| Name | acetylcholine receptor (protein family or complex) |
|---|---|
| Synonyms | Acetylcholine receptor; Acetylcholine receptors |
| Name | nitenpyram |
|---|---|
| CAS |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 9260539 | Chao SL, Dennehy TJ, Casida JE: Whitefly (Hemiptera: Aleyrodidae) binding site for imidacloprid and related insecticides: a putative nicotinic acetylcholine receptor. J Econ Entomol. 1997 Aug;90(4):879-82. Three related compounds (the nitromethylene analog of imidacloprid, acetamiprid, and nitenpyram) inhibit [3H] imidacloprid binding by 50% at 0.40, 2.9, and 57 nM, respectively. |
3(0,0,0,3) | 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 |
| 12208772 | Shimomura M, Okuda H, Matsuda K, Komai K, Akamatsu M, Sattelle DB: Effects of mutations of a residue in loop D of the alpha7 nicotinic acetylcholine receptor on agonist profiles for neonicotinoid insecticides and related ligands. Br J Pharmacol. 2002 Sep;137(2):162-9. |
2(0,0,0,2) | 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 |
| 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 |
| 12814666 | Ihara M, Matsuda K, Otake M, Kuwamura M, Shimomura M, Komai K, Akamatsu M, Raymond V, Sattelle DB: Diverse actions of neonicotinoids on chicken alpha7, alpha4beta2 and Drosophila-chicken SADbeta2 and ALSbeta2 hybrid nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes. Neuropharmacology. 2003 Jul;45(1):133-44. Imidacloprid and nitenpyram were partial agonists and a nitromethylene analog of imidacloprid (CH-IMI) was a full agonist of the alpha7 receptor, whereas their agonist actions on the alpha4beta2 receptor were very weak, contrasting with full agonist actions of DN-IMI, a desnitro derivative of imidacloprid. |
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 |
| 16153789 | Honda H, Tomizawa M, Casida JE: Neo-nicotinoid metabolic activation and inactivation established with coupled nicotinic receptor-CYP3A4 and -aldehyde oxidase systems. Toxicol Lett. 2006 Feb 20;161(2):108-14. Epub 2005 Sep 8. CYP3A4 oxidation at several molecular sites and AOX reduction at the nitro substituent result in either an increase (activation) or decrease (inactivation) of agonist potency at nicotinic acetylcholine receptors (nAChRs), both insect and vertebrate alpha 4beta 2. The AOX system coupled with the Drosophila receptor strongly inactivates clothianidin, dinotefuran, imidacloprid, desmethyl-thiamethoxam, and thiamethoxam with some inactivation of nitenpyram and nithiazine, and little or no effect on four other compounds. |
1(0,0,0,1) | Details |
| 10882381 | Matsuda K, Shimomura M, Kondo Y, Ihara M, Hashigami K, Yoshida N, Raymond V, Mongan NP, Freeman JC, Komai K, Sattelle DB: Role of loop D of the alpha7 nicotinic acetylcholine receptor in its interaction with the insecticide imidacloprid and related neonicotinoids. Br J Pharmacol. 2000 Jul;130(5):981-6. The nitroguanidine insecticide imidacloprid along with a second generation of related compounds including nitenpyram, all nicotinic receptor ligands, are used increasingly in many countries. |
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 |
| 10369463 | Tomizawa M, Casida JE: Minor structural changes in nicotinoid insecticides confer differential subtype selectivity for mammalian nicotinic acetylcholine receptors. Br J Pharmacol. 1999 May;127(1):115-22. The commercial insecticides (IMI, acetamiprid and nitenpyram) have low to moderate potency at the alpha3 and purported alpha4beta2 nicotinic AChRs and are essentially inactive at alpha1 and alpha7 nicotinic AChRs. |
1(0,0,0,1) | Details |
| 18405830 | Perry T, Heckel DG, McKenzie JA, Batterham P: Mutations in Dalpha1 or Dbeta2 nicotinic acetylcholine receptor subunits can confer resistance to neonicotinoids in Drosophila melanogaster. Insect Biochem Mol Biol. 2008 May;38(5):520-8. Epub 2008 Jan 3. Neonicotinoids target the nicotinic acetylcholine receptor (nAChR) of arthropods. EMS mutagenesis and selection for resistance to nitenpyram was performed on hybrids carrying a deficiency for this chromosomal region. |
1(0,0,0,1) | Details |