Protein Information

Name CYP3A
Synonyms CP33; CYP3; HLP; CYP3A; CP34; CYP 3A4; CYP 3; CYP3A3…

Compound Information

Name parathion
CAS

Reference List

PubMed Abstract RScore(About this table)
11913717 Hurh E, Lee EJ, Kim YG, Kim SY, Kim SH, Kim YC, Lee MG: Effects of neostigmine on the pharmacokinetics of intravenous parathion in rats. Res Commun Mol Pathol Pharmacol. 2000;108(3-4):261-73.

The purpose of this study is to explain the protective effects of neostigmine against paraoxon toxicity by suppressing CYP3A and hence decreasing formation of toxic metabolite, paraoxon by neostigmine.
2(0,0,0,2) Details
11514953 Hurh E, Lee EJ, Kim YG, Kim SY, Kim SH, Kim YC, Lee MG: Effects of physostigmine on the pharmacokinetics of intravenous parathion in rats. Biopharm Drug Dispos. 2000 Nov;21(8):331-8.

The purpose of this study is to explain the protective effects of physostigmine against paraoxon toxicity by suppressing CYP3A, and hence, decreasing formation of a toxic metabolite, paraoxon.
2(0,0,0,2) Details
11245398 Gelal A, Gumustekin M, Kalkan S, Guven H, Eminoglu O: Effects of subchronic parathion exposure on cyclosporine pharmacokinetics in rats. J Toxicol Environ Health A. 2001 Feb 23;62(4):289-94.

The CYP3A family is known to be responsible for the majority of cyclosporine metabolism.
1(0,0,0,1) Details
12620367 Buratti FM, Volpe MT, Meneguz A, Vittozzi L, Testai E: CYP-specific bioactivation of four organophosphorothioate pesticides by human liver microsomes. Toxicol Appl Pharmacol. 2003 Feb 1;186(3):143-54.

The bioactivation of azinphos-methyl (AZIN), chlorpyrifos (CPF), diazinon (DIA), and parathion (PAR), four widely used organophosphorothioate (OPT) pesticides has been investigated in human liver microsomes (HLM).
Our data indicated that CYP1A2 is mainly involved in OPT desulfuration at low pesticide concentrations, while the role of CYP3A4 is more significant to the low-affinity component of OPT bioactivation.
1(0,0,0,1) Details
9473531 Miranda CL, Henderson MC, Buhler DR: Evaluation of chemicals as inhibitors of trout cytochrome P450s. Toxicol Appl Pharmacol. 1998 Feb;148(2):237-44.


These imidazole compounds, as well as ellipticine, parathion, and alpha-naphthoflavone, were the strongest inhibitors of DMBA-OH and PROG-OH activities.
0(0,0,0,0) Details
9023313 Butler AM, Murray M: Biotransformation of parathion in human liver: participation of CYP3A4 and its inactivation during microsomal parathion oxidation. J Pharmacol Exp Ther. 1997 Feb;280(2):966-73.
274(3,4,4,4) Details
10414794 Mutch E, Blain PG, Williams FM: The role of metabolism in determining susceptibility to parathion toxicity in man. Toxicol Lett. 1999 Jun 30;107(1-3):177-87.

The activation of parathion (200 microM) was positively correlated with nifedipine oxidation, indicating the involvement of CYP3A.
118(1,2,3,3) Details
10996483 Sams C, Mason HJ, Rawbone R: Evidence for the activation of organophosphate pesticides by cytochromes P450 3A4 and 2D6 in human liver microsomes. Toxicol Lett. 2000 Aug 16;116(3):217-21.

The unexpected finding that CYP2D6, as well as CYP3A4, catalysed oxidative biotransformation was confirmed for chlorpyrifos and parathion using microsomes prepared from a human lymphoblastoid cell line expressing CYP2D6.
112(1,2,2,2) Details
15690761 Murray M, Butler AM: Comparative inhibition of inducible and constitutive CYPs in rat hepatic microsomes by parathion. Xenobiotica. 2004 Aug;34(8):723-39.

However, preincubation of parathion with NADPH-fortified microsomes intensified the extent of inhibition of CYP3A-dependent 6beta-hydroxylation.
82(1,1,1,2) Details
16757081 Mutch E, Williams FM: Diazinon, chlorpyrifos and parathion are metabolised by multiple cytochromes P450 in human liver. Toxicology. 2006 Jul 5;224(1-2):22-32. Epub 2006 Apr 26.

There were significant relationships between paraoxon formation from parathion (5 microM, 20 microM and 200 microM) and the CYP3A4/5, CYP2C8 and CYP1A2 mediated reactions, although only the latter two isoforms correlated significantly with the lowest parathion concentration.
32(0,1,1,2) Details
10484078 Nadin L, Murray M: Participation of CYP2C8 in retinoic acid 4-hydroxylation in human hepatic microsomes. Biochem Pharmacol. 1999 Oct 1;58(7):1201-8.

Greater inhibition was produced by the less selective CYP3A inhibitors parathion, quinidine, and ketoconazole; CYP1A inhibitors were ineffective.
32(0,1,1,2) Details
10794390 Eaton DL: Biotransformation enzyme polymorphism and pesticide susceptibility. Neurotoxicology. 2000 Feb-Apr;21(1-2):101-11.

Recent studies using cDNA expressed human CYPs have suggested that CYP3A4 is the principal human CYP involved in the oxidation of parathion and probably other organo (thio) phosphate (OP) insecticides and thus PM in this CYP might influence susceptibility to OP.
81(1,1,1,1) Details
12669189 Mutch E, Daly AK, Leathart JB, Blain PG, Williams FM: Do multiple cytochrome P450 isoforms contribute to parathion metabolism in man?. Arch Toxicol. 2003 Jun;77(6):313-20. Epub 2003 Mar 21.

These data indicate that CYP3A4/5 and CYP2C8, which constitute up to 40% of human liver P450s, are the most significant participants in the metabolism of parathion.
32(0,1,1,2) Details
17110060 Buratti FM, Leoni C, Testai E: Foetal and adult human CYP3A isoforms in the bioactivation of organophosphorothionate insecticides. Toxicol Lett. 2006 Dec 15;167(3):245-55. Epub 2006 Oct 24.

Since OPT-induced neurodevelopmental effects may be due to in situ bioactivation by foetal enzymes, the catalytic activity of the foetal CYP3A7 toward chlorpyrifos (CPF), parathion (PAR), malathion (MAL) and fenthion (FEN) has been assessed by using recombinant enzymes.
4(0,0,0,4) Details