| Name | acetylcholine receptors (protein family or complex) |
|---|---|
| Synonyms | Acetylcholine receptor; Acetylcholine receptors |
| Name | anabasine |
|---|---|
| CAS |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 18187282 | Maciuk A, Moaddel R, Haginaka J, Wainer IW: Screening of tobacco smoke condensate for nicotinic acetylcholine receptor ligands using cellular membrane affinity chromatography columns and missing peak chromatography. J Pharm Biomed Anal. 2008 Sep 29;48(2):238-46. Epub 2007 Nov 26. Known strong ligands ((S)- (R,S)- N'-nitrosonornicotine), weak ligands ((R,S)- anabasine) as well as known non-ligands (1'S,2'S)- 1'-oxide) have been identified in the complex extract. |
2(0,0,0,2) | Details |
| 19223664 | Papke RL, Kem WR, Soti F, Lopez-Hernandez GY, Horenstein NA: Activation and desensitization of nicotinic alpha7-type acetylcholine receptors by benzylidene anabaseines and J Pharmacol Exp Ther. 2009 May;329(2):791-807. Epub 2009 Feb 17. |
2(0,0,0,2) | Details |
| 20116429 | Green BT, Lee ST, Panter KE, Welch KD, Cook D, Pfister JA, Kem WR: Actions of piperidine alkaloid teratogens at fetal nicotinic acetylcholine receptors. Neurotoxicol Teratol. 2010 Jan 29. A pharmacodynamic comparison of the alkaloids ammodendrine, anabasine, anabaseine, anagyrine, and coniine in SH-SY5Y cells and TE-671 cells was made. |
2(0,0,0,2) | Details |
| 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. |
2(0,0,0,2) | Details |
| 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. |
2(0,0,0,2) | Details |
| 17265057 | Ihara M, Shimomura M, Ishida C, Nishiwaki H, Akamatsu M, Sattelle DB, Matsuda K: A hypothesis to account for the selective and diverse actions of neonicotinoid insecticides at their molecular targets, nicotinic acetylcholine receptors: catch and release in bond networks. Invert Neurosci. 2007 Mar;7(1):47-51. Epub 2007 Jan 30. |
2(0,0,0,2) | 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. |
2(0,0,0,2) | Details |
| 19339660 | Williams DK, Stokes C, Horenstein NA, Papke RL: Differential regulation of receptor activation and agonist selectivity by highly conserved tryptophans in the nicotinic acetylcholine receptor binding site. J Pharmacol Exp Ther. 2009 Jul;330(1):40-53. Epub 2009 Apr 1. |
2(0,0,0,2) | Details |
| 12110318 | Sultana I, Ikeda I, Ozoe Y: Structure-activity relationships of benzylidene anabaseines in nicotinic acetylcholine receptors of cockroach nerve cords. Bioorg Med Chem. 2002 Sep;10(9):2963-71. |
2(0,0,0,2) | Details |
| 19696737 | Hibbs RE, Sulzenbacher G, Shi J, Talley TT, Conrod S, Kem WR, Taylor P, Marchot P, Bourne Y: Structural determinants for interaction of partial agonists with binding protein and neuronal alpha7 nicotinic acetylcholine receptor. EMBO J. 2009 Oct 7;28(19):3040-51. Epub 2009 Aug 20. |
2(0,0,0,2) | Details |
| 10771012 | Papke RL, Meyer E, Nutter T, Uteshev VV: alpha7 receptor-selective agonists and modes of alpha7 receptor activation. Eur J Pharmacol. 2000 Mar 30;393(1-3):179-95. Our results confirm that 4OH-GTS-21 is a potent activator of neuronal alpha7 nicotinic-acetylcholine receptor. |
1(0,0,0,1) | Details |
| 12611953 | Uteshev VV, Meyer EM, Papke RL: Regulation of neuronal function by and 4OH-GTS-21 through alpha 7 nicotinic receptors. J Neurophysiol. 2003 Apr;89(4):1797-806. Epub 2002 Dec 4. A unique feature of alpha7 nicotinic acetylcholine receptor physiology is that, under normal physiological conditions, alpha7 receptors are constantly perfused with their natural selective agonist, |
1(0,0,0,1) | Details |
| 12183330 | Papke RL, Porter Papke JK: Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis. Br J Pharmacol. 2002 Sep;137(1):49-61. Pharmacological studies of alpha7 nicotinic acetylcholine receptors are confounded by the fact that rapid desensitization to high agonist concentration causes alpha7 peak responses to occur well in advance of complete solution exchange. |
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. |
1(0,0,0,1) | Details |
| 8032906 | Brioni JD, Kim DJ, O'Neill AB, Williams JE, Decker MW: Clozapine attenuates the discriminative stimulus properties of (-)- Brain Res. 1994 Apr 18;643(1-2):1-9. The effect of neuronal nicotinic acetylcholine receptor (nAChR) agonists and antagonists were verified, and the participation of dopaminergic receptors subtypes in the expression of the (-)- cue was investigated with cis-flupentixol (D1-D2 antagonist), haloperidol (D2 antagonist) and clozapine (D4 antagonist). The stereoselectivity of the behavioral response was indicated by the 10-fold less sensitivity to (+)- in (-)--trained rats. (+/-)-Anabasine and (-)-cytisine exhibited partial agonist profiles at the 1.9 mumol/kg dose while (-)-lobeline was devoid of any effect in doses up to 19 mumol/kg. (-)-Lobeline did not show antagonist properties in this paradigm. |
1(0,0,0,1) | Details |
| 9873508 | Vernier JM, Holsenback H, Cosford ND, Whitten JP, Menzaghi F, Reid R, Rao TS, Sacaan AI, Lloyd GK, Suto CM, Chavez-Noriega LE, Washburn MS, Urrutia A, McDonald IA: Conformationally restricted analogues of and anabasine. . Bioorg Med Chem Lett. 1998 Aug 18;8(16):2173-8. A series of conformationally restricted analogues of has been synthesized and evaluated as agonists of neuronal acetylcholine receptors. |
1(0,0,0,1) | Details |
| 9864273 | Meyer EM, Kuryatov A, Gerzanich V, Lindstrom J, Papke RL: Analysis of 3-(4- 2-Methoxybenzylidene) anabaseine selectivity and activity at human and rat alpha-7 nicotinic receptors. J Pharmacol Exp Ther. 1998 Dec;287(3):918-25. Because this drug improves memory-related performance in nonhuman primates, and is presently in a clinical trial for Alzheimer's disease, we investigated the potential effects of its primary human metabolite, 3-(4- 2-methoxy-benzylidene) anabaseine) on human as well as rat nicotinic acetylcholine receptor. 4OH-GTS-21 exhibited a similar level of efficacy for both rat and human alpha-7 receptors expressed in Xenopus oocytes. |
1(0,0,0,1) | 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. |
1(0,0,0,1) | Details |
| 17189260 | Horenstein NA, McCormack TJ, Stokes C, Ren K, Papke RL: Reversal of agonist selectivity by mutations of conserved amino acids in the binding site of nicotinic acetylcholine receptors. J Biol Chem. 2007 Feb 23;282(8):5899-909. Epub 2006 Dec 21. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |
| 19778187 | Schep LJ, Slaughter RJ, Beasley DM: Nicotinic plant poisoning. Clin Toxicol. 2009 Sep;47(8):771-81. They contain the toxic alkaloids anabasine, cytisine, n-methylcytisine, coniine, n-methylconiine, and gamma-coniceine. The nicotinic-type acetylcholine receptor can vary both in its subunit composition and in its distribution within the body (the central and autonomic nervous systems, the neuromuscular junctions, and the adrenal medulla). |
1(0,0,0,1) | Details |
| 16398274 | El-Shazly AM, Dora G, Wink M: Alkaloids of Haloxylon salicornicum (Moq.) Bunge ex Boiss. (Chenopodiaceae). Pharmazie. 2005 Dec;60(12):949-52. A GLC/MS analysis revealed the presence of 17 additional known alkaloids of which piperidine, halosaline, anabasine, N-methyltyramine, haloxine and aldotripiperideine had been previously reported in this genus. Some of these alkaloids are known be strong agonists at nicotinic acetylcholine receptors and it is thus likely that they serve as chemical defencecompounds against insects and mammalian herbivores. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |
| 15519158 | Debnath B, Gayen S, Basu A, Ghosh B, Srikanth K, Jha T: Quantitative structure-activity relationship study using refractotopological state atom index on some neonicotinoid insecticides. Bioorg Med Chem. 2004 Dec 1;12(23):6137-45. This was used to identify the important atoms/fragments related to dispersive/van der Waals interactions of neonicotinoids with the nicotinic acetylcholine receptor (nAChR). |
1(0,0,0,1) | Details |
| 18363376 | Bhatti BS, Strachan JP, Breining SR, Miller CH, Tahiri P, Crooks PA, Deo N, Day CS, Caldwell WS: Synthesis of 2-(pyridin-3-yl)-1-azabicyclo [3.2.2] nonane, 2-(pyridin-3-yl)-1-azabicyclo [2.2.2] and 2-(pyridin-3-yl)-1-azabicyclo [3.2.1] a class of potent nicotinic acetylcholine receptor-ligands. J Org Chem. 2008 May 2;73(9):3497-507. Epub 2008 Mar 26. In an attempt to generate nicotinic acetylcholine receptor (nAChR) ligands selective for the alpha4beta2 and alpha7 subtype receptors we designed and synthesized constrained versions of anabasine, a naturally occurring nAChR ligand. 2-(Pyridin-3-yl)-1-azabicyclo [2.2.2] 2-(pyridin-3-yl)-1-azabicyclo [3.2.2] nonane, and several of their derivatives have been synthesized in both an enantioselective and a racemic manner utilizing the same basic synthetic approach. |
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| 9084060 | Tani Y, Saito K, Tsuneyoshi A, Imoto M, Ohno T: Nicotinic acetylcholine receptor (nACh-R) agonist-induced changes in brain monoamine turnover in mice. Psychopharmacology. 1997 Feb;129(3):225-32. The aim of the present study was to evaluate the effects of nicotinic acetylcholine receptor (nACh-R) agonists such as (-)- and related compounds on brain monoamine turnover. The changes in the monoamine turnover induced by (+/-)-anabasine were similar to those induced by (-)- while (-)-lobeline and (-)-cytisine had little effect, and 1,1-dimethyl-4-phenyl-piperazinium increased NA and turnover but not DA turnover at all doses tested. (S)-3-Methyl-5-(l-methyl-2- pyrrolidinyl) isoxazole (ABT-418), a selective neuronal nACh-R agonist, increased NA, DA and turnover, but had a weaker effect on DA turnover than NA and turnover. |
1(0,0,0,1) | Details |
| 19253973 | Ohno I, Tomizawa M, Durkin KA, Casida JE, Kagabu S: Neonicotinoid substituents forming a water bridge at the nicotinic acetylcholine receptor. J Agric Food Chem. 2009 Mar 25;57(6):2436-40. |
1(0,0,0,1) | Details |
| 14675945 | Debnath B, Gayen S, Naskar SK, Roy K, Jha T: Quantitative structure-activity relationship study on some azidopyridinyl neonicotinoid insecticides for their selective affinity towards the drosophila nicotinic receptor over mammalian alpha4beta2 receptor using electrotopological state atom index. Drug Des Discov. 2003;18(2-3):81-9. Fundamental differences between the nicotinic acetylcholine receptors (nAChRs) of insects and mammals confer remarkable selectivity of the neonicotinoids at insect nAChR over mammalian nAChR. |
1(0,0,0,1) | Details |
| 15265637 | Mastropaolo J, Rosse RB, Deutsch SI: Anabasine, a selective nicotinic acetylcholine receptor agonist, antagonizes MK-801-elicited mouse popping behavior, an animal model of schizophrenia. Behav Brain Res. 2004 Aug 31;153(2):419-22. |
66(0,2,2,6) | Details |
| 16266703 | Papke RL, McCormack TJ, Jack BA, Wang D, Bugaj-Gaweda B, Schiff HC, Buhr JD, Waber AJ, Stokes C: Rhesus monkey alpha7 nicotinic acetylcholine receptors: comparisons to human alpha7 receptors expressed in Xenopus oocytes. Eur J Pharmacol. 2005 Nov 7;524(1-3):11-8. Epub 2005 Nov 2. |
3(0,0,0,3) | Details |
| 19338581 | Arias HR, Xing H, Macdougall K, Blanton MP, Soti F, Kem WR: Interaction of benzylidene-anabaseine analogues with agonist and allosteric sites on muscle nicotinic acetylcholine receptors. Br J Pharmacol. 2009 May;157(2):320-30. Epub 2009 Mar 26. |
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. |
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