| Name | CYP3A4 |
|---|---|
| Synonyms | CP33; CYP3; HLP; CYP3A; CP34; CYP 3A4; CYP 3; CYP3A3… |
| Name | permethrin |
|---|---|
| CAS | (3-phenoxyphenyl)methyl 3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropanecarboxylate |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 16565514 | Lemaire G, Mnif W, Pascussi JM, Pillon A, Rabenoelina F, Fenet H, Gomez E, Casellas C, Nicolas JC, Cavailles V, Duchesne MJ, Balaguer P: Identification of new human pregnane X receptor ligands among pesticides using a stable reporter cell system. Toxicol Sci. 2006 Jun;91(2):501-9. Epub 2006 Mar 24. Some of the newly identified hPXR activators were also checked for their ability to induce cytochrome P450 3A4 expression in a primary culture of human hepatocytes. Pesticides from various chemical classes were demonstrated, for the first time, to be hPXR activators: (1) herbicides: pretilachlor, metolachlor, and alachlor chloracetanilides, oxadiazon oxiconazole, and isoproturon urea; (2) fungicides: bupirimate and fenarimol pyrimidines, propiconazole, fenbuconazole, prochloraz conazoles, and imazalil triazole; and (3) insecticides: toxaphene organochlorine, permethrin pyrethroid, fipronil pyrazole, and diflubenzuron urea. |
1(0,0,0,1) | Details |
| 18948380 | Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. Epub 2008 Oct 23. Human P450 isoforms that showed activity toward multiple pyrethroids were CYP2C8, CYP2C9, CYP2C19, and CYP3A4. The pyrethroids bifenthrin, S-bioallethrin, bioresmethrin, beta-cyfluthrin, cypermethrin, cis-permethrin, and trans-permethrin were incubated in rat and human hepatic microsomes in the presence or absence of |
1(0,0,0,1) | Details |
| 12587253 | Abu-Qare AW, Abou-Donia MB: Combined exposure to DEET (N,N-diethyl-m-toluamide) and permethrin: pharmacokinetics and toxicological effects. J Toxicol Environ Health B Crit Rev. 2003 Jan-Feb;6(1):41-53. Concurrent application of DEET and permethrin induced urinary excretion of and markers of DNA damage and oxidative stress in rats, increased the release of rat brain mitochondrial cytochrome c, disrupted the blood-brain barrier (BBB) in rats, decreased m2 muscarinic acetylcholine receptor ligand binding density in rat brain, increased urinary excretion of 6 beta-hydroxycortisol, a marker CYP3A4 induction, altered sensorimotor and locomotor activities in rats, and changed in vivo and in vitro metabolism and pharmacokinetic profiles of the individual compound. |
31(0,1,1,1) | Details |
| 19326768 | Das PC, Streit TM, Cao Y, Rose RL, Cherrington N, Ross MK, Wallace AD, Hodgson E: Pyrethroids: cytotoxicity and induction of CYP isoforms in human hepatocytes. Drug Metabol Drug Interact. 2008;23(3-4):211-36. Permethrin-mediated CYP induction was much less potent, 4-fold or less for CYP1A1, CYP3A4, CYP3A5, CYP2B6 and CYP2A6. |
82(1,1,1,2) | Details |
| 16790556 | Usmani KA, Cho TM, Rose RL, Hodgson E: Inhibition of the human liver microsomal and human cytochrome P450 1A2 and 3A4 metabolism of by deployment-related and other chemicals. Drug Metab Dispos. 2006 Sep;34(9):1606-14. Epub 2006 Jun 21. Preincubation of CYP3A4 with chlorpyrifos, fonofos, deltamethrin, or permethrin resulted in 94, 87, 58, and 37% inhibition of E2 metabolism. |
35(0,1,1,5) | Details |
| 11700004 | Abu-Qare AW, Abou-Donia MB: DEET (N,N-diethyl-m-toluamide) alone and in combination with permethrin increased urinary excretion of 6beta-hydroxycortisol in rats, a marker of hepatic CYP3A induction. J Toxicol Environ Health A. 2001 Nov 9;64(5):373-84. |
6(0,0,1,1) | Details |
| 17936932 | Hodgson E, Rose RL: Human metabolic interactions of environmental chemicals. J Biochem Mol Toxicol. 2007;21(4):182-6. OPs are potent irreversible inhibitors of metabolism by cytochrome P450 (CYP) 3A4 and of metabolism by CYP3A4 and CYP1A2. It has also been shown that the esterase (s) responsible for the initial step in permethrin metabolism in human liver is inhibited by both chlorpyrifos oxon and carbaryl. |
2(0,0,0,2) | Details |
| 18322939 | Hodgson E, Rose RL: Metabolic interactions of agrochemicals in humans. Pest Manag Sci. 2008 Jun;64(6):617-21. The insecticides chlorpyrifos, carbaryl, carbofuran and fipronil, as well as the repellant DEET, are all extensively metabolized by human liver microsomes and, although a number of CYP isoforms may be involved, CYP2B6 and CYP3A4 are usually the most important. Permethrin is hydrolyzed by esterase (s) present in both human liver microsomes and cytosol. |
2(0,0,0,2) | Details |
| 8541882 | Wang XP, Hobbs AA: Isolation and sequence analysis of a cDNA clone for a pyrethroid inducible cytochrome P450 from Helicoverpa armigera. Insect Biochem Mol Biol. 1995 Oct;25(9):1001-9. This sequence is also present in mammalian members of family CYP3. Induction studies indicate that the smaller mRNA is inducible by phenobarbital while the larger mRNA is inducible by the pyrethroid insecticide permethrin. |
1(0,0,0,1) | Details |
| 11854147 | Usmani KA, Rose RL, Goldstein JA, Taylor WG, Brimfield AA, Hodgson E: In vitro human metabolism and interactions of repellent N,N-diethyl-m-toluamide. Drug Metab Dispos. 2002 Mar;30(3):289-94. Preincubation of human or rodent microsomes with chlorpyrifos, permethrin, and pyridostigmine bromide alone or in combination can lead to either stimulation or inhibition of DEET metabolism. Among 15 cDNA-expressed P450 enzymes examined, CYP1A2, 2B6, 2D6*1 (Val (374)), and 2E1 metabolized DEET to the BALC metabolite, whereas CYP3A4, 3A5, 2A6, and 2C19 produced the ET metabolite. |
1(0,0,0,1) | Details |