Protein Information

Name VKORC1
Synonyms Vitamin K epoxide reductase; IMAGE3455200; MST134; MST576; MSTP134; MSTP576; Phylloquinone epoxide reductase; UNQ308…

Compound Information

Name bromadiolone
CAS

Reference List

PubMed Abstract RScore(About this table)
17994578 Markussen MD, Heiberg AC, Fredholm M, Kristensen M: Characterization of bromadiolone resistance in a danish strain of Norway rats, Rattus norvegicus, by hepatic gene expression profiling of genes involved in vitamin K-dependent gamma-carboxylation. J Biochem Mol Toxicol. 2007;21(6):373-81.

We compared liver expression of the VKORC1 gene, which encodes a protein of the vitamin K 2,3-epoxide reductase complex, the NQO1 gene, which encodes a NAD (P) H quinone dehydrogenase and the Calumenin gene between bromadiolone-resistant and anticoagulant-susceptible rats upon saline and bromadiolone administration.
113(1,2,2,3) Details
8129744 Misenheimer TM, Lund M, Baker EM, Suttie JW: Biochemical basis of warfarin and bromadiolone resistance in the house mouse, Mus musculus domesticus. Biochem Pharmacol. 1994 Feb 11;47(4):673-8.

The hepatic vitamin K epoxide reductase in the bromadiolone-resistant mice and in one phenotype of warfarin-resistant mice was highly insensitive to in vitro inhibition by warfarin and bromadiolone.
31(0,1,1,1) Details
16933704 Kupper J, Grobosch T, Kistler R, Sydler T, Naegeli H: [Bromadiolone poisoning in foxes] . Schweiz Arch Tierheilkd. 2006 Aug;148(8):405-8.

Bromadiolone is an anticoagulant rodenticide that inhibits the reactivation of vitamin K1 by the enzyme vitamin K1-epoxide reductase.
81(1,1,1,1) Details
18080289 Markussen MD, Heiberg AC, Fredholm M, Kristensen M: Differential expression of cytochrome P450 genes between bromadiolone-resistant and anticoagulant-susceptible Norway rats: a possible role for pharmacokinetics in bromadiolone resistance. Pest Manag Sci. 2008 Mar;64(3):239-48.

To examine the involvement of pharmacokinetics in bromadiolone resistance in male and female rats, liver expression profiles of seven cytochrome P450 genes from a Danish bromadiolone-resistant rat strain (with an Y139C-VKORC1 mutation) were compared with profiles from an anticoagulant-susceptible strain.
7(0,0,1,2) Details
19752778 Grandemange A, Kohn MH, Lasseur R, Longin-Sauvageon C, Berny P, Benoit E: Consequences of the Y139F Vkorc1 mutation on resistance to AVKs: in-vivo investigation in a 7th generation of congenic Y139F strain of rats. Pharmacogenet Genomics. 2009 Oct;19(10):742-50.

RESULTS AND CONCLUSION: In this manuscript we report the prothrombin times measured in the F7 generation after exposure to chlorophacinone, bromadiolone, difenacoum and difethialone.
6(0,0,0,6) Details
15879509 Pelz HJ, Rost S, Hunerberg M, Fregin A, Heiberg AC, Baert K, MacNicoll AD, Prescott CV, Walker AS, Oldenburg J, Muller CR: The genetic basis of resistance to anticoagulants in rodents. Genetics. 2005 Aug;170(4):1839-47. Epub 2005 May 6.

Anticoagulant compounds, i.e., derivatives of either 4-hydroxycoumarin (e.g., warfarin, bromadiolone) or indane-1,3-dione (e.g., diphacinone, chlorophacinone), have been in worldwide use as rodenticides for > 50 years.
These compounds inhibit blood coagulation by repression of the vitamin K reductase reaction (VKOR).
4(0,0,0,4) Details