The Mode of Action of Aldrin and Dieldrin in Periplaneta Americana (L.)1

Giannotti, O.; Metcalf, Robert L.; March, Ralph B.

doi:10.1093/aesa/49.6.588

Cited by 45 publications

(11 citation statements)

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“…in rats (Allen et al, 1979). In comparison, the topical LD 50 in American cockroaches was 1.3 to 1.5 mg/kg (Giannotti et al, 1959;O'Brien, 1967). For fipronil, the oral LD 50 in rats was 91 mg/kg, and the LD 50 values in insects were 0.07 mg/kg in corn rootworm (Scharf and Siegfried, 1999) and 0.13 mg/kg in house fly (Hainzl and Casida, 1996).…”

mentioning

confidence: 95%

Differential Actions of Fipronil and Dieldrin Insecticides on GABA-Gated Chloride Channels in Cockroach Neurons

Zhao

Salgado

Yeh³

et al. 2003

J Pharmacol Exp Ther

118

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Fipronil and dieldrin are known to inhibit GABA receptors in both mammals and insects. However, the mechanism of selective toxicity of these insecticides between mammals and insects remains to be seen. One possible mechanism is that insect GABA receptors are more sensitive than mammalian GABA A receptors to fipronil and dieldrin. We examined differential actions of fipronil and dieldrin on GABA-gated chloride channels in insects and compared them with the data on mammalian GABA A receptors. Neurons were acutely dissociated from the American cockroach thoracic ganglia, and currents evoked by GABA were recorded by the whole-cell patch-clamp technique. GABA-evoked currents were carried by chloride ions, blocked by picrotoxinin, but not by bicuculline. Fipronil inhibited GABA currents with an IC 50 value of 28 nM, whereas dieldrin exhibited a dual action potentiation with an EC 50 value of 4 nM followed by inhibition with an IC 50 value of 16 nM. Fipronil and dieldrin acted on the resting receptor at comparable rates, whereas fipronil blocked the activated receptor 10 times faster than dieldrin. Fipronil inhibition was partially reversible, whereas dieldrin inhibition was irreversible. Fipronil was 59 times more potent on cockroach GABA receptors than on rat GABA A receptors. However, the potentiating and inhibitory potencies of dieldrin in cockroach GABA receptors were comparable with those in rat GABA A receptors. It was concluded that the higher toxicity of fipronil in insects than in mammals is due partially to the higher sensitivity of GABA receptors. The mechanism of dieldrin's selective toxicity must lie in factors other than the sensitivity of GABA receptors.The selective toxicity between mammals and insects is one of the most important factors for the development of new insecticides. In fact, most insecticides on the market are more toxic to insects than to mammals. However, the mechanisms underlying high insecticidal activity and low mammalian toxicity of insecticides are not fully understood. Although the selective toxicity of certain insecticides (e.g., organophosphates) is due primarily to the differences in metabolism (O'

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confidence: 95%

Differential Actions of Fipronil and Dieldrin Insecticides on GABA-Gated Chloride Channels in Cockroach Neurons

Zhao

Salgado

Yeh³

et al. 2003

J Pharmacol Exp Ther

118

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“…Gowdey et al (1952) showed that aldrin augmented the reflex activity of the spinal cord and the excitability of spinal centres to acetylcholine and pentylenetetrazol (Metrazol). Aldrin is rapidly converted to dieldrin in the animal body and the effects of aldrin will therefore also hold good for dieldrin (Giannotti et al, 1956;Bann et al, 1965;Brooks, 1960). That dieldrin increases sensitivity to pentylene-tetrazol was confirmed also by Natoff and Reiff (1967).…”

Section: Introductionmentioning

confidence: 91%

Excitatory and depressant effects of dieldrin and aldrin-transdiol in the spinal cord of the toad (Xenopus laevis)

Akkermans

Bercken

Versluijs-Helder

1975

European Journal of Pharmacology

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L.M.A. AKKERMANS, J. VAN DEN BERCKEN and M. VERSLUIJS-HELDER, Excitatory and depressant effects of dieldrin and aldrin-transdiol in the spinal cord of the toad (Xenopus laevis), European J. Pharmacol. 34 (1975) 133--142. An investigation was made into the action of the insecticide dieldrin and one of its metabolites, aldrin-transdiol, on the isolated spinal cord of the toad, Xenopus laevis. Conventional electrophysiological techniques were used for stimulating and recording of dorsal and ventral spinal roots. An augmentation of polysynaptic reflex activity along with a marked reduction of orthodromic postsynaptic inhibition could be demonstrated in preparations isolated from dieldrin-poisoned animals. However, application of dieldrin to the isolated spinal cord failed to produce any significant effect. Application of aldrin-transdiol, on the other hand, caused a potentiation of spinal reflex activity and an increase in spontaneous activity of ventral and dorsal roots. Aldrin-transdiol also produced a marked reduction of spinal inhibitory mechanisms. The excitatory effects of aldrin-transdiol were followed by a strong depressant action on spinal excitability. Isolated spinal cord Postsynaptic inhibition Spinal root potentials Presynaptic inhibition DieldrinAldrin-transdiol

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“…In contrast to the conversion of aldrin and isodrin into their stable 6,7-epoxides, dieldrin and endrin (Giannotti et al, 1957;Kunze and Laug, 1953), 6,7-dihydroaldrin (9, Figure 96.1) and 6,7-dihydroisodrin (10) lacking the olefinic double bond, are monohydroxylated in the 6-(7) position by microsomal oxidases (Brooks, 1966;Brooks and Harrison, 1969a) and in vivo in houseflies. The stereoselective monohydroxylation of dihydroisodrin provided an alternative to the epoxidation reaction for the measurement of MFO activity (Krieger, 2008).…”

Section: Inhibitorsmentioning

confidence: 99%

Interactions with the Gamma-Aminobutyric Acid A-Receptor

Brooks¹

2010

Hayes' Handbook of Pesticide Toxicology

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The Mode of Action of Aldrin and Dieldrin in Periplaneta Americana (L.)1

Cited by 45 publications

References 0 publications

Differential Actions of Fipronil and Dieldrin Insecticides on GABA-Gated Chloride Channels in Cockroach Neurons

Differential Actions of Fipronil and Dieldrin Insecticides on GABA-Gated Chloride Channels in Cockroach Neurons

Excitatory and depressant effects of dieldrin and aldrin-transdiol in the spinal cord of the toad (Xenopus laevis)

Interactions with the Gamma-Aminobutyric Acid A-Receptor

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