| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Guanethidine targets the sympathetic nervous system by inhibiting the release of norepinephrine from post-ganglionic adrenergic nerve terminals. It competes with norepinephrine for uptake into presynaptic terminals via the norepinephrine transporter. By blocking the release of norepinephrine, it reduces sympathetic tone, leading to vasodilation and decreased blood pressure.
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| ln Vitro |
Guanethidine is not typically used in standard pharmacological activity assays. Its activity is characterized by its ability to inhibit the release of norepinephrine. This can be assessed in isolated tissue preparations or by measuring neurotransmitter release in cell-based assays. Its antihypertensive effects are well-established.
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| ln Vivo |
Guanetidine (5–40 mg/kg; i.p.; daily; 4-28 days; male Wistar rats) Treatment at 40 mg/kg for 28 days causes partial sympathectomy and related reaction to norepinephrine; however, 5 mg/kg does not result in permanent hemodynamic alterations or histological changes [3].
Guanethidine is used in vivo as an antihypertensive agent to lower blood pressure. It is effective in treating high blood pressure, particularly in patients who do not respond to other antihypertensives. Its use has also been explored in the relief of chronic pain caused by complex regional pain syndrome. It is administered orally. |
| Enzyme Assay |
The in vitro activity of Guanethidine can be assessed by measuring its ability to inhibit norepinephrine uptake in neuronal cell cultures or synaptosomal preparations. Radiolabeled norepinephrine is used to track uptake, and the inhibition by the compound is measured. Its effects on neurotransmitter release can be assessed in isolated tissue preparations.
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| Cell Assay |
Cellular assays for Guanethidine involve treating neuronal cells with the compound and measuring its effects on norepinephrine uptake and release. The inhibition of uptake is measured using radiolabeled norepinephrine. The effects on neurotransmitter release can be assessed by stimulating the cells and measuring the amount of norepinephrine released into the medium.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat (approximately 200 grams) [3]
Doses: 5 mg/kg or 40 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; continued for 4, 8, 14 or 28 days Experimental Results: blood pressure diminished by 40 mg/kg, the decrease in blood pressure can be reversed after stopping the drug. The hypersensitivity reaction was partially reversible after discontinuation of the drug, but a significant increase in heart rate sensitivity to norepinephrine was observed 60 days after discontinuation of the drug, and 40 mg/kg was administered for 28 days. Histologically, severe loss of superior cervical ganglion nerve cells was observed at the 40 mg/kg dose. In vivo animal experiments for Guanethidine involve administering the compound to animal models of hypertension to assess its blood pressure-lowering effects. Its effects on sympathetic nerve activity and neurotransmitter release are also studied. Its efficacy in relieving pain has been explored in animal models of complex regional pain syndrome. |
| ADME/Pharmacokinetics |
Guanethidine sulfate has a molecular weight of 296.39 g/mol and a molecular formula of C10H24N4O4S. Its IUPAC name is 2-[2-(azocan-1-yl)ethyl]guanidine; sulfuric acid. It is soluble in water at ≥12.75 mg/mL. It is typically stored as a powder.
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| Toxicity/Toxicokinetics |
Guanethidine sulfate is a prescription drug with a well-established safety profile. Common adverse effects include orthostatic hypotension, dizziness, and fatigue. It can cause diarrhea and sexual dysfunction. It is contraindicated in patients with pheochromocytoma and should be used with caution in patients with coronary artery disease.
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| References |
[1]. Mitchell JR, et al. Antagonism of the antihypertensive action of guanethidine sulfate by desipramine hydrochloride. JAMA. 1967 Dec 4;202(10):973-6.
[2]. Nielsen GD. Guanethidine induced sympathectomy in the adult rat. I. Functional effects following subacute administration. Acta Pharmacol Toxicol (Copenh). 1977 Sep;41(3):203-8. [3]. Fabiani ME, et al. 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. |
| Additional Infomation |
An antihypertensive drug that works by selectively inhibiting postganglionic adrenergic neurotransmission. Its primary mechanism of action is believed to be the prevention of norepinephrine release from nerve endings, leading to depletion of norepinephrine in peripheral sympathetic nerve endings and tissues.
See also: Guanethidine (active moiety); Guanethidine monosulfate; Hydrochlorothiazide (component). Guanethidine sulfate is an antihypertensive agent that acts by inhibiting the release of norepinephrine from sympathetic nerve endings. It is used to treat high blood pressure, particularly in patients who do not respond to other medications. It is also known as guanethidine monosulfate and is available as a pharmaceutical product and from various chemical suppliers for research purposes. |
| Molecular Formula |
C10H22N4.H2SO4
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|---|---|
| Molecular Weight |
296.39
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| Exact Mass |
296.151
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| CAS # |
645-43-2
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| Related CAS # |
Guanethidine;55-65-2
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| PubChem CID |
86471
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| Appearance |
White to off-white solid powder
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| Boiling Point |
345.6ºC at 760 mmHg
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| Flash Point |
162.8ºC
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| LogP |
2.292
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
248
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YUFWAVFNITUSHI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H22N4.H2O4S/c11-10(12)13-6-9-14-7-4-2-1-3-5-8-14;1-5(2,3)4/h1-9H2,(H4,11,12,13);(H2,1,2,3,4)
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| Chemical Name |
2-[2-(azocan-1-yl)ethyl]guanidine;sulfuric acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~337.39 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (337.39 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | 1.6870 mL | 3.3739 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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