Home Neuronal Signaling Adrenergic Receptor agonist Guanabenz Acetate For research use only.

Guanabenz Acetate

Synonyms: WY-8678 Acetate

Guanabenz Acetate (WY-8678) is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively.

Guanabenz Acetate Chemical Structure

Guanabenz Acetate Chemical Structure

CAS No. 23256-50-0

Purity & Quality Control

Guanabenz Acetate Related Products

Signaling Pathway

Adrenergic Receptor Signaling Pathways

Adrenergic Receptor Signaling Pathway

Biological Activity

Description Guanabenz Acetate (WY-8678) is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively.
Targets
α2a-adrenergic receptor [1] α2b-adrenergic receptor [1] α2c-adrenergic receptor [1]
8.25(pEC50) 7.01(pEC50) <5(pEC50)
In vitro
In vitro Guanabenz at a concentration of 30 μM causes a time-dependent loss of nNOS-activity, which is present in cytosol prepared from rat nNOS transfected HEK 293 cells, with a Ki of 1 μM. Guanabenz can induce a concentration-dependent loss of nNOS activity. Within the first 3 h of treatment, 50 μM Guanabenz decreases the accumulation of nitrite and nitrate by approximately 75% in cells. Treatment of HEK 293 cells for 24 h with Guanabenz (100 μM) causes an approximately 35% decrease in the amount of immunodetectable nNOS protein. Guanabenz enhances proteolysis of the protein with the half-life decreasing by one-half from 20 to 10 h. [2] Guanabenz is active against [ PSI+] prion in the yeast-based assay independent of its agonist activity on α2-adrenergic receptors. Guanabenz (10 μM) promote complete PrPSc clearance in mammalian MovS6 cell-based assay. [3]
In Vivo
In vivo Guanabenz injected i.v. in doses of 0.1 mg/kg causes an initial increase in blood pressure followed by a prolonged fall and a decrease in cardiac output, contractile force and heart rate in anesthetized dogs, which requires the presence of sympathetic tone. Guanabenz inhibits pressor responses to various procedures which initiate general sympathetic discharge. Guanabenz also antagonizes responses to sympathetic nerve stimulation. [4] Guanabenz injected at doses of 0.5 mg/kg and above lowers blood pressure and heart rate in unanesthetized hypertensive rats and dogs. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02423083 Terminated
Multiple Sclerosis Relapsing-Remitting|Multiple Sclerosis
National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC)
 April 21 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 291.13 Formula

C8H8Cl2N4.C2H4O2
CAS No. 23256-50-0 SDF Download Guanabenz Acetate SDF
Smiles CC(=O)O.C1=CC(=C(C(=C1)Cl)C=NN=C(N)N)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 15 mg/mL ( (51.52 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
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