Sarizotan EMD 128130|cas:351862-32-3|西域试剂

Sarizotan EMD 128130,98.74%

产品编号：Bellancom-100820| CAS NO：351862-32-3| 分子式：C₂₂H₂₁FN₂O| 分子量：348.41

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货号	价格	库存与货期
Bellancom-100820	￥2500.00	杭州北京（现货）
Bellancom-100820	￥3800.00	杭州北京（现货）
Bellancom-100820	￥7500.00	杭州北京（现货）
Bellancom-100820	￥12000.00	杭州北京（现货）

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Sarizotan EMD 128130

产品介绍

Sarizotan (EMD 128130) 是具有口服活性的 5-HT_1A 受体 和多巴胺受体的激动剂，其 IC₅₀ 值分别为 6.5 nM (rat 5-HT_1A)、 0.1 nM (human 5-HT_1A)、15.1 nM (rat D₂)、17 nM (human D₂)、6.8 nM (human D₃) 和 2.4 nM (human D_4.2)。

生物活性

Sarizotan (EMD 128130) is an orally active serotonin 5-HT_1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively.

体外研究

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

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

体内研究

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.
Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease.
Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats.

西域 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).
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).

体内研究

西域 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).
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).

性状

Viscous liquid

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式