1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. Guanoxabenz hydrochloride

Guanoxabenz hydrochloride (Synonyms: Hydroxyguanabenz hydrochloride)

Cat. No.: HY-U00123A Purity: 99.72%
Handling Instructions

Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor.

For research use only. We do not sell to patients.

Guanoxabenz hydrochloride Chemical Structure

Guanoxabenz hydrochloride Chemical Structure

CAS No. : 23256-40-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 440 In-stock
Estimated Time of Arrival: December 31
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3400 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor[1][2][3].

In Vitro

The formation of high-affinity Guanoxabenz binding seems to be inhibited by a series of N-hydroxyguanidine analogs to Guanoxabenz, as well as by a series of metabolic inhibitors that included allopurinol, 1-chloro-2,4-dinitrobenzene, 5,59-dithiobis-(2-nitrobenzoic acid), cibacron blue, phenyl-p-benzoquinone, didox, and trimidox. The formation of Guanoxabenz high-affinity binding is also inhibited in a time- and concentration-dependent fashion by preincubating the membranes with the LW03 N-hydroxyguanidine analogue of Guanoxabenz[1]. The spleen cytosolic fraction mediates the reduction of Guanoxabenz to guanabenz, the latter having an almost 100-fold higher affinity for rat alpha2A-adrenoceptors than Guanoxabenz itself[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Guanoxabenz and guanabenz are both known as centrally active antihypertensive drugs. High affinity Guanoxabenz binding is induced in rat brain membranes after addition of NADH or NADPH cofactors. The rat cerebral cortex contains an enzymatic activity that may activate Guanoxabenz leading to formation of a metabolite showing high affinity for alpha 2-adrenoceptors[3].
Guanoxabenz (0.1-3 mg/kg, i.p.) causes a dose-related reduction in locomotor activity; a dose of 1 mg/kg is selected since this induces a pronounced and sustained behavioural hypoactivity[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats[4].
Dosage: 0.5 mg/kg (RX 781094 or saline vehicle was injected intravenously (tail vein) at the time of peak effect of the agonist (20min for clonidine and 30 min for Guanoxabenz).
Administration: IP.
Result: RX 781094 (0.1-1.0 mg/kg, i.v.) produces a rapid (< 5 set) and complete antagonism of the EEG and behavioural effects induced by clonidine and Guanoxabenz.
Molecular Weight

283.54

Formula

C₈H₉Cl₃N₄O

CAS No.
SMILES

ClC1=C(/C=N/NC(NO)=N)C(Cl)=CC=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (293.89 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5268 mL 17.6342 mL 35.2684 mL
5 mM 0.7054 mL 3.5268 mL 7.0537 mL
10 mM 0.3527 mL 1.7634 mL 3.5268 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.34 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.34 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.34 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GuanoxabenzHydroxyguanabenzAdrenergic ReceptorBeta ReceptorAntihypertensiveCNSEEGa2AInhibitorinhibitorinhibit

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Guanoxabenz hydrochloride
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