| Name | CYP1A2 |
|---|---|
| Synonyms | CP12; CYP1A2; CYPIA 2; CYPIA2; Cytochrome P450 1A2; Dioxin inducible P3 450; P(3)450; P3 450… |
| Name | thiabendazole |
|---|---|
| CAS |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 16261361 | Bapiro TE, Sayi J, Hasler JA, Jande M, Rimoy G, Masselle A, Masimirembwa CM: Artemisinin and thiabendazole are potent inhibitors of cytochrome P450 1A2 (CYP1A2) activity in humans. Eur J Clin Pharmacol. 2005 Nov;61(10):755-61. Epub 2005 Oct 29. |
226(2,4,4,6) | Details |
| 19299526 | Thelingwani RS, Zvada SP, Dolgos H, Ungell AL, Masimirembwa CM: In vitro and in silico identification and characterization of thiabendazole as a mechanism-based inhibitor of CYP1A2 and simulation of possible pharmacokinetic drug-drug interactions. Drug Metab Dispos. 2009 Jun;37(6):1286-94. Epub 2009 Mar 19. |
163(2,2,2,3) | Details |
| 11124226 | Bapiro TE, Egnell AC, Hasler JA, Masimirembwa CM: Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5. In addition, our results suggest CYP1A2 inhibition as the mechanism behind the observed thiabendazole/ and primaquine/antipyrine interactions in vivo. |
112(1,2,2,2) | Details |
| 19754423 | Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. In particular, several therapeutic drugs including antofloxacin, carbamazepine, dihydralazine, furafylline, isoniazid, rofecoxib, clorgyline, thiabendazole, and zileuton are mechanism-based inhibitors of CYP1A2. |
96(1,1,1,16) | Details |
| 10936227 | Coulet M, Eeckhoutte C, Larrieu G, Sutra JF, Alvinerie M, Mace K, Pfeifer A, Zucco F, Stammati AL, De Angelis I, Vignoli AL, Galtier P: Evidence for cytochrome P4501A2-mediated protein covalent binding of thiabendazole and for its passive intestinal transport: use of human and rabbit derived cells. Chem Biol Interact. 2000 Jul 3;127(2):109-24. Thiabendazole (TBZ), an anthelmintic and fungicide benzimidazole, was recently demonstrated to be extensively metabolized by cytochrome P450 (CYP) 1A2 in man and rabbit, yielding 5-hydroxythiabendazole (5OH-TBZ), the major metabolite furtherly conjugated, and two minor unidentified metabolites (M1 and M2). |
84(1,1,1,4) | Details |
| 8819304 | Rey-Grobellet X, Eeckhoutte C, Sutra JF, Alvinerie M, Galtier P: Major involvement of rabbit liver cytochrome P4501A in thiabendazole 5-hydroxylation. Xenobiotica. 1996 Jul;26(7):765-78. In the CYP1A subfamily, CYP1A2 appears to be responsible for basal 5-hydroxylation and further unidentified metabolism of thiabendazole in control livers. |
81(1,1,1,1) | Details |
| 9565779 | Coulet M, Dacasto M, Eeckhoutte C, Larrieu G, Sutra JF, Alvinerie M, Mace K, Pfeifer AM, Galtier P: Identification of human and rabbit cytochromes P450 1A2 as major isoforms involved in thiabendazole 5-hydroxylation. Fundam Clin Pharmacol. 1998;12(2):225-35. Thus, CYP1A2 is a major isoenzyme involved in thiabendazole 5-hydroxylation. |
32(0,1,1,2) | Details |
| 18570159 | Price RJ, Scott MP, Giddings AM, Walters DG, Stierum RH, Meredith C, Lake BG: Effect of butylated hydroxytoluene, propyl and thiabendazole on cytochrome P450 forms in cultured human hepatocytes. Xenobiotica. 2008 Jun;38(6):574-86. Treatment of human hepatocytes for 72 h with 2-200 microM TB produced concentration-dependent increases in CYP1A2, CYP2B6 and CYP3A4 mRNA levels, whereas treatment with BHT increased CYP2B6 and CYP3A4 mRNA levels. |
2(0,0,0,2) | Details |
| 18539377 | Stierum R, Conesa A, Heijne W, Ommen B, Junker K, Scott MP, Price RJ, Meredith C, Lake BG, Groten J: Transcriptome analysis provides new insights into liver changes induced in the rat upon dietary administration of the food additives butylated hydroxytoluene, propyl and thiabendazole. Food Chem Toxicol. 2008 Aug;46(8):2616-28. Epub 2008 Apr 25. TB changed the expression of 12 genes, including CYP1A2. |
2(0,0,0,2) | Details |
| 8607843 | Rey-Grobellet X, Ferre N, Eeckhoutte C, Larrieu G, Pineau T, Galtier P: Structural requirements for the induction of cytochromes P450 by benzimidazole anthelmintic derivatives in cultured rabbit hepatocytes. Biochem Biophys Res Commun. 1996 Mar 27;220(3):789-94. The effect of -containing benzimidazoles (thiabendazole, 5--thiabendazole, cambendazole) and -free derivatives (benzimidazole, carbendazim and 5-hydroxycarbendazim) on cytochrome P450 enzymes was investigated in primary cultures of rabbit hepatocytes considered 72 h after plating. Experiments using actinomycin D strongly suggest that these compounds have a transcriptional control on both CYP1A1 and CYP1A2 genes in primary hepatocytes. |
1(0,0,0,1) | Details |
| 16714371 | Diani-Moore S, Papachristou F, Labitzke E, Rifkind AB: Induction of CYP1A and cyp2-mediated epoxygenation and suppression of by derivatives including the aromatase inhibitor vorozole. Drug Metab Dispos. 2006 Aug;34(8):1376-85. Epub 2006 May 19. We report here that derivative drugs: the anthelminthics, albendazole and thiabendazole; the proton pump inhibitor, the thromboxane synthase inhibitor, benzylimidazole; and the aromatase (CYP19) inhibitor vorozole (R76713, racemate; and R83842, (+) enantiomer) increased hepatic microsomal EET formation in a chick embryo model. Albendazole increased EETs by transcriptional induction of CYP1A5 and the others by combined induction of CYP1A5 and CYP2H, the avian orthologs of mammalian CYP1A2 and CYP2B, respectively. |
1(0,0,0,1) | Details |
| 15110098 | Price RJ, Scott MP, Walters DG, Stierum RH, Groten JP, Meredith C, Lake BG: Effect of thiabendazole on some rat hepatic xenobiotic metabolising enzymes. Food Chem Toxicol. 2004 Jun;42(6):899-908. The administration of high doses of TB resulted in the induction of 7-ethoxyresorufin O-deethylase and 7-pentoxyresorufin O-depentylase activities, CYP1A1, CYP1A2, CYP2B1 and CYP2B1/2 mRNA levels and CYP1A2 and CYP2B1/2 apoprotein levels. |
1(0,0,0,1) | Details |