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Sarizotan
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Sarizotan图片
CAS NO:351862-32-3
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
EMD 128130
产品介绍
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)。
生物活性

Sarizotan (EMD 128130) is an orally active serotonin5-HT1Areceptoranddopamine receptoragonist. Sarizotan (EMD 128130) exhibitsIC50values 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-HT1AReceptor

6.5 nM (IC50, rat)

5-HT1AReceptor

0.1 nM (IC50, human)

rD2Receptor

15.1 nM (IC50, rat)

D3Receptor

6.8 nM (IC50, human)

5-HT1BReceptor

600 nM (IC50, rat)

5-HT1DReceptor

500 nM (IC50, calf)

5-HT2AReceptor

960 nM (IC50, rat, agonist site)

5-HT2AReceptor

587 nM (IC50, human, antagonist site)

5-HT2BReceptor

108 nM (IC50, human)

5-HT2CReceptor

800 nM (IC50, pig)

5-HT3Receptor

3500 nM (IC50, NG 108 cells)

5-HT5AReceptor

313 nM (IC50, human)

5-HT6Receptor

3300 nM (IC50, human)

5-HT7Receptor

10 nM (IC50, human)

hD4.2Receptor

2.4 nM (IC50)

hD2Receptor

17 nM (IC50)

体外研究
(In Vitro)

Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC50value of 150 nM (Emax40% at 1 mM)[1].

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].

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

性状

Viscous liquid

Formula

C22H21FN2O

CAS 号

351862-32-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.8702 mL14.3509 mL28.7018 mL
5 mM0.5740 mL2.8702 mL5.7404 mL
10 mM0.2870 mL1.4351 mL2.8702 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。