Actions of the insecticide 2(nitromethylene)tetrahydro-1,3-thiazine on insect and vertebrate nicotinic acetylcholine receptors.

Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character
D B SattelleT E May

Abstract

The nitromethylene heterocyclic compound 2(nitromethylene)tetrahydro)1,3-thiazine (NMTHT) inhibits the binding of [125I]alpha-bungarotoxin to membranes prepared from cockroach (Periplaneta americana) nerve cord and fish (Torpedo californica) electric organ. Electrophysiological studies on the cockroach fast coxal depressor motorneuron (Df) reveal a dose-dependent depolarization in response to bath-applied NMTHT. Responses to ionophoretic application of NMTHT onto the cell-body membrane of motorneuron Df are suppressed by bath-applied mecamylamine (1.0 x 10(-4) M) and alpha-bungarotoxin (1.0 x 10(-7) M). These findings, together with the detection of a reversal potential close to that estimated for acetylcholine, provide evidence for an agonist action of this nitromethylene on an insect neuronal nicotinic acetylcholine receptor. The binding of [3H]H12-histrionicotoxin to Torpedo membranes was enhanced in the presence of NMTHT indicating an agonist action at this vertebrate peripheral nicotinic acetylcholine receptor. NMTHT is ineffective in radioligand binding assays for rat brain GABAA receptors, rat brain L-glutamate receptors and insect (Musca domestica) L-glutamate receptors. Partial block of rat brain muscarinic acetylcholi...Continue Reading

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Citations

Dec 1, 1996·Journal of Neurocytology·H A BaylisN J Lane
Apr 1, 1995·Toxicon : Official Journal of the International Society on Toxinology·C TornøeD B Sattelle
Jul 1, 1993·Toxicology in Vitro : an International Journal Published in Association with BIBRA·M OortgiesenH P Vijverberg
Nov 8, 2001·Trends in Pharmacological Sciences·K MatsudaD B Sattelle
Mar 2, 2002·Neuroscience Letters·Patrice DégliseMonique Gauthier
Jul 31, 1999·Bioorganic & Medicinal Chemistry·M HashimotoK Nakanishi
Jul 1, 1996·Pharmacology & Toxicology·T Narahashi
Mar 27, 2009·Molecular Pharmacology·Kazuhiko MatsudaDavid B Sattelle
Sep 5, 2002·Annual Review of Entomology·Motohiro Tomizawa, John E Casida
Apr 12, 2005·Annual Review of Pharmacology and Toxicology·Motohiro Tomizawa, John E Casida
Jan 16, 2013·Annual Review of Entomology·John E Casida, Kathleen A Durkin
Aug 21, 2008·Pest Management Science·Peter Jeschke, Ralf Nauen
Oct 8, 2016·Chemical Research in Toxicology·John E Casida, Kathleen A Durkin
Jun 23, 2005·Toxicon : Official Journal of the International Society on Toxinology·Samy ZalatIan R Mellor
Dec 16, 1997·Archives of Insect Biochemistry and Physiology·I YamamotoK Sumikawa
Jul 11, 1998·The Journal of Biological Chemistry·B HermsenA Maelicke
Jan 1, 1994·Archives of Insect Biochemistry and Physiology·D B SattelleM Ishida
Aug 13, 2013·Angewandte Chemie·Peter JeschkeMichael Edmund Beck
Mar 1, 1997·The Journal of General Physiology·J P DilgerA M Vidal
Jan 10, 2020·Annual Review of Pharmacology and Toxicology·Kazuhiko MatsudaDavid B Sattelle

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