Rimantadine (hydrochloride)

具有抗病毒活性的金刚烷胺衍生物；抑制在X.laevis卵母细胞中表达的重组甲型流感M2蛋白（IC50=10.8µM）；抑制在HEK293细胞中表达的重组HCVp7蛋白（对于HCV基因型1a、2a、3a和4a的IC50分别为0.7、24、1.6和3.0nM）；在MDCK细胞中抑制由甲型流感病毒株A/PR/8/34(H1N1)和A/HK/7/87(H3N2)诱导的细胞毒性，但不抑制乙型流感病毒株B/HK/72诱导的细胞毒性（EC50分别为18、0.62和>500µM）；感染A型流感病毒株A2/Jap/305后两小时给药，剂量为24mg/kg，可使感染该病毒株的小鼠存活率从20%提高至90%；体外对血液中的布氏锥虫具有杀锥虫活性(IC50=1.26µg/ml)。A derivative of amantadine with antiviral activity; inhibits recombinant influenza A M2 protein expressed in X. laevis oocytes (IC50 = 10.8 µM); inhibits recombinant HCV p7 protein expressed in HEK293 cells (IC50s = 0.7, 24, 1.6, and 3.0 nM for HCV genotypes 1a, 2a, 3a, and 4a, respectively); inhibits cytotoxicity induced by the influenza A strains A/PR/8/34 (H1N1) and A/HK/7/87 (H3N2), but not the influenza B strain B/HK/72, in MDCK cells (EC50s = 18, 0.62, and >500 µM, respectively); increases the survival rate of mice infected with the influenza A strain infected with the influenza A strain A2/Jap/305 from 20 to 90% at 24 mg/kg when administered two hours post-infection; has trypanocidal activity against bloodstream forms of T. brucei in vitro (IC50 = 1.26 µg/ml).