Protein Information

Name cytochrome P450 1A2
Synonyms CP12; CYP1A2; CYPIA 2; CYPIA2; Cytochrome P450 1A2; Dioxin inducible P3 450; P(3)450; P3 450…

Compound Information

Name diazinon
CAS

Reference List

PubMed Abstract RScore(About this table)
11708902 Kappers WA, Edwards RJ, Murray S, Boobis AR: Diazinon is activated by CYP2C19 in human liver. . Toxicol Appl Pharmacol. 2001 Nov 15;177(1):68-76.

These data indicate that CYP2C19 is the major enzyme involved in diazinon activation in human liver, while other enzymes including CYP1A2 may play a more minor role.
113(1,2,2,3) Details
15764407 Sams C, Cocker J, Lennard MS: Biotransformation of chlorpyrifos and diazinon by human liver microsomes and recombinant human cytochrome P450s (CYP). Xenobiotica. 2004 Oct;34(10):861-73.

In contrast, both desulphuration and dearylation of diazinon were catalysed at similar rates, in the rank order CYP2C19 > CYP1A2 > CYP2B6 > CYP3A4.
81(1,1,1,1) 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).
Oxon formation in phenotyped individual HLM showed a significant correlation with CYP1A2-, 3A4-, and 2B6-related activities, at different levels depending on the OPT concentration.
4(0,0,0,4) Details
15557345 Buratti FM, D'Aniello A, Volpe MT, Meneguz A, Testai E: Malathion bioactivation in the human liver: the contribution of different cytochrome p450 isoforms. Drug Metab Dispos. 2005 Mar;33(3):295-302. Epub 2004 Nov 22.

These results are in line with those found with chlorpyrifos, diazinon, azynphos-methyl, and parathion, characterized by the presence of an aromatic ring in the molecule.
Results from different approaches indicated that, at low malathion concentration, malaoxon formation is catalyzed by CYP1A2 and, to a lesser extent, 2B6, whereas the role of 3A4 is relevant only at high malathion levels.
2(0,0,0,2) Details
18789379 Ueyama J, Kamijima M, Asai K, Mochizuki A, Wang D, Kondo T, Suzuki T, Takagi K, Takagi K, Kanazawa H, Miyamoto K, Wakusawa S, Hasegawa T: Effect of the organophosphorus pesticide diazinon on glucose tolerance in type 2 diabetic rats. Toxicol Lett. 2008 Nov 10;182(1-3):42-7. Epub 2008 Aug 22.

The activity of hepatic drug-metabolizing enzymes and expression of hepatic cytochrome P450 (CYP) 1A2, CYP3A2 and CYP2D1, which oxidize DZN to DZN-oxon, a potent ChE inhibitor, were measured before DZN injection.
1(0,0,0,1) Details
17442507 Ueyama J, Wang D, Kondo T, Saito I, Takagi K, Takagi K, Kamijima M, Nakajima T, Miyamoto K, Wakusawa S, Hasegawa T: Toxicity of diazinon and its metabolites increases in diabetic rats. Toxicol Lett. 2007 May 15;170(3):229-37. Epub 2007 Mar 24.

Hepatic drug-metabolizing enzyme activity was also estimated by measuring the systemic clearance of antipyrine, and the expression of hepatic cytochrome P450 (CYP) 3A2 and CYP1A2, which is closely related to the metabolism from DZN to DZN-oxon, a strong inhibitor of both ChE and AChE.
1(0,0,0,1) 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.
1(0,0,0,1) Details