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编 号:F229554
分子式:C18H33ClN2O5S
分子量:424.98
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5mg
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10mg
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25mg
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生物活性:
Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria.

体内研究:
Clindamycin (50-300 mg/kg; 静脉注射, 口服) 剂量不会影响大鼠的药代动力学参数。Clindamycin (160-600 mg/kg; 静脉注射) 在内毒素休克小鼠模型中以剂量依赖的方式提高生存率.Clindamycin (17-50 mg/kg, 静脉注射) 对大鼠肌肉组织有很好的渗透作用,可用于抑制引起牙源性感染的主要细菌。1.19药代动力学分析RouteDose (mg/kg)t1/2 (h)Cmax (mg/mL)Tmax (h)aAUC0-inf (h.mg/L)?T
i.v.51(Plasma)2.51 (2.37–2.83)35.21 (25.04–42.65)0.08 ± 0.0044.78 (28.82–65.65)/
i.v.51(Tissue)2.82 (2.57–3.05)14.20 (10.63–14.89)0.25 ± 0.0016.54 (13.83–18.35)1.10
i.v.17(Tissue)3.25 (3.13–3.44)4.82 (3.35–6.660.25 ± 0.00//
Animal Model:Endotoxic shock mouse model
Dosage:160-600 mg/kg
Administration:Intravenous injection (i.v.)
Result:Decreased survival rates to 92 and 36% treated with 520- and 600-mg/kg doses.Lowered the peak concentrations of tumor necrosis factor alpha (TNF-α) and interleukin-1β (IL-1β) in serum.Increased the the peak concentrations of IL-6 in the sera.

体外研究:
Clindamycin (25 μg/mL, 1-18 h) 抑制 E. coli O55:B5 中头孢他啶 (HY-B0593) 诱导的内毒素的释放.Clindamycin (50-100 μg/mL, 0-12 min) 增强金黄色葡萄球菌 (Staphylococcus aureus) 中抗体和补体依赖性吞噬作用。Clindamycin (0-500 μg/mL, 24-72 h) 抑制成骨细胞培养模型中的细胞增殖,在 10 μg/mL 浓度下刺激成骨细胞的细胞代谢。
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