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编 号:F067583
分子式:C19H22FN3O3
分子量:359.39
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生物活性:
Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile.

体内研究:
Grepafloxacin (OPC-17116; 200 mg/kg; p.o.; Balb/c mice) displays good safety profile in terms of phototoxicity.Grepafloxacin (25-200 mg/kg; p.o.; 5 days/week for 4 weeks; female C57BL6/J-Lyst bg-J/ mice/beige mice) has modest activities in both intranasal (IN) infection and intravenous (IV) Mycobacterium avium infection models.Animal Model:Female Balb/c mice (5-6 weeks)
Dosage:200 mg/kg
Administration:Oral administration; once
Result:Had mild and short-lived erythema and no changed auricular thickness.
Animal Model:Female C57BL6/J-Lyst bg-J/ mice/beige mice with mycobacterium avium infection
Dosage:25, 50, 100, and 200 mg/kg
Administration:Oral administration; 5 days/week for 4 weeks
Result:Had bactericidal activity and limited the growth of the bacteria.

体外研究:
Grepafloxacin (OPC-17116; 0-1 mg/L; 14-21 d) has antibiotic activity with a MIC value of ≤ 0.006 mg/L for E. coli strain.Grepafloxacin (0-1 mg/L; 3 h) has antimicrobial activity against mycobacteria in macrophages with a MIC value of 0.5 mg/L for M. avium.Grepafloxacin exhibits potent in vitro antibacterial activity against Gram-positive bacteria such as Streptococcus pneumoniae and high in vivo efficacy on the experimental systemic infections caused by the Gram-positive and -negative bacteria tested.
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