| Name | acetylcholine receptor (protein family or complex) |
|---|---|
| Synonyms | Acetylcholine receptor; Acetylcholine receptors |
| Name | imidacloprid |
|---|---|
| CAS |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 15056916 | Ihara M, Matsuda K, Shimomura M, Sattelle DB, Komai K: Super agonist actions of clothianidin and related compounds on the SAD beta 2 nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes. Biosci Biotechnol Biochem. 2004 Mar;68(3):761-3. 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. |
7(0,0,1,2) | Details |
| 12974354 | Nishiwaki H, Nakagawa Y, Kuwamura M, Sato K, Akamatsu M, Matsuda K, Komai K, Miyagawa H: Correlations of the electrophysiological activity of neonicotinoids with their binding and insecticidal activities. Pest Manag Sci. 2003 Sep;59(9):1023-30. The electrophysiological actions of various neonicotinoids, including substituted benzyl derivatives, against recombinant Drosophila SAD/chicken beta2 hybrid nicotinic acetylcholine receptor (nAChR) were measured to analyze the relationships between the in vivo (insecticidal) and in vitro (binding and agonist) activities. Variations in the agonist activity were well correlated with those in the binding potency evaluated using [3H] imidacloprid as well as insecticidal activities. |
1(0,0,0,1) | Details |
| 15246549 | Zafeiridou G, Theophilidis G: The action of the insecticide imidacloprid on the respiratory rhythm of an insect: the beetle Tenebrio molitor. Neurosci Lett. 2004 Jul 29;365(3):205-9. Imidacloprid is an insecticide which has the nicotinic acetylcholine receptors (nAChRs) as its primary site of action; acetylcholine is the major excitatory neurotransmitter in the insect central nervous system (CNS). |
6(0,0,1,1) | Details |
| 14584674 | Dussourd DE: Chemical stimulants of leaf-trenching by cabbage loopers: natural products, neurotransmitters, insecticides, and drugs. J Chem Ecol. 2003 Sep;29(9):2023-47. Lactucin, myristicin, and lobeline all affect the nervous system of mammals, with lobeline acting specifically as an antagonist of nicotinic acetylcholine receptors. Active compounds included the insecticide imidacloprid, and various drugs such as ipratropium, apomorphine, and metoclopramide. |
1(0,0,0,1) | Details |
| 9397513 | Yamamoto I, Tomizawa M, Saito T, Miyamoto T, Walcott EC, Sumikawa K: Structural factors contributing to insecticidal and selective actions of neonicotinoids. Arch Insect Biochem Physiol. 1998;37(1):24-32. N-Me-imidacloprid was found to be a propesticide of imidacloprid. Both types of insecticides interact with nicotinic acetylcholine receptor (nAChR) of insect origin. |
1(0,0,0,1) | Details |
| 10728888 | Lansdell SJ, Millar NS: The influence of nicotinic receptor subunit composition upon agonist, alpha-bungarotoxin and insecticide (imidacloprid) binding affinity. Neuropharmacology. 2000 Feb 14;39(4):671-9. A series of cell lines stably expressing recombinant nicotinic acetylcholine receptors (nAChRs) has been established by transfection of mammalian (rat) and insect (Drosophila) nicotinic subunit cDNAs. |
1(0,0,0,1) | Details |
| 11579144 | Tomizawa M, Wen Z, Chin HL, Morimoto H, Kayser H, Casida JE: Photoaffinity labeling of insect nicotinic acetylcholine receptors with a novel [(3) H] azidoneonicotinoid. J Neurochem. 2001 Sep;78(6):1359-66. Compared to their non-azido parents, both probes are of decreased potencies at Drosophila (fruit fly) and Musca (housefly) receptors but AzNN retains full potency at the Myzus (aphid) receptor. [(3) H] AzNN was therefore radiosynthesized at high specific activity (84 Ci/mmol) as a novel photoaffinity probe. [(3) H] AzNN binds to a single high-affinity site in Myzus that is competitively inhibited by imidacloprid and and further characterized as to its pharmacological profile with various nicotinic ligands. [(3) H] AzNN photoaffinity labeling of Myzus and Homalodisca (leafhopper) detects a single radiolabeled peak in each case displaceable with imidacloprid and and with molecular masses corresponding to approximately 45 and approximately 56 kDa, respectively. |
2(0,0,0,2) | Details |
| 16116270 | Matsuda K, Shimomura M, Ihara M, Akamatsu M, Sattelle DB: Neonicotinoids show selective and diverse actions on their nicotinic receptor targets: electrophysiology, molecular biology, and receptor modeling studies. Biosci Biotechnol Biochem. 2005 Aug;69(8):1442-52. Neonicotinoid insecticides, which act selectively on insect nicotinic acetylcholine receptors (nAChRs), are used worldwide for insect pest management. Computational modeling of nAChR-imidacloprid interaction has assisted in the interpretation of these results. |
1(0,0,0,1) | Details |
| 11695184 | Tomizawa M, Casida JE: Structure and diversity of insect nicotinic acetylcholine receptors. . Pest Manag Sci. 2001 Oct;57(10):914-22. |
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 |
| 18790701 | Toshima K, Kanaoka S, Yamada A, Tarumoto K, Akamatsu M, Sattelle DB, Matsuda K: Combined roles of loops C and D in the interactions of a neonicotinoid insecticide imidacloprid with the alpha4beta2 nicotinic acetylcholine receptor. Neuropharmacology. 2009 Jan;56(1):264-72. Epub 2008 Aug 26. Neonicotinoid insecticides are widely used for crop protection based on their selective actions on insect nicotinic acetylcholine receptors (insect nAChRs). |
1(0,0,0,1) | Details |
| 18080902 | Abou-Donia MB, Goldstein LB, Bullman S, Tu T, Khan WA, Dechkovskaia AM, Abdel-Rahman AA: Imidacloprid induces neurobehavioral deficits and increases expression of glial fibrillary acidic protein in the motor cortex and hippocampus in offspring rats following in utero exposure. J Toxicol Environ Health A. 2008;71(2):119-30. On postnatal day (PND) 30, all male and female offspring were evaluated for (a) acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activity, (b) ligand binding for nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (m2 mAChR), (c) sensorimotor performance (inclined plane, beam-walking, and forepaw grip), and (d) pathological alterations in the brain (using cresyl violet and glial fibrillary acidic protein [GFAP] immunostaining). |
1(0,0,0,1) | Details |
| 16899070 | Brown LA, Ihara M, Buckingham SD, Matsuda K, Sattelle DB: Neonicotinoid insecticides display partial and super agonist actions on native insect nicotinic acetylcholine receptors. J Neurochem. 2006 Oct;99(2):608-15. Epub 2006 Aug 8. Here, we have used whole-cell patch-clamp recording of cholinergic neurons cultured from the central nervous system of 3rd instar Drosophila larvae to examine the actions of and as well as the neonicotinoids imidacloprid, clothianidin and P-CH-clothianidin on native nAChRs of these neurons. |
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 |
| 15937112 | Liu Z, Williamson MS, Lansdell SJ, Denholm I, Han Z, Millar NS: A nicotinic acetylcholine receptor mutation conferring target-site resistance to imidacloprid in Nilaparvata lugens (brown planthopper). Proc Natl Acad Sci U S A. 2005 Jun 14;102(24):8420-5. Epub 2005 Jun 3. |
112(1,2,2,2) | Details |
| 18004599 | Barbara GS, Grunewald B, Paute S, Gauthier M, Raymond-Delpech V: Study of nicotinic acetylcholine receptors on cultured antennal lobe neurones from adult honeybee brains. Invert Neurosci. 2008 Mar;8(1):19-29. Epub 2007 Nov 15. The classical nicotinic agonists and imidacloprid elicited respectively 45 and 43% of the maximum -induced currents. |
2(0,0,0,2) | Details |
| 18675908 | Yao X, Song F, Chen F, Zhang Y, Gu J, Liu S, Liu Z: Amino acids within loops D, E and F of insect nicotinic acetylcholine receptor beta subunits influence neonicotinoid selectivity. Insect Biochem Mol Biol. 2008 Sep;38(9):834-40. Epub 2008 Jul 15. Introduction of the insect-specific loops D, E and F, singly or together, into rat beta2 subunit resulted in a leftward shift of the imidacloprid dose-response curves for nAChRs Nlalpha1-beta2 chimeras, reflecting decreases in EC (50), compared to wildtype nAChRs Nlalpha1-beta2. |
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. To evaluate these moieties in neonicotinoid interactions with nicotinic AChR alpha subunits, the actions of imidacloprid and related compounds on the chicken alpha7, alpha4beta2 and Drosophila melanogaster-chicken hybrid (SADbeta2 and ALSbeta2) receptors expressed in Xenopus laevis oocytes were studied by voltage-clamp electrophysiology. |
2(0,0,0,2) | Details |
| 14561066 | Kiriyama K, Nishiwaki H, Nakagawa Y, Nishimura K: Insecticidal activity and nicotinic acetylcholine receptor binding of dinotefuran and its analogues in the housefly, Musca domestica. Pest Manag Sci. 2003 Oct;59(10):1093-100. Dinotefuran was less active than imidacloprid and clothianidin by a factor of 10 in molar concentrations. |
1(0,0,0,1) | Details |
| 15500966 | Zhang N, Tomizawa M, Casida JE: Drosophila nicotinic receptors: evidence for imidacloprid insecticide and alpha-bungarotoxin binding to distinct sites. Neurosci Lett. 2004 Nov 16;371(1):56-9. The principal mammalian brain nicotinic acetylcholine receptors (nAChRs) are the alpha-bungarotoxin (alpha-BGT)-insensitive alpha 4 beta 2 and the alpha-BGT-sensitive alpha 7 subtypes assayed with radiolabeled nicotinoids and alpha-BGT, respectively. |
1(0,0,0,1) | Details |
| 15182942 | Shimomura M, Yokota M, Matsuda K, Sattelle DB, Komai K: Roles of loop C and the loop B-C interval of the nicotinic receptor alpha subunit in its selective interactions with imidacloprid in insects. Neurosci Lett. 2004 Jun 17;363(3):195-8. The P242E mutation in loop C of the Drosophila SAD subunit (the second alpha-like Drosophila nicotinic acetylcholine receptor subunit, also called Dalpha2 subunit) reduced imidacloprid sensitivity of the SAD-chicken beta2 hybrid nAChR, whereas the E219P mutation of the alpha4 subunit increased the imidacloprid sensitivity of the alpha4beta2 nAChR. |
112(1,2,2,2) | Details |
| 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. |
93(0,3,3,3) | Details |
| 17854993 | Ihara M, Hirata K, Ishida C, Kagabu S, Matsuda K: Blocking actions of alkylene-tethered bis-neonicotinoids on nicotinic acetylcholine receptors expressed by terminal abdominal ganglion neurons of Periplaneta americana. Neurosci Lett. 2007 Oct 2;425(3):137-40. Epub 2007 Jul 5. Of the compounds tested, HK-13, which possesses two imidacloprid units linked with a hexamethylene bridge, had the highest antagonist potency. |
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. By contrast, the Q79E mutation scarcely influenced responses of the alpha7 nicotinic receptor to (-)- and desnitro-imidacloprid (DN-IMI), an imidacloprid derivative lacking the nitro group, whereas the Q79K and Q79R mutations reduced the sensitivity to these ligands. |
2(0,0,0,2) | Details |
| 11408603 | Courjaret R, Lapied B: Complex intracellular messenger pathways regulate one type of neuronal alpha-bungarotoxin-resistant nicotinic acetylcholine receptors expressed in insect neurosecretory cells (dorsal unpaired median neurons). Mol Pharmacol. 2001 Jul;60(1):80-91. Finally, we reported that phosphorylation/dephosphorylation of nAChR1 strongly affected the action of the widely used neonicotinoid insecticide imidacloprid. |
2(0,0,0,2) | Details |
| 19619141 | Liu Z, Cao G, Li J, Bao H, Zhang Y: Identification of two Lynx proteins in Nilaparvata lugens and the modulation on insect nicotinic acetylcholine receptors. J Neurochem. 2009 Sep;110(5):1707-14. Epub 2009 Jul 8. For example, Nl-lynx1 increased I (max) of and imidacloprid to 3.56-fold and 1.72-fold of that of Nlalpha1/beta2 alone, and these folds for Nl-lynx2 were 3.25 and 1.51. |
1(0,0,0,1) | Details |
| 15922528 | Proenca P, Teixeira H, Castanheira F, Pinheiro J, Monsanto PV, Marques EP, Vieira DN: Two fatal intoxication cases with imidacloprid: LC/MS analysis. Forensic Sci Int. 2005 Oct 4;153(1):75-80. It is the first highly effective insecticide that, like acts on the nervous system, causing blockage of postsynaptic nicotinergic acetylcholine receptors. |
1(0,0,0,1) | Details |
| 11464788 | Nauen R, Ebbinghaus-Kintscher U, Schmuck R: Toxicity and nicotinic acetylcholine receptor interaction of imidacloprid and its metabolites in Apis mellifera (Hymenoptera: Apidae). Pest Manag Sci. 2001 Jul;57(7):577-86. |
87(1,1,2,2) | 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. Thiamethoxam, a new neonicotinoid insecticide acting at nicotinic acetylcholine receptors, was characterized in competition binding assays with [3-H]-imidacloprid, a specific nicotinic ligand, using membranes from the aphids Aphis craccivora and Myzus persicae, and from the locust Locusta migratoria. |
82(1,1,1,2) | Details |
| 19046356 | Liu Z, Han Z, Zhang Y, Song F, Yao X, Liu S, Gu J, Millar NS: Heteromeric co-assembly of two insect nicotinic acetylcholine receptor alpha subunits: influence on sensitivity to neonicotinoid insecticides. J Neurochem. 2009 Jan;108(2):498-506. Epub 2008 Nov 19. Neonicotinoid insecticides, such as imidacloprid, are selective agonists of insect nicotinic acetylcholine receptors (nAChRs) and are used extensively in areas of crop protection and animal health to control a variety of insect pest species. |
82(1,1,1,2) | Details |
| 11698101 | Matsuda K, Buckingham SD, Kleier D, Rauh JJ, Grauso M, Sattelle DB: Neonicotinoids: insecticides acting on insect nicotinic acetylcholine receptors. Trends Pharmacol Sci. 2001 Nov;22(11):573-80. Imidacloprid is increasingly used worldwide as an insecticide. |
2(0,0,0,2) | Details |
| 14608492 | Raymond Delpech V, Ihara M, Coddou C, Matsuda K, Sattelle DB: Action of nereistoxin on recombinant neuronal nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes. Invert Neurosci. 2003 Nov;5(1):29-35. Epub 2003 Nov 8. Thus, the site of action on nicotinic AChRs of NTX, to which the insecticide Cartap is metabolised in insects, differs from that of the major nicotinic AChR-active insecticide, imidacloprid. |
2(0,0,0,2) | Details |
| 15770687 | Sattelle DB, Jones AK, Sattelle BM, Matsuda K, Reenan R, Biggin PC: Edit, cut and paste in the nicotinic acetylcholine receptor gene family of Drosophila melanogaster. Bioessays. 2005 Apr;27(4):366-76. |
1(0,0,0,1) | Details |
| 17156860 | Thany SH, Lenaers G, Raymond-Delpech V, Sattelle DB, Lapied B: Exploring the pharmacological properties of insect nicotinic acetylcholine receptors. Trends Pharmacol Sci. 2007 Jan;28(1):14-22. Epub 2006 Dec 6. Studies on insects resistant to the insecticide imidacloprid and on laboratory-generated hybrid and chimaeric nACh receptors in vitro have provided information about the molecular basis of receptor diversity, neonicotinoid resistance and selectivity. |
1(0,0,0,1) | Details |
| 10377228 | Latli B, D'Amour K, Casida JE: Novel and potent 6-chloro-3-pyridinyl ligands for the alpha4beta2 neuronal nicotinic acetylcholine receptor. J Med Chem. 1999 Jun 17;42(12):2227-34. 1-[(6-Chloro-3-pyridinyl) methyl]-2-imidazolidine (1), the N-desnitro metabolite of the major insecticide imidacloprid, is known to have similar potency to that of (-)- as an inhibitor of [3H](-)- binding at the rat recombinant alpha4beta2 neuronal nicotinic acetylcholine receptor (nAChR); IC50 values in the present study are 3.8 nM for (-)- 6.0 nM for 1, and 155 nM for imidacloprid. |
82(1,1,1,2) | Details |
| 9026029 | Latli B, Tomizawa M, Casida JE: Synthesis of a novel [125I] neonicotinoid photoaffinity probe for the Drosophila nicotinic acetylcholine receptor. Bioconjug Chem. 1997 Jan-Feb;8(1):7-14. The insect nicotinic acetylcholine receptor (nAChR) is the target for the major insecticide imidacloprid (IMI) and for the first candidate photoaffinity probe described here. |
82(1,1,1,2) | Details |
| 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 |
| 15963641 | Shimomura M, Satoh H, Yokota M, Ihara M, Matsuda K, Sattelle DB: Insect-vertebrate chimeric nicotinic acetylcholine receptors identify a region, loop B to the N-terminus of the Drosophila Dalpha2 subunit, which contributes to neonicotinoid sensitivity. Neurosci Lett. 2005 Sep 9;385(2):168-72. The actions of the neonicotinoid insecticide imidacloprid were examined. |
2(0,0,0,2) | Details |
| 12233176 | Nauen R, Stumpf N, Elbert A: Toxicological and mechanistic studies on neonicotinoid cross resistance in Q-type Bemisia tabaci (Hemiptera: Aleyrodidae). Pest Manag Sci. 2002 Sep;58(9):868-75. One of the latest group of insecticides introduced to the market were the neonicotinoids (chloronicotinyls), acting agonistically on insect nicotinic acetylcholine receptors. Our study revealed that neonicotinoid-resistant Q-type strains from Almeria were often more than 100-fold less susceptible to thiamethoxam, acetamiprid and imidacloprid when tested in discontinuous systemic laboratory bioassays. |
1(0,0,0,1) | Details |
| 10771176 | Huang Y, Williamson MS, Devonshire AL, Windass JD, Lansdell SJ, Millar NS: Cloning, heterologous expression and co-assembly of Mpbeta1, a nicotinic acetylcholine receptor subunit from the aphid Myzus persicae. Neurosci Lett. 2000 Apr 21;284(1-2):116-20. Nicotinic acetylcholine receptors (nAChRs) play a major role in excitatory synaptic transmission in insects and are also the target site for chloronicotinyl insecticides such as imidacloprid. |
1(0,0,0,1) | Details |
| 9453215 | Tomizawa M, Casida JE: [125I] Azidonicotinoid photoaffinity labeling of insecticide-binding subunit of Drosophila nicotinic acetylcholine receptor. Neurosci Lett. 1997 Nov 21;237(2-3):61-4. The novel synthetic nicotinoid insecticide imidacloprid is a high affinity ligand for the insect nicotinic acetylcholine receptor (nAChR). |
82(1,1,1,2) | Details |
| 11561406 | Nishiwaki H, Nakagawa Y, Ueno T, Kagabu S, Nishimura K: Insecticidal and binding activities of N3-substituted imidacloprid derivatives against the housefly Musca domestica and the alpha-bungarotoxin binding sites of nicotinic acetylcholine receptors. Pest Manag Sci. 2001 Sep;57(9):810-4. |
82(1,1,1,2) | Details |
| 19853623 | Bal R, Erdogan S, Theophilidis G, Baydas G, Naziroglu M: Assessing the effects of the neonicotinoid insecticide imidacloprid in the cholinergic synapses of the stellate cells of the mouse cochlear nucleus using whole-cell patch-clamp recording. Neurotoxicology. 2010 Jan;31(1):113-20. Epub 2009 Oct 22. Imidacloprid (IMI) is widely used systemic insecticide that acts as an agonist on nicotinic acetylcholine receptors (nAChRs). |
81(1,1,1,1) | Details |
| 16453147 | Jepson JE, Brown LA, Sattelle DB: The actions of the neonicotinoid imidacloprid on cholinergic neurons of Drosophila melanogaster. Invert Neurosci. 2006 Mar;6(1):33-40. Epub 2006 Feb 2. The neonicotinoid insecticide imidacloprid is an agonist on insect nicotinic acetylcholine receptors (nAChRs). |
81(1,1,1,1) | 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. |
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 |
| 20002807 | Yang B, Yao X, Gu S, Zhang Y, Liu Z, Zhang Y: Selectivity of lynx proteins on insect nicotinic acetylcholine receptors in the brown planthopper, Nilaparvata lugens. Insect Mol Biol. 2009 Dec 11. Nl-lynx1 and Nl-lynx2 increased I (max) (maximum responses) of to 4.85-fold and 2.40-fold of that of Nlalpha1/Nlalpha2/beta2 alone, and they also increased I (max ) of imidacloprid to 2.57-fold and 1.25-fold. |
2(0,0,0,2) | Details |
| 12759130 | Guez D, Belzunces LP, Maleszka R: Effects of imidacloprid metabolites on habituation in honeybees suggest the existence of two subtypes of nicotinic receptors differentially expressed during adult development. Pharmacol Biochem Behav. 2003 Apr;75(1):217-22. Here we tested our hypothesis that this effect is associated with a differential expression of two subtypes of nicotinic acetylcholine receptors (nAChRs). |
1(0,0,0,1) | Details |
| 15518655 | Salgado VL, Saar R: Desensitizing and non-desensitizing subtypes of alpha-bungarotoxin-sensitive nicotinic acetylcholine receptors in cockroach neurons. J Insect Physiol. 2004 Oct;50(10):867-79. Two alpha-bungarotoxin-sensitive nicotinic receptor subtypes in cockroach neurons are identified as desensitizing (nAChD), selectively inhibitable with 100 nM imidacloprid, and non-desensitizing (nAChN), selectively inhibitable with 100 pM methyllycaconitine. |
1(0,0,0,1) | 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 |
| 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 |
| 11673842 | Lambin M, Armengaud C, Raymond S, Gauthier M: Imidacloprid-induced facilitation of the proboscis extension reflex habituation in the honeybee. Arch Insect Biochem Physiol. 2001 Nov;48(3):129-34. Imidacloprid is a new insecticide from the family of the neonicotinoids, which interact with the insect nicotinic acetylcholine receptor. |
81(1,1,1,1) | Details |
| 19849723 | Xu X, Bao H, Shao X, Zhang Y, Yao X, Liu Z, Li Z: Pharmacological characterization of cis-nitromethylene neonicotinoids in relation to imidacloprid binding sites in the brown planthopper, Nilaparvata lugens. Insect Mol Biol. 2010 Feb;19(1):1-8. Epub 2009 Oct 22. Neonicotinoid insecticides, such as imidacloprid, are selective agonists of the insect nicotinic acetylcholine receptors (nAChRs) and extensively used in areas of crop protection and animal health to control a variety of insect pest species. |
81(1,1,1,1) | Details |
| 12639053 | Byrne FJ, Castle S, Prabhaker N, Toscano NC: Biochemical study of resistance to imidacloprid in B biotype Bemisia tabaci from Guatemala. Pest Manag Sci. 2003 Mar;59(3):347-52. Detoxification of imidacloprid by housefly MFOs may account for reports of lower toxicity of the insecticide towards this insect compared with whiteflies, despite similar binding properties between imidacloprid and the nicotinic acetylcholine receptors in both species. |
81(1,1,1,1) | Details |
| 8858952 | Tomizawa M, Latli B, Casida JE: Novel neonicotinoid-agarose affinity column for Drosophila and Musca nicotinic acetylcholine receptors. J Neurochem. 1996 Oct;67(4):1669-76. Neonicotinoids such as the insecticide imidacloprid (IMI) act as agonists at the insect nicotinic acetylcholine receptor (nAChR). |
81(1,1,1,1) | Details |
| 12696952 | Lee SJ, Tomizawa M, Casida JE: Nereistoxin and cartap neurotoxicity attributable to direct block of the insect nicotinic receptor/channel. J Agric Food Chem. 2003 Apr 23;51(9):2646-52. However, NTX and cartap are equally potent, direct-acting, and competitive displacers of [(3) H] thienylcyclohexylpiperidine binding at the noncompetitive blocker (NCB) site of the Apis nicotinic acetylcholine receptor (nAChR)/channel. NTX also binds at the Apis [(3) H] imidacloprid agonist site, but cartap does not. |
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| 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. A structure-activity study of the mode of [3H] imidacloprid displacement in Myzus persicae and Aphis craccivora.. Neonicotinoids bind selectively to insect nicotinic acetylcholine receptors with nanomolar affinity to act as potent insecticides. |
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| 18339894 | Amiri S, Shimomura M, Vijayan R, Nishiwaki H, Akamatsu M, Matsuda K, Jones AK, Sansom MS, Biggin PC, Sattelle DB: A role for Leu118 of loop E in agonist binding to the alpha 7 nicotinic acetylcholine receptor. Mol Pharmacol. 2008 Jun;73(6):1659-67. Epub 2008 Mar 13. The functional studies also demonstrated that residues at position 118 have a dramatic effect on the actions of imidacloprid (a partial agonist of wild-type alpha7 receptors) and its des-nitro derivative. |
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| 12370061 | Narahashi T: Nerve membrane ion channels as the target site of insecticides. Mini Rev Med Chem. 2002 Aug;2(4):419-32. However, the major target receptors are limited to channels, GABA receptors, and nicotinic acetylcholine receptors. Imidacloprid modulates nicotinic receptors in a complex manner. |
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| 17216517 | Jones AK, Brown LA, Sattelle DB: Insect nicotinic acetylcholine receptor gene families: from genetic model organism to vector, pest and beneficial species. Invert Neurosci. 2007 Mar;7(1):67-73. Epub 2007 Jan 11. Electrophysiological studies on cultured Drosophila cholinergic neurons show partial agonist actions of the neonicotinoid imidacloprid and super-agonist actions of another neonicotinoid, clothianidin, on native nAChRs. |
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| 14667058 | Zewen L, Zhaojun H, Yinchang W, Lingchun Z, Hongwei Z, Chengjun L: Selection for imidacloprid resistance in Nilaparvata lugens: cross-resistance patterns and possible mechanisms. Pest Manag Sci. 2003 Dec;59(12):1355-9. |
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| 16637697 | Honda H, Tomizawa M, Casida JE: Insect nicotinic acetylcholine receptors: neonicotinoid binding site specificity is usually but not always conserved with varied substituents and species. J Agric Food Chem. 2006 May 3;54(9):3365-71. The diversity of neonicotinoid insecticides acting as insect nicotinic receptor (nAChR) agonists is illustrated by imidacloprid (IMI) with chloropyridinylmethyl (CPM) and N-nitroimine substituents, dinotefuran (DIN) with tetrahydrofurylmethyl (TFM) and N-nitroimine moieties, and acetamiprid (ACE) with CPM and N-cyanoimine groups. |
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| 11515536 | Matsuda K, Ihara M, Nishimura K, Sattelle DB, Komai K: Insecticidal and neural activities of candidate photoaffinity probes for neonicotinoid binding sites. Biosci Biotechnol Biochem. 2001 Jul;65(7):1534-41. Photoreactive derivatives of imidacloprid and its nitromethylene analogue were synthesized as candidate photoaffinity probes for identifying the amino acid residues of nicotinic acetylcholine receptors (nAChRs) that interact with the neonicotinoid insecticides. |
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| 19627438 | Yixi Z, Liu Z, Han Z, Song F, Yao X, Shao Y, Li J, Millar NS: Functional co-expression of two insect nicotinic receptor subunits (Nlalpha3 and Nlalpha8) reveals the effects of a resistance-associated mutation (Nlalpha3) on neonicotinoid insecticides. J Neurochem. 2009 Sep;110(6):1855-62. Epub 2009 Jul 14. Neonicotinoid insecticides, such as imidacloprid, are selective agonists of insect nicotinic acetylcholine receptors (nAChRs) and are used extensively to control a variety of insect pest species. |
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| 16470540 | Miyagi S, Komaki I, Ozoe Y: Identification of a high-affinity binding site for dinotefuran in the nerve cord of the American cockroach. Pest Manag Sci. 2006 Apr;62(4):293-8. The binding of the neonicotinoid insecticide dinotefuran to insect nicotinic acetylcholine receptors (nAChRs) was examined by a centrifugation method using the nerve cord membranes of American cockroaches and [3H] dinotefuran (78 Ci mmol-1). Imidacloprid and nereistoxin displayed lower potencies than dinotefuran but higher potencies than epibatidine. |
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| 12565964 | Zhang N, Tomizawa M, Casida JE: 5-Azidoepibatidine: an exceptionally potent photoaffinity ligand for neuronal alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors. Bioorg Med Chem Lett. 2003 Feb 10;13(3):525-7. |
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| 14635178 | Rauch N, Nauen R: Identification of biochemical markers linked to neonicotinoid cross resistance in Bemisia tabaci (Hemiptera: Aleyrodidae). Arch Insect Biochem Physiol. 2003 Dec;54(4):165-76. Target site resistance to imidacloprid using [(3) H] imidacloprid in nicotinic acetylcholine receptor (nAChR) binding assays could not be detected in any of these highly resistant strains. |
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| 18824080 | Zhang Y, Liu S, Gu J, Song F, Yao X, Liu Z: Imidacloprid acts as an antagonist on insect nicotinic acetylcholine receptor containing the Y151M mutation. Neurosci Lett. 2008 Dec 3;446(2-3):97-100. |
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| 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). |
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| 20005950 | Li J, Shao Y, Ding Z, Bao H, Liu Z, Han Z, Millar NS: Native subunit composition of two insect nicotinic receptor subtypes with differing affinities for the insecticide imidacloprid. Insect Biochem Mol Biol. 2010 Jan;40(1):17-22. Epub 2009 Dec 30. Neonicotinoid insecticides, such as imidacloprid, are selective agonists of insect nicotinic acetylcholine receptors (nAChRs) and are used extensively to control a variety of insect pest species. |
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| 19916392 | Chin-Chen ML, Esteve-Romero J, Carda-Broch S: Determination of the insecticide imidacloprid in fruit juices using micellar high-performance liquid chromatography. J AOAC Int. 2009 Sep-Oct;92(5):1551-6. A simple and reliable HPLC method was developed to determine imidacloprid, a chloronicotinyl insecticide that has a highly specific affinity to the nicotinic acetylcholine receptor of insects, above its permissible limit of consumption in fruit juices (orange, apple, and a mixture of pineapple and pear). |
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| 9580620 | Nagata K, Song JH, Shono T, Narahashi T: Modulation of the neuronal nicotinic acetylcholine receptor-channel by the nitromethylene heterocycle imidacloprid. J Pharmacol Exp Ther. 1998 May;285(2):731-8. |
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| 19321668 | Matsuda K, Kanaoka S, Akamatsu M, Sattelle DB: Diverse actions and target-site selectivity of neonicotinoids: structural insights. Mol Pharmacol. 2009 Jul;76(1):1-10. Epub 2009 Mar 25. The nicotinic acetylcholine receptors (nAChRs) are targets for human and veterinary medicines as well as insecticides. The crystal structures showed that 1) in loop D, corresponding to the basic residues of insect nAChRs, bonds with the NO (2) group of imidacloprid and 2) neonicotinoid-unique stacking and CH-pi bonds at the LBD. |
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| 15481822 | Wellmann H, Gomes M, Lee C, Kayser H: Comparative analysis of neonicotinoid binding to insect membranes: II. Pest Manag Sci. 2004 Oct;60(10):959-70. Neonicotinoids represent a class of insect-selective ligands of nicotinic acetylcholine receptors. Imidacloprid, the first commercially used neonicotinoid insecticide, has been studied on neuronal preparations from many insects to date. |
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| 11281847 | Tonder JE, Olesen PH: Agonists at the alpha4beta2 nicotinic acetylcholine receptors: structure-activity relationships and molecular modelling. Curr Med Chem. 2001 May;8(6):651-74. In this review, the published nicotinic agonists are presented and, on the basis of the molecular structure, the compounds are divided into three compound classes, nicotinoids (structurally close to bicyclic compounds (structurally close to epibatidine and anatoxin-a), and analogues of imidacloprid (structurally close to the insecticide imidacloprid). On the basis of computational studies of ligands for the nicotinic acetylcholine receptors the structure-activity relationships are discussed and a possible binding mode suggested. |
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| 9326496 | Buckingham S, Lapied B, Corronc H, Sattelle F: Imidacloprid actions on insect neuronal acetylcholine receptors . J Exp Biol. 1997;200(Pt 21):2685-92. The neonicotinoid insecticide Imidacloprid acts at three pharmacologically distinct acetylcholine receptor (AChR) subtypes in the cockroach (Periplaneta americana) nervous system, but is ineffective on muscarinic receptors. |
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| 10386991 | Huang Y, Williamson MS, Devonshire AL, Windass JD, Lansdell SJ, Millar NS: Molecular characterization and imidacloprid selectivity of nicotinic acetylcholine receptor subunits from the peach-potato aphid Myzus persicae. J Neurochem. 1999 Jul;73(1):380-9. The recent introduction of the chloronicotinyl insecticide imidacloprid, targeting insect nicotinic acetylcholine receptors (nAChRs), emphasises the importance of a detailed molecular characterisation of these receptors. |
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| 14575878 | Shimomura M, Yokota M, Okumura M, Matsuda K, Akamatsu M, Sattelle DB, Komai K: Combinatorial mutations in loops D and F strongly influence responses of the alpha7 nicotinic acetylcholine receptor to imidacloprid. Brain Res. 2003 Nov 21;991(1-2):71-7. The nitro group of a neonicotinoid, imidacloprid, plays a key role in its selective actions on insect nicotinic acetylcholine receptors (nicotinic AChRs) and is postulated to bind close to residues Q79 in loop D and G189 in loop F of the chicken alpha7 nicotinic AChR. |
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| 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. |
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| 19371559 | Panigrahi AK, Subrahmanyam DK, Mukku KK: Imidacloprid poisoning: a case report. Am J Emerg Med. 2009 Feb;27(2):256.e5-6. Its effects are mediated through acetylcholine receptor blockade. |
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| 10431725 | Mehlhorn H, Mencke N, Hansen O: Effects of imidacloprid on adult and larval stages of the flea Ctenocephalides felis after in vivo and in vitro application: a light- and electron-microscopy study. Parasitol Res. 1999 Aug;85(8-9):625-37. The compound led to a continuous blockage of insect-specific nicotinic-acetylcholine receptors (nAChR), causing tetanic muscle cotractions within minutes of exposure. |
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| 18338186 | Ihara M, Okajima T, Yamashita A, Oda T, Hirata K, Nishiwaki H, Morimoto T, Akamatsu M, Ashikawa Y, Kuroda S, Mega R, Kuramitsu S, Sattelle DB, Matsuda K: Crystal structures of Lymnaea stagnalis AChBP in complex with neonicotinoid insecticides imidacloprid and clothianidin. Invert Neurosci. 2008 Jun;8(2):71-81. Epub 2008 Mar 13. Neonicotinoid insecticides, which act on nicotinic acetylcholine receptors (nAChRs) in a variety of ways, have extremely low mammalian toxicity, yet the molecular basis of such actions is poorly understood. |
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| 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. For receptor assay, either the Drosophila nAChR and [(3) H] imidacloprid or the alpha4 beta2 nicotinic receptor and [(3) H](-)- are added to determine changes in neo-nicotinoid potency. |
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| 16360954 | Bass C, Lansdell SJ, Millar NS, Schroeder I, Turberg A, Field LM, Williamson MS: Molecular characterisation of nicotinic acetylcholine receptor subunits from the cat flea, Ctenocephalides felis (Siphonaptera: Pulicidae). Insect Biochem Mol Biol. 2006 Jan;36(1):86-96. Epub 2005 Dec 1. As part of a program to monitor the susceptibility of cat flea populations to the insecticide imidacloprid we have examined the cat flea nicotinic acetylcholine receptor, the target site protein of the neonicotinoid group of insecticides. |
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| 11872245 | Deglise P, Grunewald B, Gauthier M: The insecticide imidacloprid is a partial agonist of the nicotinic receptor of honeybee Kenyon cells. Neurosci Lett. 2002 Mar 15;321(1-2):13-6. The main targets of the insecticide imidacloprid are neuronal nicotinic acetylcholine receptors (nAChRs) within the insect brain. |
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| 15532678 | Suchail S, De Sousa G, Rahmani R, Belzunces LP: In vivo distribution and metabolisation of 14C-imidacloprid in different compartments of Apis mellifera L. Pest Manag Sci. 2004 Nov;60(11):1056-62. The olefin derivative and 4/5--imidacloprid preferentially occurred in head, thorax and abdomen, which are nicotinic acetylcholine receptor-rich tissues. |
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| 11561413 | Grewal PS, Power KT, Shetlar DJ: Neonicotinoid insecticides alter diapause behavior and survival of overwintering white grubs (Coleoptera: Scarabaeidae). Pest Manag Sci. 2001 Sep;57(9):852-7. As both imidacloprid and thiamethoxam act on post-synaptic nicotinic acetylcholine receptors and modify insect behavior, we hypothesized that the two compounds will interfere with overwintering behavior of scarabs, thus reducing their ecological fitness and exposing them to increased winter mortality. |
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| 11695183 | Maienfisch P, Angst M, Brandl F, Fischer W, Hofer D, Kayser H, Kobel W, Rindlisbacher A, Senn R, Steinemann A, Widmer H: Chemistry and biology of thiamethoxam: a second generation neonicotinoid. Pest Manag Sci. 2001 Oct;57(10):906-13. Novel variations of the nitroimino-heterocycle of imidacloprid led to 4-nitroimino-1,3,5-oxadiazinanes exhibiting high insecticidal activity. Thiamethoxam acts by binding to nicotinic acetylcholine receptors. |
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| 11699773 | Suchail S, Guez D, Belzunces LP: Discrepancy between acute and chronic toxicity induced by imidacloprid and its metabolites in Apis mellifera. Environ Toxicol Chem. 2001 Nov;20(11):2482-6. As an agonist of the acetylcholine receptor, it attacks the insect nervous system and is extremely effective against various sucking and mining pests. |
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| 19473841 | Ohno I, Tomizawa M, Durkin KA, Casida JE, Kagabu S: Bis-neonicotinoid insecticides: Observed and predicted binding interactions with the nicotinic receptor. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3449-52. Epub 2009 May 9. The bis-pharmacophore approach applied to neonicotinoid insecticides reveals high binding affinity for heptamethylene bis-N (3),N (3')-imidacloprid fitting a nicotinic acetylcholine receptor model wherein the chloropyridine moieties contact loops E and F and the alkylene linker bridges these two distant domains. |
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| 12425057 | Ishaaya I, Kontsedalov S, Mazirov D, Horowitz AR: Biorational agents--mechanism and importance in IPM and IRM programs for controlling agricultural pests. Meded Rijksuniv Gent Fak Landbouwkd Toegep Biol Wet. 2001;66(2a):363-74. In addition, efforts have been made to develop compounds acting selectively on groups of insects by inhibiting or enhancing biochemical sites such as respiration (diafenthiuron), the nicotinyl acetylcholine receptors (imidacloprid and acetamiprid), the GABA receptors (avermectins), the salivary glands of sucking pests (pymetrozine) and others. |
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| 8804044 | Nagata K, Aistrup GL, Song JH, Narahashi T: Subconductance-state currents generated by imidacloprid at the nicotinic acetylcholine receptor in PC 12 cells. Neuroreport. 1996 Apr 10;7(5):1025-8. |
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| 16291090 | Tomizawa M, Millar NS, Casida JE: Pharmacological profiles of recombinant and native insect nicotinic acetylcholine receptors. Insect Biochem Mol Biol. 2005 Dec;35(12):1347-55. Epub 2005 Sep 15. Nicotinic acetylcholine receptors (nAChRs) are targets for insect-selective neonicotinoid insecticides exemplified by imidacloprid (IMI) and mammalian-selective nicotinoids including and epibatidine (EPI). |
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| 19583978 | Thany SH: Agonist actions of clothianidin on synaptic and extrasynaptic nicotinic acetylcholine receptors expressed on cockroach sixth abdominal ganglion. Neurotoxicology. 2009 Nov;30(6):1045-52. Epub 2009 Jul 5. Moreover, because clothianidin currents were blocked by d-tubocurarine and mecamylamine, we provided that clothianidin was an agonist of both nAChRs: imidacloprid-sensitive nAChR1 and -insensitive nAChR2 subtypes. Clothianidin is new neonicotinoid insecticide acting selectively on insect nicotinic acetylcholine receptors (nAChRs). |
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| 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 major nitroimine insecticide imidacloprid (IMI) and the nicotinic analgesics epibatidine and ABT-594 contain the 6-chloro-3-pyridinyl moiety important for high activity and/or selectivity. |
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| 8841090 | Narahashi T: Neuronal ion channels as the target sites of insecticides. Pharmacol Toxicol. 1996 Jul;79(1):1-14. Nitromethylene heterocycles including imidacloprid act on nicotinic acetylcholine receptors. |
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| 11150171 | Kagabu S, Maienfisch P, Zhang A, Granda-Minones J, Haettenschwiler J, Kayser H, Maetzke T, Casida JE: 5-Azidoimidacloprid and an acyclic analogue as candidate photoaffinity probes for mammalian and insect nicotinic acetylcholine receptors. J Med Chem. 2000 Dec 28;43(26):5003-9. The 5-azido analogue of the major insecticide imidacloprid, 1-(5-azido-6-chloropyridin-3-ylmethyl)-2-nitroiminoimidaz olidine (1), and an acyclic analogue, N-(5-azido-6-chloropyridin-3-ylmethyl)-N'-methyl-N' '-nitroguanidine (2), were prepared in good yields as candidate photoaffinity probes for mammalian and insect nicotinic acetylcholine receptors (nAChRs). |
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| 19818849 | Song F, You Z, Yao X, Cheng J, Liu Z, Lin K: Specific loops D, E and F of nicotinic acetylcholine receptor beta1 subunit may confer imidacloprid selectivity between Myzus persicae and its predatory enemy Pardosa pseudoannulata. Insect Biochem Mol Biol. 2009 Nov;39(11):833-41. Epub 2009 Oct 8. |
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| 9504393 | Matsuda K, Buckingham SD, Freeman JC, Squire MD, Baylis HA, Sattelle DB: Effects of the alpha subunit on imidacloprid sensitivity of recombinant nicotinic acetylcholine receptors. Br J Pharmacol. 1998 Feb;123(3):518-24. |
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| 16868180 | Shimomura M, Yokota M, Ihara M, Akamatsu M, Sattelle DB, Matsuda K: Role in the selectivity of neonicotinoids of insect-specific basic residues in loop D of the nicotinic acetylcholine receptor agonist binding site. Mol Pharmacol. 2006 Oct;70(4):1255-63. Epub 2006 Jul 25. The insecticide imidacloprid and structurally related neonicotinoids act selectively on insect nicotinic acetylcholine receptors (nAChRs). |
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| 19865835 | Liu GY, Ju XL, Cheng J: Selectivity of Imidacloprid for fruit fly versus rat nicotinic acetylcholine receptors by molecular modeling. J Mol Model. 2010 May;16(5):993-1002. Epub 2009 Oct 29. |
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| 11997976 | Kagabu S, Nishiwaki H, Sato K, Hibi M, Yamaoka N, Nakagawa Y: Nicotinic acetylcholine receptor binding of imidacloprid-related diaza compounds with various ring sizes and their insecticidal activity against Musca domestica. Pest Manag Sci. 2002 May;58(5):483-90. The binding activity of each compound to nicotinic acetylcholine receptor in vitro was measured using [125I] alpha-bungarotoxin. |
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