Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Curr Med Chem
2017 Jan 01;2427:2912-2924. doi: 10.2174/0929867323666161216143844.
Show Gene links
Show Anatomy links
Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides.
Silver K
,
Dong K
,
Zhorov BS
.
???displayArticle.abstract???
Sodium channel blocker insecticides (SCBIs) are a relatively new class of insecticides that are represented by two commercially registered compounds, indoxacarb and metaflumizone. SCBIs, like pyrethroids and DDT, target voltage-gated sodium channels (VGSCs) to intoxicate insects. In contrast to pyrethroids, however, SCBIs inhibit VGSCs at a distinct receptor site that overlaps those of therapeutic inhibitors of sodium channels, such as local anesthetics, anticonvulsants and antiarrhythmics. This review will recount the development of the SCBI insecticide class from its roots as chitin synthesis inhibitors, discuss the symptoms of poisoning and evidence supporting inhibition of VGSCs as their mechanism of action, describe the current model for SCBI-induced inhibition of VGSCs, present a model for the receptor for SCBIs on VGSCs, and highlight differences between data collected from mammalian and insect experimental models.
???displayArticle.pubmedLink???
27993108
???displayArticle.pmcLink???PMC5730267 ???displayArticle.link???Curr Med Chem ???displayArticle.grants???[+]
,
Metaflumizone: a novel insecticide for application in animal health. Proceedings of the Fort Dodge Animal Health Global Roundtable, October 2006, Coral Gables, Florida, USA and the symposium of the World Association for the Advancement of Veterinary Parasitology, August 2007, Ghent, Belgium.
2008, Pubmed
,
Metaflumizone: a novel insecticide for application in animal health. Proceedings of the Fort Dodge Animal Health Global Roundtable, October 2006, Coral Gables, Florida, USA and the symposium of the World Association for the Advancement of Veterinary Parasitology, August 2007, Ghent, Belgium.
2008,
Pubmed
Ahmad,
Synergism of insecticides provides evidence of metabolic mechanisms of resistance in the obliquebanded leafroller Choristoneura rosaceana (Lepidoptera: Tortricidae).
2004,
Pubmed
Catterall,
From ionic currents to molecular mechanisms: the structure and function of voltage-gated sodium channels.
2000,
Pubmed
Creveling,
Batrachotoxin-induced depolarization and [3H]batrachotoxinin-a 20 alpha-benzoate binding in a vesicular preparation from guinea pig cerebral cortex.
1983,
Pubmed
Dong,
Insect sodium channels and insecticide resistance.
2007,
Pubmed
,
Xenbase
Dong,
Molecular biology of insect sodium channels and pyrethroid resistance.
2014,
Pubmed
Du,
Molecular evidence for dual pyrethroid-receptor sites on a mosquito sodium channel.
2013,
Pubmed
,
Xenbase
Goldin,
Mechanisms of sodium channel inactivation.
2003,
Pubmed
Goldin,
Resurgence of sodium channel research.
2001,
Pubmed
Hempel,
Toxicological properties of metaflumizone.
2007,
Pubmed
Jiang,
Mutations in the transmembrane helix S6 of domain IV confer cockroach sodium channel resistance to sodium channel blocker insecticides and local anesthetics.
2015,
Pubmed
,
Xenbase
Khakame,
Baseline toxicity of metaflumizone and lack of cross resistance between indoxacarb and metaflumizone in diamondback moth (Lepidoptera: Plutellidae).
2013,
Pubmed
Lapied,
Indoxacarb, an oxadiazine insecticide, blocks insect neuronal sodium channels.
2001,
Pubmed
Lavialle-Defaix,
How does calcium-dependent intracellular regulation of voltage-dependent sodium current increase the sensitivity to the oxadiazine insecticide indoxacarb metabolite decarbomethoxylated JW062 (DCJW) in insect pacemaker neurons?
2010,
Pubmed
Leong,
Insecticidal arylalkylbenzhydrolpiperidines: novel inhibitors of voltage-sensitive sodium and calcium channels in mammalian brain.
2001,
Pubmed
Lipkind,
Molecular modeling of local anesthetic drug binding by voltage-gated sodium channels.
2005,
Pubmed
Liu,
Differential interactions of lamotrigine and related drugs with transmembrane segment IVS6 of voltage-gated sodium channels.
2003,
Pubmed
,
Xenbase
Mike,
The enigmatic drug binding site for sodium channel inhibitors.
2010,
Pubmed
Mulder,
A new class of insecticides.
1975,
Pubmed
Nau,
Point mutations at N434 in D1-S6 of mu1 Na(+) channels modulate binding affinity and stereoselectivity of local anesthetic enantiomers.
1999,
Pubmed
O'Reilly,
Residue-specific effects on slow inactivation at V787 in D2-S6 of Na(v)1.4 sodium channels.
2001,
Pubmed
Oh,
Methemoglobinemia associated with metaflumizone poisoning.
2014,
Pubmed
Oxford,
Removal of sodium channel inactivation in squid giant axons by n-bromoacetamide.
1978,
Pubmed
Park,
Successful treatment of methemoglobinemia and acute renal failure after indoxacarb poisoning.
2011,
Pubmed
Prasanna,
Indoxacarb poisoning: an unusual presentation as methemoglobinemia.
2008,
Pubmed
Ragsdale,
Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channels.
1996,
Pubmed
Ragsdale,
Molecular determinants of state-dependent block of Na+ channels by local anesthetics.
1994,
Pubmed
,
Xenbase
Rugg,
Dose determination of a novel formulation of metaflumizone plus amitraz for control of cat fleas (Ctenocephalides felis felis) and brown dog ticks (Rhipicephalus sanguineus) on dogs.
2007,
Pubmed
Salgado,
Metaflumizone is a novel sodium channel blocker insecticide.
2007,
Pubmed
,
Xenbase
Salgado,
Slow voltage-dependent block of sodium channels in crayfish nerve by dihydropyrazole insecticides.
1992,
Pubmed
Sayyed,
Genetics and evidence for an esterase-associated mechanism of resistance to indoxacarb in a field population of diamondback moth (Lepidoptera: Plutellidae).
2006,
Pubmed
Silver,
Differential sensitivity of rat voltage-sensitive sodium channel isoforms to pyrazoline-type insecticides.
2006,
Pubmed
,
Xenbase
Silver,
State-dependent block of rat Nav1.4 sodium channels expressed in xenopus oocytes by pyrazoline-type insecticides.
2005,
Pubmed
,
Xenbase
Silver,
Role of the sixth transmembrane segment of domain IV of the cockroach sodium channel in the action of sodium channel blocker insecticides.
2009,
Pubmed
,
Xenbase
Silver,
Point mutations at the local anesthetic receptor site modulate the state-dependent block of rat Na v1.4 sodium channels by pyrazoline-type insecticides.
2007,
Pubmed
,
Xenbase
Silver,
Mechanism of action of sodium channel blocker insecticides (SCBIs) on insect sodium channels.
2010,
Pubmed
Silver,
Voltage-Gated Sodium Channels as Insecticide Targets.
2014,
Pubmed
Song,
Molecular basis of differential sensitivity of insect sodium channels to DCJW, a bioactive metabolite of the oxadiazine insecticide indoxacarb.
2006,
Pubmed
,
Xenbase
Song,
Analysis of the action of lidocaine on insect sodium channels.
2011,
Pubmed
,
Xenbase
Starkus,
Modification of slow sodium inactivation in nerve after internal perfusion with trypsin.
1978,
Pubmed
Takagi,
Discovery of metaflumizone, a novel semicarbazone insecticide.
2007,
Pubmed
Tikhonov,
Sodium channels: ionic model of slow inactivation and state-dependent drug binding.
2007,
Pubmed
Tsurubuchi,
Modulation of sodium channels by the oxadiazine insecticide indoxacarb and its N-decarbomethoxylated metabolite in rat dorsal root ganglion neurons.
2003,
Pubmed
Wang,
Two novel sodium channel mutations associated with resistance to indoxacarb and metaflumizone in the diamondback moth, Plutella xylostella.
2016,
Pubmed
Wang,
A common local anesthetic receptor for benzocaine and etidocaine in voltage-gated mu1 Na+ channels.
1998,
Pubmed
Wang,
State-dependent block of voltage-gated Na+ channels by amitriptyline via the local anesthetic receptor and its implication for neuropathic pain.
2004,
Pubmed
Wang,
Voltage-gated sodium channels as primary targets of diverse lipid-soluble neurotoxins.
2003,
Pubmed
Wierenga,
Insecticidal activity of N-arylalkylbenzhydrolpiperidines.
2002,
Pubmed
Wismer,
Toxicology of newer insecticides in small animals.
2012,
Pubmed
Wu,
Methemoglobinemia induced by indoxacarb intoxication.
2010,
Pubmed
Yarov-Yarovoy,
Molecular determinants of voltage-dependent gating and binding of pore-blocking drugs in transmembrane segment IIIS6 of the Na(+) channel alpha subunit.
2001,
Pubmed
,
Xenbase
Yarov-Yarovoy,
Role of amino acid residues in transmembrane segments IS6 and IIS6 of the Na+ channel alpha subunit in voltage-dependent gating and drug block.
2002,
Pubmed
,
Xenbase
Zhang,
The Receptor Site and Mechanism of Action of Sodium Channel Blocker Insecticides.
2016,
Pubmed
Zhao,
Block of two subtypes of sodium channels in cockroach neurons by indoxacarb insecticides.
2005,
Pubmed
Zhao,
Voltage-dependent block of sodium channels in mammalian neurons by the oxadiazine insecticide indoxacarb and its metabolite DCJW.
2003,
Pubmed
Zhorov,
Potassium, sodium, calcium and glutamate-gated channels: pore architecture and ligand action.
2004,
Pubmed
von Stein,
Role of the local anesthetic receptor in the state-dependent inhibition of voltage-gated sodium channels by the insecticide metaflumizone.
2012,
Pubmed
,
Xenbase
von Stein,
Compound-specific effects of mutations at Val787 in DII-S6 of Nav 1.4 sodium channels on the action of sodium channel inhibitor insecticides.
2012,
Pubmed
,
Xenbase
von Stein,
Indoxacarb, Metaflumizone, and Other Sodium Channel Inhibitor Insecticides: Mechanism and Site of Action on Mammalian Voltage-Gated Sodium Channels.
2013,
Pubmed
,
Xenbase
