Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM. Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270 μM)[3]. At all doses (100, 200, 350, 500 μM) tested, nevirapine significantly inhibited cell proliferation after 48 h treatment. At high dose (500 μM), nevirapine significantly increased the percentage of apoptotic cells compared with control (P<0.01). At lower doses (200 μM and 350 μM), nevirapine did not induce cell apoptosis, but up-regulated NIS and THSR mRNA expression in a dose-dependent manner[4]. Nevirapine also has an important role in preventing mother-to-child transmission of HIV. Nevirapine interacts with cytochrome P450 enzymes both as a substrate and as an inducer[5]. Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) showed significant (P < 0.05) reduction in ulcer severity score and ulcer index as compared to the control in the models,.with corresponding increase in percentage inhibition[6]. Nevirapine inhibits replication of multiple HIV-1 strains and clinical isolates in cultured human T cells, but has no activity against other retroviral RTs (including HIV-2 RT) or endogenous human DNA polymerases[7].
Nevirapine 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
293T cells
Function assay
Inhibition of wild type HIV1 reverse transcriptase in 293T cells, IC50=0.06 μM
16527484
CEM-SS cells
Function assay
Antiviral activity against HIV1 RF in CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay, EC50=1.5 nM
18222088
HeLa cells
Function assay
Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay, IC50=0.053 μM
18665583
human C1866 cells
Cytotoxicity assay
72 h
Cytotoxicity against human C1866 cells after 72 hrs by MTT assay, EC50=0.04943 μM
Inhibition of wild type HIV1 reverse transcriptase in 293T cells, IC50=0.06 μM
16527484
CEM-SS cells
Function assay
Antiviral activity against HIV1 RF in CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay, EC50=1.5 nM
18222088
HeLa cells
Function assay
Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay, IC50=0.053 μM
18665583
human C1866 cells
Cytotoxicity assay
72 h
Cytotoxicity against human C1866 cells after 72 hrs by MTT assay, EC50=0.04943 μM
21194939
human Jurkat E6-1 cells
Function assay
2 days
Antiviral activity against HIV1 Env-pseudovirus infected in human Jurkat E6-1 cells after 2 days by luciferase assay, IC50=0.04 μM
21414776
human MT2 cells
Function assay
4 days
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA, EC50=0.053 μM
20527972
human MT4 cells
Function assay
Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity, EC50=0.00488 μM
19933797
MDCK2 cells
10 μM
Function assay
Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay
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