultrasonic)

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
10 mM 0.2870 mL 1.4351 mL 2.8702 mL
*

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。

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
Sarizotan
目录号:
HY-100820
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