Disease relevance of BRN 1383873

• Much emphasis is given to the metabolism of carbofuran, and the impact of carbofuran and its two major metabolites (3-hydroxycarbofuran and 3-ketocarbofuran) on overall toxicity [1].

High impact information on BRN 1383873

• Chlorpyrifos, an irreversible non-competitive inhibitor of CYP3A4, inhibits the formation of 3-hydroxycarbofuran in HLM (IC50: 39 microM) [2].
• The affinity of carbofuran for CYP enzymes involved in the oxidation to 3-hydroxycarbofuran is significantly less in HLM (Km=1.950 mM) than in RLM (Km=0.210 mM), or MLM (Km=0.550 mM) [2].
• Carbofuran is metabolized by cytochrome P450 (CYP) leading to the production of one major ring oxidation metabolite, 3-hydroxycarbofuran, and two minor metabolites [2].
• Results indicated that rapid RBC AchE recovery closely paralleled carbofuran metabolism and the primary in vivo disposition of 3-hydroxycarbofuran was metabolic conjugation [3].
• 3-Hydroxycarbofuran, a significant oxidative metabolite of carbofuran with anticholinesterase activity, was rapidly formed and subject to enterohepatic circulation (plasma t1/2 = 64 +/- 5 min) [3].

Associations of BRN 1383873 with other chemical compounds

• Determination of carbofuran and 3-hydroxycarbofuran residues in plant tissue by nitrogen selective gas chromatography [4].
• This is substantiated by the fact that ketoconazole, a specific inhibitor of CYP3A4, is an excellent inhibitor of 3-hydroxycarbofuran formation in HLM (IC50: 0.31 microM) [2].

Analytical, diagnostic and therapeutic context of BRN 1383873

• Direct analysis of carbofuran and 3-hydroxycarbofuran in rape plants by reverse-phase high-pressure liquid chromatography [5].

References