NAS-181 dimesylate|cas:1217474-40-2|西域试剂

NAS-181 dimesylate,98.44%

产品编号：Bellancom-103156| CAS NO：1217474-40-2| 分子式：C₂₁H₃₄N₂O₁₀S₂| 分子量：538.63

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货号	价格	库存与货期
Bellancom-103156	￥2800.00	杭州北京（现货）
Bellancom-103156	￥4500.00	杭州北京（现货）
Bellancom-103156	￥9000.00	杭州北京（现货）
Bellancom-103156	￥15000.00	杭州北京（现货）

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NAS-181 dimesylate

产品介绍

NAS181 是一种有效和选择性的大鼠 5-HT_1B 受体拮抗剂，K_i 值为 47 nM。NAS181 对 r5-HT_1B 的选择性比牛 5-HT_1B 受体 (K_i=630 nM) 高 13 倍。NAS181 通过抑制末端 r5-HT_1B 自身受体来增加 5-HT 转换和 5-HT 的突触浓度。

生物活性

NAS181 is a potent and selective antagonist of rat 5-HT_1B receptor, with a K_i of 47 nM. NAS181 shows 13-fold selectivity for r5-HT_1B over bovine 5-HT_1B receptor (K_i=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT_1B autoreceptors.

体外研究

NAS181 has very low affinities (K_i>3000 nM) for all other receptors examined, including 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7, α1-, α2-, and β-adrenoceptors, and dopamine D1 and D2.
NAS181 (10-1000 nM) dose-dependently potentiates the K⁺-stimulated [³H]-5-HT release in preloaded rat occipital cortical slices.

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

体内研究

NAS181 (1-10 mg/kg; s.c.) dose-dependently increases acetylcholine (ACh) release in the frontal, ventral hippocampus cortex and VHipp.
NAS181 (20 mg/kg; s.c.) enhances the 5-HT turnover in four rat brain regions (hypothalamus, hippocampus, striatum, and frontal cortex) with about 40%.
NAS181 (3 mg/kg; s.c.) produces a significant increase in the number of wet dog shakes in rats.

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

Animal Model:	Adult male Sprague-Dawley rats (250-300 g)
Dosage:	1, 5, 10 mg/kg
Administration:	S.c. in the scruff of the neck
Result:	Increased the ACh release in the frontal cortex, reaching the maximal value of 500% of the control group within 80 min after the injection of the highest dose. Increased the ACh releases in VHipp with a maximum of 230% of the control values at 80 min after the injection of the highest dose.

体内研究

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

Animal Model:	Adult male Sprague-Dawley rats (250-300 g)
Dosage:	1, 5, 10 mg/kg
Administration:	S.c. in the scruff of the neck
Result:	Increased the ACh release in the frontal cortex, reaching the maximal value of 500% of the control group within 80 min after the injection of the highest dose. Increased the ACh releases in VHipp with a maximum of 230% of the control values at 80 min after the injection of the highest dose.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (116.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8566 mL	9.2828 mL	18.5656 mL
5 mM	0.3713 mL	1.8566 mL	3.7131 mL
10 mM	0.1857 mL	0.9283 mL	1.8566 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 (sealed storage, away from moisture)。-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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献