Spiradoline U-62066|cas:87151-85-7|西域试剂

Spiradoline U-62066

产品编号：Bellancom-106756| CAS NO：87151-85-7| 分子式：C₂₂H₃₀Cl₂N₂O₂| 分子量：425.39

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货号	价格	库存与货期
Bellancom-106756	￥1450.00	杭州北京（现货）
Bellancom-106756	￥2500.00	杭州北京（现货）
Bellancom-106756	￥4500.00	杭州北京（现货）

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Spiradoline U-62066

产品介绍

Spiradoline (U-62066) 是一种芳基乙酰胺，是一种选择性 kappa 阿片受体 (κ-opioid receptor, KOR) 激动剂，在豚鼠中的 K_i 为 8.6 nM。Spiradoline 对 μ 和 δ 受体的 K_i 值分别为 252 nM 和 9400 nM。Spiradoline 具有强效的利尿，止痛，抗心律失常，镇咳，神经保护作用，并易于穿过血脑屏障。

生物活性

Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a K_i of 8.6 nM in guinea pig. The K_i values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier.

体外研究

Using the patch-clamp method in isolated rat cardiac myocytes, indicated that Spiradoline (15 to 500 μM) produces its antiarrythmic effect via blockade of sodium channels (and at the higher doses also of potassium currents) in myocardial tissue. Thus, Spiradoline reduces the peak sodium current, increased the decay rate of the transient outward potassium current, and reduced the sustained plateau potassium amplitude.

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

体内研究

Spiradoline (U-62066; 0.1-0.4 mg/kg; subcutaneous injection; once; Sprague-Dawley rats) treatment dose-dependently reduces social behaviors in non-stressed adults, producing social avoidance at the highest dose tested, while younger animals displays reduced sensitivity to this socially suppressing effect of Spiradoline. In stressed animals, the socially suppressing effects of the Spiradoline are blunted at all ages, with juveniles and adolescents exhibiting increased social preference in response to certain doses of U-62066.

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

Animal Model:	Juvenile, adolescent and adult Sprague-Dawley male and female rats exposured to repeated restraint
Dosage:	0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4 mg/kg
Administration:	Subcutaneous injection; once
Result:	Dose-dependently reduced social behaviors in non-stressed adults, producing social avoidance at the highest dose tested.

体内研究

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

Animal Model:	Juvenile, adolescent and adult Sprague-Dawley male and female rats exposured to repeated restraint
Dosage:	0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4 mg/kg
Administration:	Subcutaneous injection; once
Result:	Dose-dependently reduced social behaviors in non-stressed adults, producing social avoidance at the highest dose tested.

性状

溶解性数据

In Vitro:

DMSO : 50 mg/mL (117.54 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3508 mL	11.7539 mL	23.5078 mL
5 mM	0.4702 mL	2.3508 mL	4.7016 mL
10 mM	0.2351 mL	1.1754 mL	2.3508 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.88 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.88 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.88 mM); Suspended solution

此方案可获得 ≥ 2.5 mg/mL (5.88 mM，饱和度未知) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。