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Guanethidine Sulfate

现货
Catalog No.
A8443
抗高血压化合物
组合的产品项目
规格价格库存 数量
1g
¥ 800.00
现货
5g
¥ 2,400.00
Ship with 10-15 days

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Background

Guanethidine Sulfate is an anti-hypertensive drug involved in reducing the release of catecholamines such as norepinephrine [1].

In vitro: Guanethidine (0.1 and 1 μM) decreased S-I efflux but increased resting efflux in a concentration dependent manner[1].On the electrically stimulated mouse vas deferens, Guanethidine (3 μM) treatment inhibited twitching by 95% ± 3% in 15 min, but this effect was only partially reversed after 1 h of washing (33% ± 12% of control). When guanethidine were used in combination with prilocaine, a reversal of 80% ± 13% (at 1 h) was observed. When co-incubated with guanethidine (3 μM), the twitch was reduced to 24% ± 4% of control and was reversed to 77% ± 7% after 1 h. The reversal produced by the combination was significantly more intense (P < 0.05) when compared with guanethidine alone. Local anesthetics reduced the sympatholytic actions of guanethidine, and this could explain the variable efficacy of guanethidine in the treatment of complex regional pain syndrome [2].

References:
[1]. Fabiani ME1,Story DF. Inhibition of sympathetic noradrenergic transmission by guanabenz and guanethidine in rat isolated mesenteric artery: involvement of neuronal potassium channels.Pharmacol Res.1996 Mar;33(3):171-80.
[2]. Joyce PI1,Rizzi D,Caló G,Rowbotham DJ,Lambert DG. The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens.Anesth Analg.2002 Nov;95(5):1339-43, table of contents.

文献引用

1. Turner T, Chen X, et al. "FGF21 increases water intake, urine output and blood pressure in rats." PLoS One. 2018 Aug 14;13(8):e0202182. PMID:30106981

Chemical Properties

StorageStore at -20°C
M.Wt494.7
Cas No.60-02-6
FormulaC20H44N8.H2O4S
Solubility≥159.4mg/mL in H2O, <0.99mg/mL in DMSO
Chemical Name1-(2-(azocan-1-yl)ethyl)guanidine hemisulfate
SDFDownload SDF
Canonical SMILESOS(O)(=O)=O.N=C(N)NCCN1CCCCCCC1.N=C(N)NCCN2CCCCCCC2
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

电刺激的小鼠输精管

溶解方法

该化合物可溶于DMSO。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

3 μM

应用

在电刺激的小鼠输精管中,Guanethidine sulfate在15分钟内抑制了95%±3%的抽搐,但是在洗涤1小时后(对照的33%±12%),该作用仅部分逆转。

动物实验[1]:

动物模型

心肌梗死(MI)大鼠模型

剂量

低剂量[LG],1 mg/kg/day; 中等剂量,3 mg/kg/day; 高剂量,10 mg/kg/day; 通过渗透性微型泵给药4周

应用

在心肌梗死(MI)大鼠中,LG抑制左心室(LV)扩张(9.2±0.9mm vs.11.0±0.8mm),改善LV分数缩短(25.0±4.5%vs. 16.4±4.7%),并与血浆NE水平的减少有关(520±250pg / ml vs.1000±570pg / ml)。低剂量guanethidine减少24小时(6%)和28天死亡率(6%)。高剂量guanethidine也降低24小时死亡率(12%),但增加28天死亡率(91%)。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Joyce PI1,Rizzi D,Caló G,Rowbotham DJ,Lambert DG. The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens.Anesth Analg.2002 Nov;95(5):1339-43, table of contents.

[2]. Igawa A1, Nozawa T, Fujii N, et al. Long-term treatment with low-dose, but not high-dose, guanethidine improves ventricular function and survival of rats with heart failure after myocardial infarction. J Am Coll Cardiol. 2003 Aug 6;42(3):541-8.

质量控制

化学结构

Guanethidine Sulfate

相关生物数据

Guanethidine Sulfate