Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Guanoxabenz (Hydroxyguanabenz) hydrochloride is an agonist of α2 adrenergic receptor. It has a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor[1][2][3].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,400.00 | |
50 mg | 6-8 weeks | $ 1,820.00 | |
1 mL * 10 mM (in DMSO) | 6-8 weeks | $ 363.00 |
Description | Guanoxabenz (Hydroxyguanabenz) hydrochloride is an agonist of α2 adrenergic receptor. It has a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor[1][2][3]. |
In vitro | The inhibition of high-affinity Guanoxabenz binding is caused by both a series of N-hydroxyguanidine analogs (to Guanoxabenz) and various metabolic inhibitors, which include allopurinol, 1-chloro-2,4-dinitrobenzene, 5,59-dithiobis-(2-nitrobenzoic acid), cibacron blue, phenyl-p-benzoquinone, didox, and trimidox. Additionally, the LW03 N-hydroxyguanidine analogue of Guanoxabenz exhibits a time- and concentration-dependent inhibition of this binding when membranes are preincubated with it. Furthermore, the conversion of Guanoxabenz to guanabenz by the spleen cytosolic fraction significantly increases affinity, as guanabenz binds nearly 100 times more effectively to rat alpha2A-adrenoceptors than Guanoxabenz. |
In vivo | Guanoxabenz and guanabenz are centrally acting antihypertensive agents. They show increased binding affinity in rat brain membranes when NADH or NADPH cofactors are added, suggesting the presence of an enzyme in the rat cerebral cortex that activates Guanoxabenz, creating a metabolite with high affinity for alpha 2-adrenoceptors. Moreover, Guanoxabenz administration (0.1-3 mg/kg, i.p.) results in a dose-dependent decrease in rat locomotor activity, with 1 mg/kg being optimal for inducing significant sustained behavioral hypoactivity. In a specified animal model involving rats, a 0.5 mg/kg dose (using RX 781094 or saline as a vehicle) was injected intravenously (tail vein) to counteract the peak effects of agonists at predefined times. Notably, RX 781094 (0.1-1.0 mg/kg, i.v.) counters the EEG and behavioral effects of clonidine and Guanoxabenz rapidly and effectively within less than 5 seconds, signifying its role as a potent antagonist. |
Molecular Weight | 283.54 |
Formula | C8H9Cl3N4O |
CAS No. | 23256-40-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Guanoxabenz hydrochloride 23256-40-8 inhibitor inhibit