Abstract
To compare the actions of clothianidin, a neonicotinoid acting on insect nicotinic acetylcholine receptors, and related compounds with that of imidacloprid, the compounds were tested on the Drosophila SAD-chicken beta2 nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes using two-electrode voltage-clamp electrophysiology. The maximum response of the SAD beta 2 nicotinic receptor to clothianidin was larger than that observed for acetylcholine. Ring breakage of the imidazolidine ring of imidacloprid resulting in the generation of a guanidine group was critical for this super agonist action.
MeSH terms
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Acetylcholine / pharmacology
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Anabasine / analogs & derivatives
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Anabasine / chemistry
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Anabasine / pharmacology
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Animals
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DNA, Complementary / genetics
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DNA, Recombinant / genetics
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Drosophila Proteins
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Electrophysiology / methods
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Guanidines / chemistry*
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Guanidines / pharmacology*
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Imidazoles / chemistry
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Imidazoles / pharmacology
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Molecular Structure
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Neonicotinoids
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Nicotinic Agonists / chemistry*
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Nicotinic Agonists / pharmacology*
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Nitro Compounds
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Oocytes / drug effects
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Oocytes / metabolism
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Receptors, Nicotinic / drug effects*
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Receptors, Nicotinic / genetics
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Receptors, Nicotinic / physiology
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Thiazoles
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Transfection
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Xenopus laevis
Substances
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DNA, Complementary
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DNA, Recombinant
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Drosophila Proteins
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Guanidines
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Imidazoles
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Neonicotinoids
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Nicotinic Agonists
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Nitro Compounds
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Receptors, Nicotinic
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Thiazoles
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nicotinic acetylcholine receptor alpha-subunits, Drosophila
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nicotinic receptor beta2
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clothianidin
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imidacloprid
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Anabasine
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Acetylcholine