生物活性

• 描述Deflazacort (DFC) is a glucocorticoid used as an anti-inflammatory and immunosuppressant. It is a methyloxazoline derivative of prednisolone and has been proposed to have major advantages over other corticosteroids. It represents an inactive prodrug which is rapidly converted in the body to its active alcohol metabolite, 21-desacetyldeflazacort. In long evans rats, DFC decreases thymus weight and daily weight gain and decreases the mRNA expression of IFG-I and GHR in liver. In ADX rats receiving vehicle or different steroids, DFC is as effective as DEX in the hippocampus, pituitary, liver and thymus, but less effective in the cerebral cortex. After DFC treatment in the adrenal-intact rats, relative tissue weight is significantly increased for the testis and kidney, reflecting a partial resistance by these organs to the catabolic effects of the synthetic glucocorticoids. In sheep, DFC is more potent than prednisolone in its effect on plasma OC levels while exerting a similar hyperglycemic effect, it has a significant effect on OC at and above 0.013 mg/hour but is hyperglycemic only at the much higher dose of 0.25 mg/hour. The effect of a treatment with DFC and L-arginine not only spared dystrophic muscle from exercise-induced damage (and the ensuring regeneration from that muscle injury) and decreases the “background” severity of dystrophy in nonexercised mdx mice but additionally results in long-term potentiation of a persistent gain in function accorded by DFC alone.

• 动物研究
  剂量	Rat: 0.05 mg/kg - 0.5 mg/kg(male), 0.1 mg/kg - 1 mg/kg(female)[3] (p.o.)
  给药途径	p.o.
  动物药代数据	Animal Rats[3] Dose 0.5 mg/kg Administration p.o. Cmax 255 ng/ml AUC0→24h 978 ng·h/ml