Guanethidine Sulfate
(Synonyms: 硫酸胍乙啶; Guanethidine monosulfate) 目录号 : GC15934
An antihypertensive agent
Cas No.:645-43-2
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
the electrically stimulated mouse vas deferens |
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Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
3 μM |
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Applications |
In the electrically stimulated mouse vas deferens, Guanethidine sulfate inhibited twitching by 95%±3% in 15 min, but this effect was only partially reversed after 1 h of washing (33%±12% of control). |
| Animal experiment [1]: | |
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Animal models |
Myocardial infarction (MI) rat model |
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Dosage form |
low-dose [LG], 1 mg/kg/day; medium-dose, 3 mg/kg/day; high-dose, 10 mg/kg/day; administered via an osmotic mini-pump for 4 weeks |
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Application |
In myocardial infarction (MI) rats, LG suppressed left ventricular (LV) dilation (9.2±0.9 mm vs.11.0±0.8 mm) and improved LV fractional shortening (25.0±4.5% vs. 16.4±4.7%) in association with a reduction of plasma NE levels (520±250 pg/ml vs.1,000±570 pg/ml). Low-dose guanethidine reduced 24-h (6%) and 28-day mortality (6%). High-dose guanethidine also reduced 24-h mortality (12%) but increased 28-day mortality (91%). |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| Cas No. | 645-43-2 | SDF | |
| 别名 | 硫酸胍乙啶; Guanethidine monosulfate | ||
| 化学名 | 2-[2-(azocan-1-yl)ethyl]guanidine;sulfuric acid | ||
| Canonical SMILES | C1CCCN(CCC1)CCN=C(N)N.C1CCCN(CCC1)CCN=C(N)N.OS(=O)(=O)O | ||
| 分子式 | C10H24N4O4S | 分子量 | 296.39 |
| 溶解度 | ≥ 159.4mg/mL in Water | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3739 mL | 16.8697 mL | 33.7393 mL |
| 5 mM | 0.6748 mL | 3.3739 mL | 6.7479 mL |
| 10 mM | 0.3374 mL | 1.687 mL | 3.3739 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet