Guanabenz hydrochloride

Guanabenz hydrochloride is an orally active α-2-adrenoceptor agonist. Guanabenz hydrochloride has antihypertensive effect and antiparasitic activity. Guanabenz hydrochloride interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz hydrochloride also is used for the research of high blood pressure

In Vitro

Guanabenz hydrochloride (0.5-50 μM, 24 h) is treated with increasing concentrations for 24 hours not affect cell viability. Guanabenz hydrochloride (0.5-50 μM, 24 h) alone not affects the UPR targets, neither on mRNA or protein level nor the phosphorylation status of eIF2a. Guanabenz also not induces GADD34 or the constitutively active form CReP. Guanabenz hydrochloride (0.5-50 μM, 24 h) alone not induces ER stress in neonatal rat cardiomyocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Neonatal rat cardiac myocytes (NRCM) Concentration: 0.5-50 μM Incubation Time: 24 h Result: Did not affect cell survival. Western Blot AnalysisCell Line: Neonatal rat cardiac myocytes (NRCM) Concentration: 0.5-50 μM Incubation Time: 24 h Result: Increased the levels of low panel concentration-dependent UPR targets proteins. RT-PCRCell Line: Neonatal rat cardiac myocytes (NRCM) Concentration: 0.5-50 μM Incubation Time: 24 h Result: Did not affect levels of UPR targets.

In Vivo

Guanabenz hydrochloride (5 mg/kg/day; i.p.; for 3 weeks) can reproducibly reduce brain cyst burden. Guanabenz hydrochloride (5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks) reverses Toxoplasma-induced hyperactivity in latently infected mice. Guanabenz hydrochloride (100 and 320 μg/kg and 1 mg/kg, i.v., over a period of 5 min at intervals of 40 min) reduces sympathetic outflow, heart rate and blood pressure in debuffered cats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/cJ miceDosage: 5 mg/kg Administration: 5 mg/kg/day; i.p. ; for 3 weeks Result: Reduced the latent brain cysts in both male and female BALB/cJ mice. Animal Model: BALB/cJ miceDosage: 5 mg/kg; 10 mg/kg Administration: 5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks Result: Reversed parasite-induced hyperactivity to near-baseline levels. Animal Model: CatsDosage: 100 and 320 μg/kg and 1 mg/kg Administration: 100 and 320 μg/kg and 1 mg/kg, i.v., over a period of 5 min at intervals of 40 min Result: Declined markedly blood pressure and nerve activity.

Form:Solid

IC50& Target:Toxoplasma