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Insects 2017, 8(1), 2; doi:10.3390/insects8010002

Toxicity and Physiological Actions of Carbonic Anhydrase Inhibitors to Aedes aegypti and Drosophila melanogaster

Department of Entomology and Nematology, Emerging Pathogens Institute, University of Florida, Gainesville, FL 32610, USA
Author to whom correspondence should be addressed.
Academic Editor: Brian T. Forschler
Received: 13 November 2016 / Revised: 12 December 2016 / Accepted: 14 December 2016 / Published: 22 December 2016
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The physiological role of carbonic anhydrases in pH and ion regulation is crucial to insect survival. We examined the toxic and neurophysiological effects of five carbonic anhydrase inhibitors (CAIs) against Aedes aegypti. The 24 h larvicidal toxicities followed this rank order of potency: dichlorphenamide > methazolamide > acetazolamide = brinzolamide = dorzolamide. Larvicidal activity increased modestly in longer exposures, and affected larvae showed attenuated responses to probing without overt tremors, hyperexcitation, or convulsions. Acetazolamide and dichlorphenamide were toxic to adults when applied topically, but were of low potency and had an incomplete effect (<50% at 300 ng/mosquito) even after injection. Dichlorphenamide was also the most toxic compound when fed to adult mosquitoes, and they displayed loss of posture and occasionally prolonged fluttering of the wings. Co-exposure with 500 ng of the synergist piperonyl butoxide (PBO) increased the toxicity of dichlorphenamide ca. two-fold in feeding assays, indicating that low toxicity was not related to oxidative metabolism. Dichlorphenamide showed mild depolarizing and nerve discharge actions on insect neuromuscular and central nervous systems, respectively. These effects were increased in low buffer salines, indicating they were apparently related to loss of pH control in these tissues. Overall, sulfonamides displayed weak insecticidal properties on Aedes aegypti and are weak lead compounds. View Full-Text
Keywords: acetazolamide; brinzolamide; dichlorphenamide; dorzolamide; methazolamide insecticide; mode of action acetazolamide; brinzolamide; dichlorphenamide; dorzolamide; methazolamide insecticide; mode of action

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Francis, S.A.M.; Taylor-Wells, J.; Gross, A.D.; Bloomquist, J.R. Toxicity and Physiological Actions of Carbonic Anhydrase Inhibitors to Aedes aegypti and Drosophila melanogaster. Insects 2017, 8, 2.

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