1-Aminobenzotriazole (ABT) (Synonyms: ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) |
| カタログ番号GC14781 |
ABT (1-アミノベンゾトリアゾール) は、シトクロム P450 (P450) の非特異的かつ不可逆的な阻害剤です。
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Cas No.: 1614-12-6
Sample solution is provided at 25 µL, 10mM.
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1-Aminobenzotriazole (ABT) is an orally active nonspecific and irreversible inhibitor of cytochrome P450 (CYP)[1]. 1-Aminobenzotriazole is a substrate and inhibitor of N-acetyltransferase (NAT)[2].
In vitro, 1-Aminobenzotriazole (1mM) treatment of sandwich cultured human hepatocytes (SCHH) for 0-60min significantly inhibited the intracellular activities of CYP3A, CYP2C9, CYP2D6 and CYP1A2. The residual activity of CYP3A was 3% of the control, while the residual activities of CYP2C9, CYP2D6 and CYP1A2 remained between 5% and 35%[3].
In vivo, oral administration of 1-Aminobenzotriazole (0, 50, 100, 200, 300mg/kg) to SD rats significantly inhibited the hepatic metabolism of MDZ, but could not completely inhibit the formation of 1'-OH MDZ[4]. Oral administration of 1-Aminobenzotriazole (50mg/kg) to male mice for 3 days suppressed the dominant lethal effect of acrylamide-induced spermatocytes[5]. Treatment of rats with 1-Aminobenzotriazole (78mg/kg) increased organ weights and mortality, and increased sensitivity to inflammation-induced multiple organ failure (MOF)[6].
References:
[1] de Montellano P R O. 1-Aminobenzotriazole: a mechanism-based cytochrome P450 inhibitor and probe of cytochrome P450 biology[J]. Medicinal chemistry, 2018, 8(3).
[2] Sun Q, Harper T W, Dierks E A, et al. 1-Aminobenzotriazole, a known cytochrome P450 inhibitor, is a substrate and inhibitor of N-acetyltransferase[J]. Drug metabolism and disposition, 2011, 39(9): 1674-1679.
[3] Kimoto E, Walsky R, Zhang H, et al. Differential modulation of cytochrome P450 activity and the effect of 1-aminobenzotriazole on hepatic transport in sandwich-cultured human hepatocytes[J]. Drug Metabolism and Disposition, 2012, 40(2): 407-411.
[4] Parrish K E, Mao J, Chen J, et al. In vitro and in vivo characterization of CYP inhibition by 1‐aminobenzotriazole in rats[J]. Biopharmaceutics & drug disposition, 2016, 37(4): 200-211.
[5] Adler I D, Baumgartner A, Gonda H, et al. 1-Aminobenzotriazole inhibits acrylamide-induced dominant lethal effects in spermatids of male mice[J]. Mutagenesis, 2000, 15(2): 133-136.
[6] Carcillo J, Kost C, Korzekwa K, et al. 1-aminobenzotriazole (ABT), the cytochrome P450 suicide inhibitor, sensitizes rats to zymosan induced-multiple organ failure184[J]. Pediatric Research, 1998, 43(4): 34-34.
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