Guanabenz 是一种 α-2 肾上腺素受体激动剂，具有口服活性。Guanabenz 具有抗高血压和抗寄生虫活性。Guanabenz 干扰内质网应激信号传导，对心肌细胞具有保护作用。Guanabenz 也被用于高血压的研究。
| 生物活性 | Guanabenz is an orally activeα-2-adrenoceptoragonist. 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[1][2][3]. |
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体外研究
(In Vitro) | Guanabenz (0.5-50 μM, 24 h) is treated with increasing concentrations for 24 hours not affect cell viability[1].
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[1].
Guanabenz (0.5-50 μM, 24 h) alone not induces ER stress in neonatal rat cardiomyocytes[1].
Cell Viability Assay[1] | Cell Line: | Neonatal rat cardiac myocytes (NRCM) | | Concentration: | 0.5–50 μM | | Incubation Time: | 24 h | | Result: | Did not affect cell survival. |
RT-PCR[1] | Cell Line: | Neonatal rat cardiac myocytes (NRCM) | | Concentration: | 0.5–50 μM | | Incubation Time: | 24 h | | Result: | Did not affect levels of UPR targets. |
Western Blot Analysis[1] | Cell 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. |
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体内研究
(In Vivo) | Guanabenz (5 mg/kg/day; i.p.; for 3 weeks) can reproducibly reduce brain cyst burden[2].
Guanabenz (5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks) reverses Toxoplasma-induced hyperactivity in latently infected mice[2].
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[3].
| Animal Model: | BALB/cJ mice[2] | | 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[2] | | 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[3] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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