Description
Description | Guanabenz Acetate (Wytensin) is a specific agonist of adrenergic receptor. The pEC50 for α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor is 8.25, 7.01 and ~5, respectively. |
Targets&IC50 | α2C-adrenoceptor:<5(pEC50), α2B-adrenoceptor:7.01(pEC50), α2A-adrenoceptor:8.25(pEC50) |
In vitro | Guanabenz inhibits the response of vascular contractions in various processes and initiates normal sympathetic nerve discharge, while also antagonizing the stimulation of the sympathetic nervous system. Administering 0.5 mg/kg of Guanabenz intravenously in anesthetized hypertensive rats and dogs leads to a reduction in blood pressure and heart rate. Moreover, an intravenous injection of 0.1 mg/kg Guanabenz in anesthetized dogs initially causes an increase in blood pressure due to the action of the sympathetic nervous system, followed by a decrease in cardiac output, contractility, and heart rate. |
In vivo | In mammalian MovS6 cells, 10 μM of Guanabenz facilitates the complete clearance of PrPSc. Additionally, in HEK293 cells transfected with rat inducible nitric oxide synthase (nNOS), 30 μM Guanabenz induces a time-dependent reduction in nNOS activity, with a Ki value of 1 μM. In HEK 293 cells, treatment with 50 μM Guanabenz for 3 hours results in approximately a 75% decrease in the accumulation of nitrites and nitrates within the cells. Furthermore, treatment with 100 μM Guanabenz for 24 hours leads to about a 35% reduction in the quantity of inducible nitric oxide synthase protein detected by immunological methods. |
Synonyms | Wy8678 acetate, BR-750, Wytensin |
Molecular Weight |
291.13 |
Formula | C8H8Cl2N4·C2H4O2 |
CAS No. | 23256-50-0 |
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 21.8 mg/mL (75 mM)