Interaction of Tetramethrin and Deltamethrin at the Single Sodium Channel in Rat Hippocampal Neurons

Motomura, Haruhiko; Narahashi, Toshio

doi:10.1016/s0161-813x(01)00023-7

Cited by 43 publications

(25 citation statements)

References 21 publications

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“…The Hill coefficient (P) determined from the concentration-response curves was 2.5 for ␣ 1G , 1.3 for ␣ 1C , and 1.3 for ␣ 1A . These IC 50 values for allethrin on calcium channels are in the same range as has previously been reported for several types of pyrethroids (including allethrin) acting on mammalian sodium channels (Ginsburg and Narahashi, 1999;Motomura and Narahashi, 2001;Soderlund and Lee, 2001;Spencer et al, 2001;Wang et al, 2001;de la Cerda et al, 2002).…”

Section: Resultssupporting

confidence: 83%

“…The expression of cloned voltage-gated calcium channels in HEK cells has allowed the comprehensive analysis of the different subtypes in both electrophysiological and pharmacological studies (for review, see Catterall, 2000). The prolonged opening of mammalian sodium channels induced by pyrethroids has been well documented (Motomura and Narahashi, 2001;Soderlund and Lee, 2001;Spencer et al, 2001;Wang et al, 2001;de la Cerda et al, 2002), but the blockade of calcium channels has not been well characterized (Hagiwara et al, 1988;Satoh, 1995). Using the HEK expression system, we analyzed the effects of different concentrations of the type I pyrethroid allethrin on three distinct calcium channel subtypes: i) a low-voltage activated T-type channel, ␣ 1G (Ca v 3.1); ii) a high-voltage activated P/Q-type channel, ␣ 1A (Ca v 2.1); and iii) a dihydropyridine-sensitive, high-voltage activated L-type channel, ␣ 1C (Ca v 1.2).…”

Section: Resultsmentioning

confidence: 99%

“…It has been generally assumed that the symptoms of acute toxicity of pyrethroid pesticides in humans is caused by their action on voltage-gated sodium channels (for review, see Zlotkin, 1999;Vais et al, 2001;Soderlund et al, 2002;Wang and Wang, 2003). A number of studies have shown that the properties of mammalian sodium channels are affected by pyrethroid concentrations in the 1 to 100 M range (Motomura and Narahashi, 2001;Soderlund and Lee, 2001;Spencer et al, 2001;Wang et al, 2001;de la Cerda et al, 2002). Dose-response experiments with mammalian sodium channels have demonstrated K d values that range from 0.44 to 95 M for deltamethrin, a type II pyrethroid, and tetramethrin, a type I pyrethroid (Tatebayashi and Narahashi, 1994;Vais et al, 2000).…”

Section: Discussionmentioning

confidence: 99%

“…A number of studies have shown that pyrethroids cause delayed inactivation and slowed deactivation of sodium channels resulting in longer channel openings and leading to overstimulation of nerves and eventual paralysis (for review, see Zlotkin, 1999;Vais et al, 2001;Soderlund et al, 2002;Wang and Wang, 2003). Tetramethrin, a type I pyrethroid, causes these effects when applied to single sodium channels from rat hippocampal neurons (Motomura and Narahashi, 2001). Unlike that found for sodium channels, we find that calcium channel whole-cell currents are blocked by pyrethroids, which would result in less current and subsequently less calcium influx into neurons (or other cells affected).…”

Section: Calcium Channel Blockade By the Insecticide Allethrin 811mentioning

confidence: 99%

“…Usually, pyrethroids are used at levels that prevent acute poisoning, but these lower levels may stimulate chronic effects when exposure is prolonged or recurrent (Abou-Donia et al, 2001). Since the primary target for the insecticidal action of pyrethroids are insect voltage-gated sodium channels, it is generally believed that mammalian sodium channels are also the primary targets for toxicity in humans (Motomura and Narahashi, 2001;Soderlund and Lee, 2001;Spencer et al, 2001;Wang et al, 2001;de la Cerda et al, 2002). Other potential molecular targets for pyrethroids include chloride channels, ATPases, GABA receptors, glutamate receptors, acetylcholine receptors, and voltage-gated calcium channels (Hagiwara et al, 1988;Satoh, 1995;Forshaw et al, 2000;Soderlund et al, 2002;Kakko et al, 2003).…”

mentioning

confidence: 99%

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Mammalian Voltage-Gated Calcium Channels Are Potently Blocked by the Pyrethroid Insecticide Allethrin

Hildebrand¹,

McRory²,

Snutch³

et al. 2003

J Pharmacol Exp Ther

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Pyrethroids are commonly used insecticides for both household and agricultural applications. It is generally reported that voltage-gated sodium channels are the primary target for toxicity of these chemicals to humans. The phylogenetic and structural relatedness between sodium channels and voltagegated calcium (Ca) channels prompted us to examine the effects of the type 1 pyrethroid allethrin on the three major classes of mammalian calcium channels exogenously expressed in human embryonic kidney 293 cells. We report that all classes of mammalian calcium channels are targets for allethrin at concentrations very similar to those reported for interaction with sodium channels. Allethrin caused blockade with IC 50 values of 7.0 ⌴ for T-type ␣ 1G (Ca v 3.1), 6.8 ⌴ for L-type ␣ 1C (Ca v 1.2), and 6.7 ⌴ for P/Q-type ␣ 1A (Ca v 2.1) channels. Mechanistically, the blockade of calcium channels was found to be significantly different than the prolonged opening of mammalian sodium channels caused by pyrethroids. In all calcium channel subtypes tested, allethrin caused a significant acceleration of the inactivation kinetics and a hyperpolarizing shift in the voltage dependence of inactivation. The highvoltage-activated P/Q-and L-type channels showed a frequency of stimulation-dependent increase in block by allethrin, whereas the low-voltage-activated ␣ 1G subtype did not. Allethrin did not significantly modify the deactivation kinetics or current-voltage relationships of any of the calcium channel types. Our study indicates that calcium channels are another primary target for allethrin and suggests that blockade of different types of calcium channels may underlie some of the chronic effects of low-level pyrethroid poisoning.

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Section: Resultssupporting

confidence: 83%

Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Calcium Channel Blockade By the Insecticide Allethrin 811mentioning

confidence: 99%

mentioning

confidence: 99%

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Mammalian Voltage-Gated Calcium Channels Are Potently Blocked by the Pyrethroid Insecticide Allethrin

Hildebrand¹,

McRory²,

Snutch³

et al. 2003

J Pharmacol Exp Ther

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An analysis of lethal and sublethal interactions among type I and type II pyrethroid pesticide mixtures using standard Hyalella azteca water column toxicity tests

Hoffmann

Deanovic

Werner

et al. 2016

Enviro Toxic and Chemistry

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A novel 2-tiered analytical approach was used to characterize and quantify interactions between type I and type II pyrethroids in Hyalella azteca using standardized water column toxicity tests. Bifenthrin, permethrin, cyfluthrin, and lambda-cyhalothrin were tested in all possible binary combinations across 6 experiments. All mixtures were analyzed for 4-d lethality, and 2 of the 6 mixtures (permethrin-bifenthrin and permethrin-cyfluthrin) were tested for subchronic 10-d lethality and sublethal effects on swimming motility and growth. Mixtures were initially analyzed for interactions using regression analyses, and subsequently compared with the additive models of concentration addition and independent action to further characterize mixture responses. Negative interactions (antagonistic) were significant in 2 of the 6 mixtures tested, including cyfluthrin-bifenthrin and cyfluthrin-permethrin, but only on the acute 4-d lethality endpoint. In both cases mixture responses fell between the additive models of concentration addition and independent action. All other mixtures were additive across 4-d lethality, and bifenthrin-permethrin and cyfluthrin-permethrin were also additive in terms of subchronic 10-d lethality and sublethal responses. Environ Toxicol Chem 2016;35:2542-2549. © 2016 SETAC.

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Ion Channel Electrophysiology in Cultured Neurons

Narahashi

2011

Neuromethods

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Interaction of Tetramethrin and Deltamethrin at the Single Sodium Channel in Rat Hippocampal Neurons

Cited by 43 publications

References 21 publications

Mammalian Voltage-Gated Calcium Channels Are Potently Blocked by the Pyrethroid Insecticide Allethrin

Mammalian Voltage-Gated Calcium Channels Are Potently Blocked by the Pyrethroid Insecticide Allethrin

An analysis of lethal and sublethal interactions among type I and type II pyrethroid pesticide mixtures using standard Hyalella azteca water column toxicity tests

Ion Channel Electrophysiology in Cultured Neurons

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