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Insect Biochem Mol Biol
2011 Jan 01;411:36-41. doi: 10.1016/j.ibmb.2010.09.010.
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Analysis of the action of lidocaine on insect sodium channels.
Song W
,
Silver KS
,
Du Y
,
Liu Z
,
Dong K
.
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A new class of sodium channel blocker insecticides (SCBIs), which include indoxacarb, its active metabolite, DCJW, and metaflumizone, preferably block inactivated states of both insect and mammalian sodium channels in a manner similar to that by which local anesthetic (LA) drugs block mammalian sodium channels. A recent study showed that two residues in the cockroach sodium channel, F1817 and Y1824, corresponding to two key LA-interacting residues identified in mammalian sodium channels are not important for the action of SCBIs on insect sodium channels, suggesting unique interactions of SCBIs with insect sodium channels. However, the mechanism of action of LAs on insect sodium channels has not been investigated. In this study, we examined the effects of lidocaine on a cockroach sodium channel variant, BgNa(v)1-1a, and determined whether F1817 and Y1824 are also critical for the action of LAs on insect sodium channels. Lidocaine blocked BgNa(v)1-1a channels in the resting state with potency similar to that observed in mammalian sodium channels. Lidocaine also stabilized both fast-inactivated and slow-inactivated states of BgNa(v)1-1a channels, and caused a limited degree of use- and frequency-dependent block, major characteristics of LA action on mammalian sodium channels. Alanine substitutions of F1817 and Y1824 reduced the sensitivity of the BgNa(v)1-1a channel to the use-dependent block by lidocaine, but not to tonic blocking and inactivation stabilizing effects of lidocaine. Thus, similar to those on mammalian sodium channels, F1817 and Y1824 are important for the action of lidocaine on cockroach sodium channels. Our results suggest that the receptor sites for lidocaine and SCBIs are different on insect sodium channels.
Ahern,
Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels.
2008, Pubmed,
Xenbase
Ahern,
Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels.
2008,
Pubmed
,
Xenbase
Butterworth,
Molecular mechanisms of local anesthesia: a review.
1990,
Pubmed
Catterall,
From ionic currents to molecular mechanisms: the structure and function of voltage-gated sodium channels.
2000,
Pubmed
Feng,
Cloning and functional analysis of TipE, a novel membrane protein that enhances Drosophila para sodium channel function.
1995,
Pubmed
,
Xenbase
Gauthereau,
A mutation in the local anaesthetic binding site abolishes toluene effects in sodium channels.
2005,
Pubmed
,
Xenbase
Goldin,
Resurgence of sodium channel research.
2001,
Pubmed
Hille,
Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction.
1977,
Pubmed
Hondeghem,
Antiarrhythmic agents: the modulated receptor mechanism of action of sodium and calcium channel-blocking drugs.
1984,
Pubmed
Lapied,
Indoxacarb, an oxadiazine insecticide, blocks insect neuronal sodium channels.
2001,
Pubmed
Li,
A molecular basis for the different local anesthetic affinities of resting versus open and inactivated states of the sodium channel.
1999,
Pubmed
,
Xenbase
Liu,
Differential interactions of lamotrigine and related drugs with transmembrane segment IVS6 of voltage-gated sodium channels.
2003,
Pubmed
,
Xenbase
Nau,
Point mutations at L1280 in Nav1.4 channel D3-S6 modulate binding affinity and stereoselectivity of bupivacaine enantiomers.
2003,
Pubmed
Nau,
Point mutations at N434 in D1-S6 of mu1 Na(+) channels modulate binding affinity and stereoselectivity of local anesthetic enantiomers.
1999,
Pubmed
Pugsley,
Effects of bisaramil, a novel class I antiarrhythmic agent, on heart, skeletal muscle and brain Na+ channels.
1998,
Pubmed
,
Xenbase
Ragsdale,
Molecular determinants of state-dependent block of Na+ channels by local anesthetics.
1994,
Pubmed
,
Xenbase
Ragsdale,
Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channels.
1996,
Pubmed
Salgado,
Slow voltage-dependent block of sodium channels in crayfish nerve by dihydropyrazole insecticides.
1992,
Pubmed
Salgado,
Metaflumizone is a novel sodium channel blocker insecticide.
2007,
Pubmed
,
Xenbase
Silver,
State-dependent block of rat Nav1.4 sodium channels expressed in xenopus oocytes by pyrazoline-type insecticides.
2005,
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,
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
Song,
Molecular basis of differential sensitivity of insect sodium channels to DCJW, a bioactive metabolite of the oxadiazine insecticide indoxacarb.
2006,
Pubmed
,
Xenbase
Tan,
Alternative splicing of an insect sodium channel gene generates pharmacologically distinct sodium channels.
2002,
Pubmed
,
Xenbase
Tatebayashi,
Differential mechanism of action of the pyrethroid tetramethrin on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels.
1994,
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,
Residues in Na(+) channel D3-S6 segment modulate both batrachotoxin and local anesthetic affinities.
2000,
Pubmed
Wang,
Voltage-gated sodium channels as primary targets of diverse lipid-soluble neurotoxins.
2003,
Pubmed
Wang,
Point mutations in segment I-S6 render voltage-gated Na+ channels resistant to batrachotoxin.
1998,
Pubmed
Warmke,
Functional expression of Drosophila para sodium channels. Modulation by the membrane protein TipE and toxin pharmacology.
1997,
Pubmed
,
Xenbase
Weiser,
Differential interaction of R-mexiletine with the local anesthetic receptor site on brain and heart sodium channel alpha-subunits.
1999,
Pubmed
Wright,
Lysine point mutations in Na+ channel D4-S6 reduce inactivated channel block by local anesthetics.
1998,
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
Zhao,
Block of two subtypes of sodium channels in cockroach neurons by indoxacarb insecticides.
2005,
Pubmed
