Unique pharmacology of heteromeric α7β2 nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes

European Journal of Pharmacology

Volumn 726, Issue 1, 2014, Pages 77-86

  Zwart, Ruud ^a   Strotton, Merrick ^a   Ching, Jennifer ^a   Astles, Peter C ^a   Sher, Emanuele ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

Heteromeric; Nicotinic acetylcholine receptor; Pharmacology; Voltage clamp; Xenopus oocyte

Indexed keywords

4 CHLORO N (3 QUINUCLIDINYL)BENZAMIDE; 4 [5,6 DIHYDRO (2,3' BIPYRIDIN) 3 (4H YLIDENE)METHYL] N,N IMETHYLBENZENAMINE DIHYDROCHLORIDE; ACETYLCHOLINE; BUNGAROTOXIN RECEPTOR; CARBACHOL; CHOLINE; CYTISINE; DIHYDRO BETA ERYTHROIDINE; EPIBATIDINE; EVP 6124; ISPRONICLINE; NICOTINE; NICOTINIC AGENT; NICOTINIC RECEPTOR; NICOTINIC RECEPTOR ALPHA7BETA2; POZANICLINE; SAZETIDINE A; SSR 108911; TC 1698; TC 5619; TC 7020; UNCLASSIFIED DRUG; VARENICLINE; [1 AZABICYCLO[2.2.2]OCT 3 YL (2 PYRIDYL)]THIOPHENE 2 CARBOXAMIDE; NICOTINIC RECEPTOR ALPHA4BETA2; NICOTINIC RECEPTOR BLOCKING AGENT;

ANIMAL CELL; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG SELECTIVITY; DRUG STRUCTURE; NONHUMAN; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; RECEPTOR BLOCKING; RECEPTOR UPREGULATION; XENOPUS LAEVIS; ANIMAL; CHEMISTRY; GENE EXPRESSION; GENETICS; METABOLISM; PROTEIN MULTIMERIZATION; PROTEIN QUATERNARY STRUCTURE; RAT;

ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR; ANIMALS; GENE EXPRESSION; NICOTINIC AGONISTS; NICOTINIC ANTAGONISTS; OOCYTES; PROTEIN MULTIMERIZATION; PROTEIN STRUCTURE, QUATERNARY; RATS; RECEPTORS, NICOTINIC; XENOPUS LAEVIS;

EID: 84893644657     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2014.01.031     Document Type: Article

References (36)

1. S.P. Arneric, M. Holladay, and M. Williams Neuronal nicotinic receptors: a perspective on two decades of drug discovery research Biochem. Pharmacol. 74 2007 1092 1101 (Pubitemid 47417924)
2. L. Azam, U. Winzer-Serhan, and F.M. Leslie Co-expression of α7 and β2 nicotinic acetylcholine receptor subunit mRNAs within rat brain cholinergic neurons Neuroscience 119 2003 965 977 (Pubitemid 36776447)
3. B. Biton, O.E. Bergis, F. Galli, A. Nedelec, A.W. Lochead, S. Jegham, D. Godet, C. Lanneau, R. Santamaria, F. Chesney, J. Leonardon, P. Granger, M.W. Debono, G.A. Bohme, F. Sgard, F. Besnard, D. Graham, A. Coste, A. Oblin, O. Curet, X. Vige, C. Voltz, L. Rouquier, J. Souilhac, V. Santucci, C. Gueudet, D. Francon, R. Steinberg, G. Griebel, F. Oury-Donat, P. George, P. Avenet, and B. Scatton. SSR180177, a novel selective α7 nicotinic receptor partial agonist: (I) binding and functional profile Neuropsychopharmacology 32 2007 1 16 (Pubitemid 44967780)
4. S. Couturier, D. Bertrand, J.M. Matter, M.C. Hernandez, S. Bertrand, N. Millar, S. Valera, T. Barkas, and M. Ballivet A neuronal nicotinic acetylcholine receptor subunit (alpha7) is developmentally regulated and forms a homo-oligomeric channel blocked by alpha-BTX Neuron 5 1990 847 856
5. M. Criado, L.M. Valor, J. Mulet, S. Gerber, S. Sala, and F. Sala Expression and functional properties of α7 acetylcholine nicotinic receptors are modified in the presence of other receptor subunits J. Neurochem. 123 2012 504 514
6. J.A. Dickinson, K.E. Hanrott, M.H.S. Mok, J.N.C. Kew, and S. Wonnacott Differential coupling of α7 and non-α7 nicotinic acetylcholine receptors to calcium-induced calcium release and voltage-operated calcium channels in PC12 cells J. Neurochem. 100 2007 1089 1096 (Pubitemid 46213931)
7. Flores, C.M., Rogers, S.W., Pabreza, L.A., Wolfe, B.B., Kellar, K.J., 1992. A subtype of nicotinic cholinergic receptors in rat brain is composed of α4 and β2 subunits and is upregulated by chronic nicotine treatment. Mol. Pharmacol. 41, 31-37.
8. R. Freedman α7-Nicotinic acetylcholine receptor agonists for cognitive enhancement in Schizophrenia Ann. Rev. Med. 65 2014 245 261
9. G.J. Gatto, G.A. Bohme, W.S. Caldwell, S.R. Letchworth, V.M. Traina, M.C. Obinu, M. Laville, M. Reibaud, L. Pradier, G. Dunbar, and M. Bencheriff TC-1734: an orally active neuronal nicotinic acetylcholine receptor modulator with antidepressant, neuroprotective and long-lasting cognitive effects CNS Drug Rev. 10 2004 147 166 (Pubitemid 38879108)
10. C. Gotti, and F. Clementi Neuronal nicotinic receptors: from structure to pathology Prog. Neurobiol. 74 2004 363 396 (Pubitemid 40092737)
11. T.A. Hauser, A. Kucinski, K.G. Jordan, G.J. Gatto, S.R. Wersinger, R.A. Hesse, E.K. Stachowiak, M.K. Stachowiak, R.L. Papke, P.M. Lippiello, and M. Bencherif TC-5619: an alpha7 neuronal nicotinic receptor-selective agonist that demonstrates efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia Biochem. Pharmacol. 78 2009 803 812
12. S.N. Haydar, and J. Dunlop Neuronal nicotinic acetylcholine receptors - targets for the development of drugs to treat cognitive impairment associated with schizophrenia and Alzheimer×s disease Curr. Top. Med. Chem. 10 2010 144 152
13. R. Hurst, H. Rollema, and D. Bertrand Nicotinic acetylcholine receptors: from basic science to therapeutics Pharmacol. Ther. 137 2013 22 54
14. A.A. Jensen, B. Frolund, T. Liljefors, and P. Krogsgaard-Larsen Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations J. Med. Chem. 48 2005 4705 4745 (Pubitemid 41038456)
15. S.S. Khiroug, P.C. Harkness, P.W. Lamb, S.N. Sudweeks, I. Khiroug, N.S. Millar, and J.L. Yakel Rat nicotinic acetylcholine receptor α7 and β2 subunits co-assemble to form functional heteromeric nicotinic receptor channels J. Physiol. 540 2002 425 434 (Pubitemid 35190121)
16. R. Lape, D. Colquhoun, and L.G. Sivilotti On the nature of partial agonism in the nicotinic receptor superfamily Nature 454 2008 722 727
17. J. Liu, L.F. Yu, J.B. Eaton, B. Caldarone, K. Cavino, C. Ruiz, M. Terry, A. Fedolak, D. Wang, A. Ghavami, D.A. Lowe, D. Brunner, R.J. Lukas, and A.P. Kozikowski Discovery of isoxazole analogs of Sazetidine-A as selective α4β2-nicotinic acetylcholine receptor partial agonists for the treatment of depression J. Med. Chem. 54 2011 7280 7288
18. Q. Liu, Y. Huang, J. Shen, S. Steffensen, and J. Wu Functional α7β2 nicotinic acetylcholine receptors expressed in hippocampal interneurons exhibit high sensitivity to pathological levels of amyloid β peptides BMC Neurosci. 13 2012 155 166
19. Q. Liu, Y. Huang, F. Xue, A. Simard, J. DeChon, G. Li, J. Zhang, L. Lucero, M. Wang, M. Sierks, G. Hu, Y. Chang, R.J. Lukas, and J. Wu A novel nicotinic acetylcholine receptor subtype in basal forebrain cholinergic neurons with high sensitivity to amyloid peptides J. Neurosci. 28 2009 918 929
20. M.B. Marrero, R. Lucas, C. Salet, T.A. Hauser, A. Mazurov, P.M. Lippiello, and M. Bencherif An α7 nicotinic acetylcholine receptor-selective agonist reduces weight gain and metabolic changes in a mouse model of diabetes J. Pharmacol. Exp. Ther. 332 2010 173 190
21. M.B. Marrero, R.L. Papke, B.S. Bhatti, S. Shaw, and M. Bencheriff The neuroprotective effect of 2-(3-pyridyl)-1-azabicyclo[3.2.2]nonane (TC-1698), a novel α7 ligand, is prevented through angiotensin II activation of a tyrosine phosphatase J. Pharmacol. Exp. Ther. 309 2003 16 27 (Pubitemid 38393109)
22. K.B. Mihalak, F.I. Carroll, and C.W. Luetje Varenicline is a partial agonist at α4β2 and a full agonist at α7 neuronal nicotinic receptors Mol. Pharmacol. 70 2006 801 805 (Pubitemid 44268437)
23. T.T. Money, E. Scarr, M. Udawela, A.S. Gibbons, W.J. Jeon, M.S. Seo, and B. Dean Treating schizophrenia: novel targets for the cholinergic system CNS Neurol. Disord. - Drug Targets 9 2010 241 256
24. T.A. Murray, D. Bertrand, R.L. Papke, A.A. George, R. Pantoja, R. Srinivsan, Q. Liu, J. Wu, P. Whiteaker, H.A. Lester, and R.J. Lukas α7β2 Nicotinic acetylcholine receptors assemble, function, and are activated primarily via their α7-α7 interfaces Mol. Pharmacol. 81 2012 175 188
25. E. Palma, L. Maggi, B. Barabino, F. Eusebi, and M. Ballivet Nicotinic acetylcholine receptors assembled from the α7 and β3 subunits J. Biol. Chem. 274 1999 18335 18340
26. M.R. Piciotto, B.J. Caldarone, D.H. Brunzell, V. Zachariou, T.R. Stevens, and S.L. King Neuronal nicotinic acetylcholine receptor subunit knockout mice: physiological and behavioral phenotypes and possible clinical implications Pharmacol. Ther. 92 2001 89 108 (Pubitemid 34251128)
27. J. Prickaerts, N.P. van Goethem, R. Chesworth, G. Shapiro, F.G. Boess, C. Methfessel, O.A.H. Reneerkens, D.G. Flood, D. Hilt, M. Gawryl, S. Bertrand, D. Bertrand, and G. Konig EVP-6124, a novel and selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors Neuropharmacology 62 2012 1099 1110
28. R.J. Radek, K.L. Kohlhaas, L.E. Rueter, and E.G. Mohler Treating the cognitive deficits of Schizophrenia with α4β2 neuronal nicotinic receptor agonists Curr. Pharm. Des. 16 2010 309 322
29. J.P. Sullivan, D. Donnelly-Roberts, C.A. Briggs, D.J. Anderson, M. Gopalakrishnan, I.C. Xue, M. Piattoni-Kaplan, E. Molinari, J.E. Campbell, D.G. McKenna, D.E. Gunn, N.H. Lin, K.B. Ryther, Y. He, M.W. Holladay, S. Wonnacott, M. Williams, and S.P. Arneric ABT-089 [2-Methyl-3-(2-(S)-pyrrolidinylmethoxy) pyridine]: I. A potent and selective cholinergic channel modulator with neuroprotective properties J. Pharmacol. Exp. Ther. 283 1997 235 246 (Pubitemid 27438967)
30. D.P. Walker, D.G. Wishka, D.W. Piotrowski, S. Jia, S.C. Reitz, K.M. Yates, J.K. Myers, T.N. Vetman, B.J. Margolis, E.J. Jacobsen, B.A. Acker, V.E. Groppi, M.L. Wolfe, B.A. Thornburgh, P.M. Tinholt, L.A. Cortes-Burgos, R.R. Walters, M.R. Hester, E.P. Seest, L.A. Dolak, F. Han, B.A. Olson, L. Fitzgerald, B.A. Staton, T.J. Raub, M. Hajos, W.E. Hoffmann, K.S. Li, N.R. Higdon, T.M. Wall, R.S. Hurst, E.H.F. Wong, and B.N. Rogers Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as α7 nicotinic acetylcholine receptor agonists Bioorg. Med. Chem. 14 2006 8219 8248 (Pubitemid 44667561)
31. T.L. Wallace, and D. Bertrand α7-Neuronal nicotinic receptors as a drug target in Schizophrenia Exp. Opin. Ther. Targets 17 2013 139 155
32. N.J. Woolf Cholinergic systems in mammalian brain and spinal cord Prog. Neurobiol. 37 1991 475 524
33. Y.X. Xiao, H. Fan, J.L. Musachio, Z.L. Wei, S.K. Chellappan, A.P. Kozikowski, and K.J. Kellar Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them Mol. Pharmacol. 70 2006 1454 1460 (Pubitemid 44435998)
34. R. Zwart, A.L. Carbone, M. Moroni, I. Bermudez, A.J. Mogg, E.A. Folly, L.M. Broad, A.C. Williams, D. Zhang, C. Ding, B.A. Heinz, and E. Sher Sazetidine-A is a potent and selective agonist at native and recombinant α4β2 nicotinic acetylcholine receptors Mol. Pharmacol. 73 2008 1838 1843 (Pubitemid 351724371)
35. R. Zwart, G. De Filippi, L.M. Broad, G.I. McPhie, K.H. Pearson, T. Baldwinson, and E. Sher 5-Hydroxyindole potentiates human α7 nicotinic receptor-mediated responses and enhances acetylcholine-induced glutamate release in cerebellar slices Neuropharmacology 43 2002 374 384 (Pubitemid 35257929)
36. R. Zwart, and H.P.M. Vijverberg Four pharmacologically distinct subtypes of α4β2 nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes Mol. Pharmacol. 54 1998 1124 1131 (Pubitemid 29002058)