The potential of coumatetralyl enhanced by cholecalciferol in the control of anticoagulant-resistant Norway rats (<i>Rattus norvegicus</i>)

Endepols, Stefan; Klemann, Nicole; Richter, D.; Matuschka, Franz‐Rainer

doi:10.1002/ps.4235

Cited by 10 publications

(9 citation statements)

References 28 publications

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“…Especially interesting from the ecotoxicological aspect is the use of rodenticides with ecofriendly compounds (Kocher & Navjot, 2013;Singla et al, 2015). Endepols et. al (2017) found that a combination of vitamin D3+coumatetralyl was eff ective in controlling Tyr139Cys carriers of Rattus norvegicus.…”

Section: A New Initiative For Anticoagulant Resistancementioning

confidence: 99%

Screening and prevention of anticoagulant resistance development in house mice: A review

2020

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Unrestricted use of anticoagulants has resulted in rodents developing resistance to them. This has caused a series of problems regarding reduction in rodent populations, which has further implicated great economic losses and a serious threat to the health of people and domestic animals. The popular global trend currently is to control rodent populations by applying the least possible amounts of chemicals, which on the other hand implies that several coactive alternative measures need to be applied in an effort to reduce rodent numbers to an acceptable economic level. On the other hand, knowledge of the genetic structure of rodent populations has become an important set of information desirable to have before setting off to apply rodenticides in practice, so as to prevent ineffective use of rodenticides and prevent further spreading of resistant rodent populations. The latest trend of using combinations of low-dose anticoagulant baits requires further research as their effects on susceptible populations are known but their impact on resistant animals is still not clear.

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Section: A New Initiative For Anticoagulant Resistancementioning

confidence: 99%

Screening and prevention of anticoagulant resistance development in house mice: A review

2020

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“…在鼠类中杀鼠灵的代谢被认为与 P450 基因家族中的 CYP2C, CYP2B, CYP1A 和 CYP3A 亚家族中的某些基因相关 [45] . Ishizuka 等人 [46] 发现 , [50] .…”

Section: 耐药性都是由其特定的遗传和生理基础决定的unclassified

Genetic Mechanism of Resistance to Anticoagulant Rodent Poison in Rodents

刘¹,

王²,

李³

et al. 2016

Sci. Sin.-Vitae

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Anticoagulant rodent poison is the most widely used rodenticide during the rodent control and management in the world. However, resistance to the anticoagulants has greatly decreased the effeciency of the rodent poison. Rodents can obtain anticoagulant resistance via different molecular pathways. The vitamin K epoxide reductase complex, subunit 1 (Vkorc1) gene is the target of anticoagulant rodenticides, and amino acid changes in Vkorc1 often cause anticoagulant resistance in rats and mice. In addition, the cytochrome P450 genes, Calumin and other genes are also found to be associated with the anticoagulant resistance in rats and mice. This article gives a brief review about the current state of anticoagulant resistance in rats and mice, the genetic mechansim of resistance and the recent progress on the study of resistance mechanism in rats and mice.

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“…To mitigate such environmental risks, in several countries the more-potent anticoagulant rodenticides are only allowed to use in or nearby invaded buildings and only after there is proof of resistance to less-potent anticoagulants. Although both combination with other drugs (for instance, coumatetralyl and cholecalciferol) 8 and proposed novel brodifacoum-like compounds computationally predicted with higher binding affinities to the main target enzyme 9 have been previously reported, there is an urgent need for new anticoagulant rodenticides and/or combinations which could maximize on-target and minimize off-target effects. Alternatively, other rodent-specific targets may also be investigated, but those are unknown.…”

Section: Introductionmentioning

confidence: 99%

Computational ligands to VKORC1s and CYPs. Could they predict new anticoagulant rodenticides?

Bermejo-Nogales

Navas

Coll

2021

Preprint

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Anticoagulant-resistance in rodents and anticoagulant off-target effects are some of the world-wide problems of increasing concern. To search for new anticoagulant rodenticide candidates we have computationally explored some of the rat genes previously implicated in resistance to actual anticoagulants. In particular, we searched among hundreds of anticoagulant-similar chemotypes those binding rat wild-type VKORC1 (the best-known anticoagulant target, a Vitamin K-recycling enzyme), VKORC1L1 (a VKORC1-related enzyme), Cytochrome P450 CYP enzymes (some of the most important enzymes implicated in detoxification) and anticoagulant-resistant VKORC1-mutants (to minimize propensity to resistance). Results predicted new VKORC1 leads with binding-scores in the low nM range (high binding-affinities) predicting hydroxycoumarin- and naphtoquinone-like chemotypes. We then selected top-leads with additional high binding-scores to more than three anticoagulant-related CYPs, suggesting minimal detoxification rates and therefore maximal anticoagulation expectatives. A downsized list of top top-leads maintaining VKORC1 low-binding scores to anticoagulant resistant mutants, was finally proposed for experimental validation. The combination of different rat targets for computational studies, could be used to search for unrelated chemotypes, for reduction of off-target environmental anticoagulant impacts, and/or as new tools to explore anticoagulant molecular mechanisms.

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The potential of coumatetralyl enhanced by cholecalciferol in the control of anticoagulant-resistant Norway rats (Rattus norvegicus)

Abstract: The combination of coumatetralyl and cholecalciferol is a promising alternative approach to the most potent second-generation anticoagulants in resistance management, particularly in respect of environmental risks, such as secondary poisoning. © 2016 Society of Chemical Industry.

Cited by 10 publications

References 28 publications

Screening and prevention of anticoagulant resistance development in house mice: A review

Screening and prevention of anticoagulant resistance development in house mice: A review

Genetic Mechanism of Resistance to Anticoagulant Rodent Poison in Rodents

Computational ligands to VKORC1s and CYPs. Could they predict new anticoagulant rodenticides?

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