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编 号:F371952
分子式:C8H8Cl2N4
分子量:231.08
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生物活性:
Guanabenz is an orally active α-2-adrenoceptor agonist. Guanabenz has antihypertensive effect and antiparasitic activity. Guanabenz interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz also is used for the research of high blood pressure.

体内研究:
Guanabenz (5 mg/kg/day; i.p.; for 3 weeks) can reproducibly reduce brain cyst burden.Guanabenz (5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks) reverses Toxoplasma-induced hyperactivity in latently infected mice.Guanabenz (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.Animal Model:BALB/cJ mice
Dosage: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 mice
Dosage: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:Cats
Dosage: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.

体外研究:
Guanabenz (0.5-50 μM, 24 h) is treated with increasing concentrations for 24 hours not affect cell viability.Guanabenz (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 (0.5-50 μM, 24 h) alone not induces ER stress in neonatal rat cardiomyocytes.
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