| Name | acetylcholine receptor (protein family or complex) |
|---|---|
| Synonyms | Acetylcholine receptor; Acetylcholine receptors |
| Name | thiacloprid |
|---|---|
| CAS |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 11076703 | Tomizawa M, Casida JE: Imidacloprid, thiacloprid, and their imine derivatives up-regulate the alpha 4 beta 2 nicotinic acetylcholine receptor in M10 cells. Toxicol Appl Pharmacol. 2000 Nov 15;169(1):114-20. |
82(1,1,1,2) | Details |
| 12208819 | Tomizawa M, Casida JE: Selective toxicity of neonicotinoids attributable to specificity of insect and mammalian nicotinic receptors. Annu Rev Entomol. 2003;48:339-64. Epub 2002 Jun 4. Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). |
81(1,1,1,1) | Details |
| 17561262 | Tan J, Galligan JJ, Hollingworth RM: Agonist actions of neonicotinoids on nicotinic acetylcholine receptors expressed by cockroach neurons. Neurotoxicology. 2007 Jul;28(4):829-42. Epub 2007 Apr 20. Based on maximum inward currents, neonicotinoids could be divided into two subgroups: (1) those with a heterocyclic ring in their electronegative pharmacophore moiety (i.e. imidacloprid and thiacloprid) were relatively weak partial agonists causing only 20-25% of the maximum current and (2) open chain compounds (i.e. acetamiprid, dinotefuran, nitenpyram, and clothiandin) which were much more effective agonists producing 60-100% of the maximum current. |
2(0,0,0,2) | Details |
| 16981889 | Liu Z, Williamson MS, Lansdell SJ, Han Z, Denholm I, Millar NS: A nicotinic acetylcholine receptor mutation (Y151S) causes reduced agonist potency to a range of neonicotinoid insecticides. J Neurochem. 2006 Nov;99(4):1273-81. Epub 2006 Sep 18. The agonist potency of several nicotinic agonists has been examined, including all of the neonicotinoid insecticides that are currently licensed for either crop protection or animal health applications (acetamiprid, clothianidin, dinotefuran, imidacloprid, nitenpyram, thiacloprid and thiamethoxam). |
2(0,0,0,2) | Details |
| 10789501 | Wiesner P, Kayser H: Characterization of nicotinic acetylcholine receptors from the insects Aphis craccivora, Myzus persicae, and Locusta migratoria by radioligand binding assays: relation to thiamethoxam action. J Biochem Mol Toxicol. 2000;14(4):221-30. In all three insects, the other neonicotinoid insecticides studied competed with [3-H]-imidacloprid in the same order: thiacloprid > imidacloprid > or = acetamiprid > nitenpyram. |
2(0,0,0,2) | Details |
| 10936213 | Zhang A, Kayser H, Maienfisch P, Casida JE: Insect nicotinic acetylcholine receptor: conserved neonicotinoid specificity of [(3) H] imidacloprid binding site. J Neurochem. 2000 Sep;75(3):1294-303. The chlorothiazolyl substituent generally confers higher potency in the clothianidin and desmethylthiamethoxam series and the chloropyridinyl moiety in the imidacloprid, thiacloprid, acetamiprid, and nitenpyram series. |
2(0,0,0,2) | Details |
| 11312774 | Tomizawa M, Lee DL, Casida JE: Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors. J Agric Food Chem. 2000 Dec;48(12):6016-24. The favorable selective toxicity of neonicotinoid insecticides (represented here by imidacloprid, thiacloprid, and a nitromethylene analogue) for insects versus mammals is not shared by three of their N-unsubstituted imine derivatives or by or epibatidine. The same selectivity pattern is evident at the receptor level, i.e., the insect nicotinic acetylcholine receptor (nAChR) versus mammalian nAChR subtypes (alpha1, alpha3, alpha4, and alpha7) assayed independently. |
1(0,0,0,1) | Details |
| 11708903 | Tomizawa M, Cowan A, Casida JE: Analgesic and toxic effects of neonicotinoid insecticides in mice. Toxicol Appl Pharmacol. 2001 Nov 15;177(1):77-83. Several nicotinic agonists with the 6-chloro-3-pyridinyl moiety are potent insecticides (e.g., the neonicotinoids imidacloprid and thiacloprid) while others are candidate nonopioid and nonantiinflammatory analgesics (i.e., epibatidine and several heterocyclic analogs). This study examines the hypothesis for the first time that the neonicotinoid insecticides and their imine metabolites and analogs display analgesic (antinociceptive) activity or adverse toxic effects associated with their action on binding to the alpha 4 beta 2 nicotinic acetylcholine receptor (AChR) subtype. |
1(0,0,0,1) | Details |
| 18477694 | Talley TT, Harel M, Hibbs RE, Radic Z, Tomizawa M, Casida JE, Taylor P: Atomic interactions of neonicotinoid agonists with AChBP: molecular recognition of the distinctive electronegative pharmacophore. Proc Natl Acad Sci U S A. 2008 May 27;105(21):7606-11. Epub 2008 May 13. -binding proteins (AChBPs) from mollusks are suitable structural and functional surrogates of the nicotinic acetylcholine receptors when combined with transmembrane spans of the nicotinic receptor. Comparisons of the neonicotinoids imidacloprid and thiacloprid in the binding site from Aplysia californica AChBP at 2.48 and 1.94 A in resolution reveal a single conformation of the bound ligands with four of the five sites occupied in the pentameric crystal structure. |
1(0,0,0,1) | Details |
| 15481821 | Kayser H, Lee C, Decock A, Baur M, Haettenschwiler J, Maienfisch P: Comparative analysis of neonicotinoid binding to insect membranes: I. Pest Manag Sci. 2004 Oct;60(10):945-58. Neonicotinoids bind selectively to insect nicotinic acetylcholine receptors with nanomolar affinity to act as potent insecticides. Competitive neonicotinoids were acetamiprid, nitenpyram, thiacloprid, clothianidin and nithiazine, whereas thiamethoxam and the N-methyl analogues of imidacloprid and clothianidin showed non-competitive inhibition. |
1(0,0,0,1) | Details |