The GABA Activated Cl- Channel in Insects as Target for Insecticide Action: a Physiological Study

Keyserlingk, Harald C. von; Willis, R. John

doi:10.1007/978-94-011-2898-8_7

Cited by 17 publications

(13 citation statements)

References 25 publications

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“…2) has been noted before (Carrière, 1992a;Keyserlingk and Willis, 1992). However, the mechanism by which elevated GABA levels inhibit larval growth and development has not been established.…”

Section: Discussionmentioning

confidence: 99%

“…In vertebrates GABA receptors are restricted to the brain and are protected by the blood-brain barrier. Many commercially employed insecticides are agonists or antagonists of the GABA-gated C1-current, and are thought to cause paralysis through disruption of normal neuromuscular activity (Keyserlingk and Willis, 1992;Casida, 1993). GABA ingestion that raises levels in the hemolymph may similarly disrupt normal neuromuscular activity.…”

Section: Discussionmentioning

confidence: 99%

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Rapid [gamma]-Aminobutyric Acid Synthesis and the Inhibition of the Growth and Development of Oblique-Banded Leaf-Roller Larvae

1996

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l h e hypothesis that rapid y-aminobutyrate (GABA) accumulation is a plant defense against phytophagous insects was investigated.lncreasing GABA levels in a synthetic diet from 1.6 to 2.6 pmol g-' fresh weight reduced the growth rates, developmental rates, and survival rates of cultured Choristoneura rosaceana cv Harris larvae. Simulation of the mechanical damage resulting from phytophagous activity increased soybean (Glycine max L.) leaf GABA 10-to 25-fold within 1 to 4 min. Pulverizing leaf tissue resulted in a value of 2.15 (20.11 SE) pmol GABA g-' fresh weight.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Rapid [gamma]-Aminobutyric Acid Synthesis and the Inhibition of the Growth and Development of Oblique-Banded Leaf-Roller Larvae

1996

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“…In contrast, pentobarbital, 100 lM, enhanced both the amplitude and duration of the GABA responses of cultured locust neurones by up to 70% (Lees et al 1987). At concentrations above 5 lM, pentobarbital also enhanced ionophoretically applied GABA on locust-dissociated neurones (von Keyserlingk and Willis 1992). However, 300 lM thiopentone reversibly depressed the amplitude of fast chloride-dependent glutamate inhibitory events on snail neurones (Judge et al 1979).…”

Section: Discussionmentioning

confidence: 98%

“…The Drosophila GABA-A subunit, RDL, is sensitive to the benzodiazepine, 4-chlorodiazepam but not to flunitrazepam (Hosie and Sattelle 1996) while flunitrazepam, but not diazepam, modulates the action of GABA on locust neurones (von Keyserlingk and Willis 1992). Flunitrazepam-binding sites have been identified in the central nervous system of insects but interestingly the most potent ligand at displacing this binding, Ro5-4864, is selective for the vertebrate peripheral benzodiazepine-binding site (Lummis 1990).…”

Section: Discussionmentioning

confidence: 99%

The actions of chloride channel blockers, barbiturates and a benzodiazepine on Caenorhabditis elegans glutamate- and ivermectin-gated chloride channel subunits expressed in Xenopus oocytes

et al. 2009

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The pharmacology of Caenorhabditis elegans glutamate-gated chloride (GluCl) channels was determined by making intracellular voltage-clamp recordings from Xenopus oocytes expressing GluCl subunits. As previously reported (Cully et al. 1994), GluCla1b responded to glutamate (in a picrotoxin sensitive manner) and ivermectin, while GluClb responded only to glutamate and GluCla1 only to ivermectin. This assay was used to further investigate the action of chloride channel compounds. The arylaminobenzoate, NPPB, reduced the action of glutamate on the heteromeric GluCla1b channel (IC 50 6.03 ± 0.81 lM). The disulphonate stilbene, DNDS, blocked the effect of both glutamate and ivermectin on GluCla1b channels, the action of glutamate on GluClb subunits, and the effect of ivermectin on GluCla1 subunits (IC 50 s 1.58-3.83 lM). Surprisingly, amobarbital and pentobarbital, otherwise known as positive allosteric modulators of ligand-gated chloride channels, acted as antagonists. Both compounds reduced the action of glutamate on the GluCla1b heteromer (IC 50 s of 2.04 ± 0.5 and 17.56 ± 2.16 lM, respectively). Pentobarbital reduced the action of glutamate on the GluClb homomeric subunit with an IC 50 of 0.59 ± 0.09 lM, while reducing the responses to ivermectin on both GluCla1b and GluCla1 with IC 50 s of 8.7 ± 0.5 and 12.9 ± 2.5 lM, respectively. For all the antagonists, the mechanism is apparently noncompetitive. The benzodiazepine, flurazepam had no apparent effect on these glutamate-and ivermectin-gated chloride channel subunits. Thus, arylaminobenzoates, disulphonate stilbenes, and barbiturates are non-competitive antagonists of C. elegans GluCl channels.

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“…Our results are also generally comparable with observations on the effects of GABA on isolated neuronal cell bodies of insects. With sustained GABA applications the electrical response of Drosophila larvae (Zhang et al, 1994), locust thoracic (Bermudez et al, 1991;von Keyserlingk and Willis, 1992), cricket Kenyon (Cayre et al, 1999), and cockroach embryonic (Bermudez et al, 1991;Shimahara et al, 1987) neurones often reached a peak and then subsequently declined with a fast or a slow time course. Differences found may be due to different receptor densities or receptor types in these different cells.…”

Section: Discussionmentioning

confidence: 99%

Differential sensitivity of two insect GABA-gated chloride channels to dieldrin, fipronil and picrotoxinin

Corronc

Alix

Hue

2002

Journal of Insect Physiology

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In the central nervous system of both vertebrates and invertebrates inhibitory neurotransmission is mainly achieved through activation of γ-aminobutyric acid (GABA) receptors. Extensive studies have established the structural and pharmacological properties of vertebrate GABA receptors. Although the vast majority of insect GABA-sensitive responses share some properties with vertebrate GABAA receptors, peculiar pharmacological properties of these receptors led us to think that several GABA-gated chloride channels are present in insects. We describe here the pharmacological properties of two GABA receptor subtypes coupled to a chloride channel on dorsal unpaired median (DUM) neurones of the adult male cockroach. Long applications of GABA induce a large biphasic hyperpolarization, consisting of an initial transient hyperpolarization followed by a slow phase of hyperpolarization that is not quickly desensitized. With GABA, the transient hyperpolarization is sensitive to picrotoxinin, fipronil and dieldrin whereas the slow response is insensitive to these insecticides.When GABA is replaced by muscimol and cis-4-aminocrotonic acid (CACA) a biphasic hyperpolarization consisting of an initial transient hyperpolarization followed by a sustained phase is evoked which is blocked by picrotoxinin and fipronil. Exposure to dieldrin decreases only the early phase of the muscimol and CACA-induced biphasic response, suggesting that two GABA-gated chloride channel receptor subtypes are present in DUM neurones. This study describes, for the first time, a dieldrin resistant component different to the dieldrin-and picrotoxinin-resistant receptor found in several insect species. 

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The GABA Activated Cl- Channel in Insects as Target for Insecticide Action: a Physiological Study

Cited by 17 publications

References 25 publications

Rapid [gamma]-Aminobutyric Acid Synthesis and the Inhibition of the Growth and Development of Oblique-Banded Leaf-Roller Larvae

Rapid [gamma]-Aminobutyric Acid Synthesis and the Inhibition of the Growth and Development of Oblique-Banded Leaf-Roller Larvae

The actions of chloride channel blockers, barbiturates and a benzodiazepine on Caenorhabditis elegans glutamate- and ivermectin-gated chloride channel subunits expressed in Xenopus oocytes

Differential sensitivity of two insect GABA-gated chloride channels to dieldrin, fipronil and picrotoxinin

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