Functional screening of α7 nicotinic receptor ligands

Expert Opinion on Drug Discovery

Volumn 3, Issue 6, 2008, Pages 623-628

  Dunlop, John ^a   Peri, Ravikumar ^a   Terstappen, Georg C ^b   Bowlby, Mark ^a  

^a PFIZER INC   (United States)

^b Siena Biotech SpA   (Italy)

Author keywords

Alpha 7; Ion channel; Ligand; Nicotinic

Indexed keywords

AGENTS INTERACTING WITH TRANSMITTER, HORMONE OR DRUG RECEPTORS; BUNGAROTOXIN RECEPTOR; BUNGAROTOXIN RECEPTOR AGONIST; ION CHANNEL; LIGAND; NICOTINE;

ALZHEIMER DISEASE; DRUG DESIGN; DRUG DETERMINATION; DRUG SCREENING; DRUG TARGETING; ELECTROPHYSIOLOGY; FLUORESCENCE; HUMAN; NONHUMAN; PRIORITY JOURNAL; REVIEW; SCHIZOPHRENIA;

EID: 45949109810     PISSN: 17460441     EISSN: None     Source Type: Journal    
DOI: 10.1517/17460441.3.6.623     Document Type: Review

References (47)

1. Lindstrom J. Neuronal nicotinic acetylcholine receptors. Ion Channels 1996;4:377-450
2. Dani J. Overview of nicotinic receptors and their roles in the central nervous system. Biological Psychiatry 2001;49(166-174)
3. Gotti C, Riganti L, Vailati S, Clementi F. Brain neuronal nicotinic receptors as new targets for drug discovery. Curr Pharm Des 2006;12(4):407-28
4. Freedman R, Hall M, Adler LE, Leonard S. Evidence in postmortem brain tissue for decreased numbers of hippocampal nicotinic receptors in schizophrenia. Biol Psychiatry 1995;38(1):22-33
5. Freedman R, Leonard S, Gault JM, et al. Linkage disequilibrium for schizophrenia at the chromosome 15q13-14 locus of the alpha7-nicotinic acetylcholine receptor subunit gene (CHRNA7). Am J Med Genet 2001;105(1):20-32
6. Kar S, Slowikowski SP, Westaway D, Mount HT. Interactions between beta-amyloid and central cholinergic neurons: implications for Alzheimer's disease. J Psychiatry Neurosci 2004;29(6):427-41
7. Shimohama S, Greenwald DL, Shafron DH, et al. Nicotinic alpha 7 receptors protect against glutamate neurotoxicity and neuronal ischemic damage. Brain Res 1998;779(1-2):359-63
8. Fucile S, Renzi M, Lax P, Eusebi F. Fractional Ca(2+) current through human neuronal alpha7 nicotinic acetylcholine receptors. Cell Calcium 2003;34(2):205-9
9. Castillo M, Mulet J, Gutierrez LM, et al. Dual role of the RIC-3 protein in trafficking of serotonin and nicotinic acetylcholine receptors. J Biol Chem 2005;280(29):27062-8
10. Williams ME, Burton B, Urrutia A, et al. Ric-3 promotes functional expression of the nicotinic acetylcholine receptor alpha7 subunit in mammalian cells. J Biol Chem 2005;280(2):1257-63
11. Lansdell SJ, Gee VJ, Harkness PC, et al. RIC-3 enhances functional expression of multiple nicotinic acetylcholine receptor subtypes in mammalian cells. Mol Pharmacol 2005;68(5):1431-8
12. Feucrbach D, Lingenhohl K, Dobbins P, et al. Coupling of human nicotinic acetylcholine receptors alpha 7 to calcium channels in GH3 cells. Neuropharmacology 2005;48(2):215-27
13. Roncarati R, Seredenina T, Jow B, et al. Functional properties of alpha7 nicotinic receptors coo-expressed with RIC-3 in a stable recombinant CHO-K1 cell line. Assay Drug Devel Technol 2008; In press
14. Dajas-Bailador FA, Mogg AJ, Wonnacott S. Intracellular Ca2+ signals evoked by stimulation of nicotinic acetylcholine receptors in SH-SY5Y cells: contribution of voltage-operated Ca2+ 1channels 1and Ca2+ stores. J Neurochem 2002;81(3):606-14
15. Dickinson JA, Hanrott KE, Mok MHS, et al. Differential coupling of alpha7 and non-alpha7 nicotinic acetylcholine receptors to calcium-induced calcium release and voltage-operated calcium channels in PC12 cells. J Neurochem 2007;100(4):1089-96
16. Sheppard BJ, Williams; M, Plummer HK, Schuller HM. Activation of voltage-operated Ca2+-channels in human small cell lung carcinoma by the tobacco-specific nitrosamine 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone. Int J Oncol 2000;16(3):513-8
17. Taylor SC, Peers C. Three distinct Ca(2+) influx pathways couple acetylcholine receptor activation to catecholamine secretion from PC12 cells. J Neurochem 2000;75(4):1583-9
18. Dunlop J, Roncarati R, Jow B, et al. In vitro screening strategies for nicotinic receptor ligands. Biochem Pharmacol 2007;74(8):1172-81
19. Gronlien JH, Hakerud M, Ween H, et al. Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes. Mol Pharmacol 2007;72(3):715-24
20. Bertrand D, Gopalakrishnan M. Allosteric modulation of nicotinic acetylcholine receptors. Biochem Pharmacol 2007;74(8):1155-63
21. Hurst RS, Hajos M, Raggenbass M, et al. A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neuroscience 2005;25(17):4396-405
22. Epps DE, Wolfe ML, Groppi V. Characterization of the steady-state and dynamic fluorescence properties of the potential-sensitive dye bis-(1,3-dibutylbarbituric add)trimethine oxonol (Dibac4(3)) in model systems and cells. Chem Physics Lipids 1994;69(2):137-50
23. Fitch RW, Xiao Y, Kellar KJ, Daly JW. Membrane potential fluorescence: a rapid and highly sensitive assay for nicotinic receptor channel function. Proceedings of the National Academy of Sciences of the United States of America. 2003;100(8):4909-14
24. Baxter DF, Kirk M, Garcia AF, et al. A novel membrane potential-sensitive fluorescent dye improves cell-based assays for ion channels. J Biomol Screening 2002;7(1):79-85
25. Wolff C, Fuks B, Chatelain P. Comparative study of membrane potential-sensitive fluorescent probes and their use in ion channel screening assays. J Biomol Screening 2003;8(5):533-43
26. Adkins CE, Pillai GV, Kerby J, et al. alpha4beta3delta GABA(A) receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. J Biological Chemistry 2001;276(42):38934-9
27. Faghih R, Gopalakrishnan M, Briggs CA. Allosteric modulators of the alpha7 nicotinic acetylcholine receptor. J Med Chem 2008;51(4):701-12
28. Ng HJ, Whittemore ER, Tran MB, et al. Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators. Proc Natl Acad Sci USA 2007;104(19):8059-64
29. Papke RL. Estimation of both the potency and efficacy of alpha7 nAChR agonists from single-concentration responses. Life Sci 2006;78(24):2812-9
30. Forman SA, Zhou Q. Novel modulation of a nicotinic receptor channel mutant reveals that the open state is stabilized by ethanol. Mol Pharmacol 1999;55(1):102-8
31. Bencherif M, Bane A, Miller C, et aL TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors. Eur J Pharmacol 2000;209:45-5
32. Bencherif M, Eisenhour C, Prince R, et al. The "Calcium Antagonist" TMB-8 [3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester] is a potent, non-competitive, functional antagonist at diverse nicotinic acetylcholine receptor subtypes. J Pharmacol Exp Ther 1995;275:1418-26
33. Bencherif M, Schmitt D, Bhatti B, et al. The heterocyclic substituted pyridine derivative (+)-2+3-pyridinyl)-1-azabicyclo[2.2.2] octane (RJR-2429): a selective ligand at nicotinic acetylcholine receptors. J Pharmacol Exp Ther 1997;284:886-94
34. Puttfarcken P, Manelli A, Americ S, Donnelly-Roberts D. Evidence for nicotinic receptors potentially modulating nociceptive transmission at the level of the primary sensory neuron: studies with F11 cells. J Neurochem 1997;69(3):930-8
35. Sullivan J, Decker M, Brioni J, et al. (+/-) Epibatidine elicits a diversity of in vitro and in vivo effects mediated by nicotinic acetylcholine receptors. J Pharmacol Exp Ther 1994;271:624-31
36. Arneric S, Sullivan J, Briggs C, et al. (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: 1. in vitro characterization. J Pharmacol Exp Ther 1994;270:310-8
37. Marks M, Farnham D, Grady S, Collins A. Nicotinic receptor function determined by stimulation of rubidium efflux from mouse brain synaptosomes. J Pharmacol Exp Ther 1993;264:542-52
38. Wood SC, Forman S, Miller K. Short chain and long chain alkanols have different sites of action on nicotine acetylocholine receptor channels from Torpedo. Mol Pharmacol 1990;39(3):332-8
39. Alifimoff J, Bugge B, Forman S, Miller K. Stereoselectivity of channel inhibition by secondary allcanol enantiomers at nicotinic acetylcholine receptors. Anesthesiology 1993;79(1):122-8
40. Daly JW, Nishizawa Y, Edwards M, et al. Nicotinic receptor-elicited sodium flux in rat pheochromocytoma PC12 cells: effects of agonists, antagonism, and noncompetitive blockers. Neurochem Res 1991;16(4):489-500
41. Daly Nishizawa Y, Padgett WL, et al. Dechydroquinoline alkaloids: noncompetitive blockers for nicotinic acetylocholine receptor-channels in pheochromocytoma cells and Torpedo electroplax. Neurochem Res 1991;16(11):1207-12
42. Nishizawa Seamon KB, Daly JW, Aronstam RS. Effects of forskolin and analogues on nicotinic receptor-mediated sodium flux, voltage-dependent calcium flux, and voltage-dependent rubidiu efflux in pheochromocytoma PC 12 cells. Cell Mol Neurobiol 1990;10(3):351-68
43. Tertsappen GC. Nonradioactive Rb+ efflux amy and its application in drug discovery and development. Assay Drug Dev Technol 2004;2:553-9
44. Fitch F, Daly J. Phosphorimaging detection and quantitation for isotopic ion flux assays. Anal Biochem 2005;342:260-70
45. Davies AR, Hardick DJ, Blagbrough IS, et al. Characterization of the binding of [3H] methyllycaconitine: a new radioligand for labelling alpha 7-type neuronal nicotinic acetylcholine receptors. Neuropharmacology 1999;38(5):679-90
46. Quik M, Choremis J, Komourian J, et al. Similarity between rat brain nicotinic alpha-bungarotoxin receptors and stably expressed alpha-bungarotoxin binding sites. J Neurochem 1996;67(1):145-54
47. Dunlop J, Bowlby M, Peri R, et al. High-throughput electrophysiology: an emerging paradigm for ion channel screening and physiology. Nat Rev Drug Discov 2008;7(4):358-68