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• W2082052010 abstract "Buprenorphine is a long acting analgesic of the opiate family. Recently, it has been proposed for the opioid dependency treatment at a large scale. The drug is extensively metabolized by the hepatic cytochrome P450 in man, yielding a N-dealkylated metabolite, norbuprenorphine. The specific forms of P450 involved in this oxidative N-demethylation were examined in a panel of 18 human liver microsomal preparations previously characterized with respect to their P450 contents. Buprenorphine was N-dealkylated with an apparent Km of 89 ± 45 μM (n = 3). The metabolic rates were 3.46 ± 0.43 nmol/(min x mg of protein). This metabolic pathway was strongly correlated with 6 catalytic activities specific to P450 3A4 and with the immunodetectable P450 3A content of liver microsomal samples (r = 0.87). Buprenorphine metabolism was 62–71% inhibited by three mechanism-based inhibitors (TAO, erythralosamine, gestodene), by nifedipine as competitive inhibitor (Ki = 129 μM) and by ketoconazole 0.6 μM (25% residual activity), all these inhibitors specific to P450 3A. Among 10 heterologously expressed P450s tested, only P450 3A4 was able to dealkylate buprenorphine with a turnover number of 9.6 min−1. Morever, this catalytic activity was inhibited up to 80% (vs control) by anti-rat P450 3A antibody. Taken together, all these data demonstrate that P450 3A4 is the major enzyme involved in hepatic buprenorphine N-dealkylation." @default.
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• W2082052010 date "1997-04-01" @default.
• W2082052010 modified "2023-10-10" @default.
• W2082052010 title "Involvement of cytochrome P450 3A4 in N-dealkylation of buprenorphine in human liver microsomes" @default.
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• W2082052010 doi "https://doi.org/10.1016/s0024-3205(97)00160-4" @default.
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