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Guanethidine Sulfate Antihypertensive compound

Catalog No.A8443
Size Price Stock Qty
1g
$80.00
In stock
5g
$240.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Guanethidine Sulfate

Protocol

Cell experiment [1]:

Cell lines

the electrically stimulated mouse vas deferens

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.

Reacting condition

3 μM

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]:

Animal models

Myocardial infarction (MI) rat model

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

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%).

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.

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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Chemical Properties

Cas No. 60-02-6 SDF Download SDF
Chemical Name 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
Formula C20H44N8.H2O4S M.Wt 494.7
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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.