α7 nicotinic ACh receptors as a ligand-gated source of Ca 2+ ions: The search for a Ca 2+ optimum

Advances in Experimental Medicine and Biology

Volumn 740, Issue , 2012, Pages 603-638

  Uteshev, Victor V ^a  

^a UNIVERSITY OF NORTH TEXAS   (United States)

Author keywords

7 nAChR; ACh; Alzheimer; Auditory; Ca 2+; Choline; Cognition; Cognitive; Dementia; Extrasynaptic; Gating; Ion channel; Neuroprotection; Neurotoxicity; Nicotinic; NMDA; Permeability; PNU 120596; Positive allosteric modulator; Receptor; Schizophrenia; Synaptic; Trauma

Indexed keywords

3 (2,4 DIMETHOXYBENZYLIDENE)ANABASEINE; 5 HYDROXYINDOLE; BUNGAROTOXIN RECEPTOR; CALCIUM CHANNEL; CALCIUM CHANNEL BLOCKING AGENT; CALCIUM ION; CHOLINE; DONEPEZIL; MEMANTINE; N METHYL DEXTRO ASPARTIC ACID; NICOTINE; NICOTINIC AGENT; PNU 120596; POSITIVE ALLOSTERIC MODULATOR; UNCLASSIFIED DRUG; VOLTAGE GATED CALCIUM CHANNEL;

AGING; ALZHEIMER DISEASE; ARTICLE; BINDING AFFINITY; BINDING SITE; BIOACCUMULATION; BRAIN REGION; CALCIUM CURRENT; CALCIUM SIGNALING; CELL FATE; CELL FUNCTION; CELL MEMBRANE PERMEABILITY; CELL STIMULATION; CELL SURVIVAL; CELL TRANSPORT; CYTOSOL; DEGENERATIVE DISEASE; DEMENTIA; DIARRHEA; DISEASE ASSOCIATION; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG POTENTIATION; DRUG RESPONSE; DRUG SAFETY; DRUG STRUCTURE; DRUG TARGETING; DRUG TOLERABILITY; HUMAN; IC 50; MOLECULAR DYNAMICS; MOLECULAR PATHOLOGY; NAUSEA; NERVE CELL NECROSIS; NEUROPROTECTION; NEUROTOXICITY; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN LOCALIZATION; RECEPTOR BINDING; RECEPTOR DOWN REGULATION; SCHIZOPHRENIA; SENSITIVITY ANALYSIS; TRAUMATIC BRAIN INJURY; VOMITING;

ALLOSTERIC REGULATION; ANIMALS; CALCIUM; CHOLINE; HUMANS; ISOXAZOLES; LIGANDS; PHENYLUREA COMPOUNDS; RECEPTORS, N-METHYL-D-ASPARTATE; RECEPTORS, NICOTINIC;

EID: 84859914196     PISSN: 00652598     EISSN: None     Source Type: Book Series    
DOI: 10.1007/978-94-007-2888-2_27     Document Type: Article

References (259)

1. Franklin JL, Johnson EM Jr (1992) Suppression of programmed neuronal death by sustained elevation of cytoplasmic calcium. Trends Neurosci 15:501-508
2. Freir DB, Herron CE (2003) Inhibition of L-type voltage dependent calcium channels causes impairment of long-term potentiation in the hippocampal CA1 region in vivo. Brain Res 967:27-36
3. Fu H, Li W, Lao Y, Luo J, Lee NT, Kan KK, Tsang HW, Tsim KW, Pang Y, Li Z, Chang DC, Li M, Han Y (2006) Bis(7)-tacrine attenuates beta amyloid-induced neuronal apoptosis by regulating L-type calcium channels. J Neurochem 98:1400-1410
4. Harkany T, Abraham I, Timmerman W, Laskay G, Toth B, Sasvari M, Konya C, Sebens JB, Korf J, Nyakas C, Zarandi M, Soos K, Penke B, Luiten PG (2000) Beta-amyloid neurotoxicity is mediated by a glutamate-triggered excitotoxic cascade in rat nucleus basalis. Eur J Neurosci 12:2735-2745
5. Ikonomidou C, Stefovska V, Turski L (2000) Neuronal death enhanced by N-methyl-Daspartate antagonists. Proc Natl Acad Sci USA 97:12885-12890
6. Lopez JR, Lyckman A, Oddo S, Laferla FM, Querfurth HW, Shtifman A (2008) Increased intraneuronal resting [Ca2+] in adult Alzheimer's disease mice. J Neurochem 105:262-271
7. Mattson MP (1990) Antigenic changes similar to those seen in neurofi brillary tangles are elicited by glutamate and Ca2+ influx in cultured hippocampal neurons. Neuron 4: 105-117
8. Nimmrich V, Grimm C, Draguhn A, Barghorn S, Lehmann A, Schoemaker H, Hillen H, Gross G, Ebert U, Bruehl C (2008) Amyloid beta oligomers (A beta(1-42) globulomer) suppress spontaneous synaptic activity by inhibition of P/Q-type calcium currents. J Neurosci 28:788-797
9. Papadia S, Hardingham GE (2007) The dichotomy of NMDA receptor signaling. Neuroscientist 13:572-579
10. Pierrot N, Ghisdal P, Caumont AS, Octave JN (2004) Intraneuronal amyloid-beta1-42 production triggered by sustained increase of cytosolic calcium concentration induces neuronal death. J Neurochem 88:1140-1150
11. Scragg JL, Fearon IM, Boyle JP, Ball SG, Varadi G, Peers C (2005) Alzheimer's amyloid peptides mediate hypoxic up-regulation of L-type Ca2+ channels. FASEB J 19:150-152
12. Bezprozvanny I, Mattson MP (2008) Neuronal calcium mishandling and the pathogenesis of Alzheimer's disease. Trends Neurosci 31:454-463
13. Davare MA, Hell JW (2003) Increased phosphorylation of the neuronal L-type Ca(2+) channel Ca(v)1.2 during aging. Proc Natl Acad Sci USA 100:16018-16023
14. Thibault O, Hadley R, Landfield PW (2001) Elevated postsynaptic [Ca2+]i and L-type calcium channel activity in aged hippocampal neurons: relationship to impaired synaptic plasticity. J Neurosci 21:9744-9756
15. Thibault O, Landfield PW (1996) Increase in single L-type calcium channels in hippocampal neurons during aging. Science 272:1017-1020
16. Ueda K, Shinohara S, Yagami T, Asakura K, Kawasaki K (1997) Amyloid beta protein potentiates Ca2+ influx through L-type voltage-sensitive Ca2+ channels: a possible involvement of free radicals. J Neurochem 68:265-271
17. Weiss JH, Pike CJ, Cotman CW (1994) Ca2+ channel blockers attenuate beta-amyloid peptide toxicity to cortical neurons in culture. J Neurochem 62:372-375
18. Akaike A, Tamura Y, Yokota T, Shimohama S, Kimura J (1994) Nicotine-induced protection of cultured cortical neurons against N-methyl-D-aspartate receptor-mediated glutamate cytotoxicity. Brain Res 644:181-187
19. Bok J, Wang Q, Huang J, Green SH (2007) CaMKII and CaMKIV mediate distinct prosurvival signaling pathways in response to depolarization in neurons. Mol Cell Neurosci 36:13-26
20. Collins F, Schmidt MF, Guthrie PB, Kater SB (1991) Sustained increase in intracellular calcium promotes neuronal survival. J Neurosci 11:2582-2587
21. Egea J, Rosa AO, Sobrado M, Gandia L, Lopez MG, Garcia AG (2007) Neuroprotection afforded by nicotine against oxygen and glucose deprivation in hippocampal slices is lost in alpha7 nicotinic receptor knockout mice. Neuroscience 145:866-872
22. Franklin JL, Johnson EM (1998) Control of neuronal size homeostasis by trophic factormediated coupling of protein degradation to protein synthesis. J Cell Biol 142:1313-1324
23. Kihara T, Shimohama S, Sawada H, Kimura J, Kume T, Kochiyama H, Maeda T, Akaike A (1997) Nicotinic receptor stimulation protects neurons against beta-amyloid toxicity. Ann Neurol 42:159-163
24. Koike T, Martin DP, Johnson EM Jr (1989) Role of Ca2+ channels in the ability of membrane depolarization to prevent neuronal death induced by trophic-factor deprivation: evidence that levels of internal Ca2+ determine nerve growth factor dependence of sympathetic ganglion cells. Proc Natl Acad Sci USA 86:6421-6425
25. Li Y, Papke RL, He YJ, Millard WJ, Meyer EM (1999) Characterization of the neuroprotective and toxic effects of alpha7 nicotinic receptor activation in PC12 cells. Brain Res 830:218-225
26. Shimohama S, Greenwald DL, Shafron DH, Akaike A, Maeda T, Kaneko S, Kimura J, Simpkins CE, Day AL, Meyer EM (1998) Nicotinic à7 receptors protect against glutamate neurotoxicity and neuronal ischemic damage. Brain Res 779:359-363
27. Shimohama S, Kihara T (2001) Nicotinic receptor-mediated protection against beta-amyloid neurotoxicity. Biol Psychiatry 49:233-239
28. Vaillant AR, Mazzoni I, Tudan C, Boudreau M, Kaplan DR, Miller FD (1999) Depolarization and neurotrophins converge on the phosphatidylinositol 3-kinase-Akt pathway to synergistically regulate neuronal survival. J Cell Biol 146:955-966
29. Sarkar SN, Huang RQ, Logan SM, Yi KD, Dillon GH, Simpkins JW (2008) Estrogens directly potentiate neuronal L-type Ca2+ channels. Proc Natl Acad Sci USA 105:15148-15153
30. Blair LA, Bence-Hanulec KK, Mehta S, Franke T, Kaplan D, Marshall J (1999) Aktdependent potentiation of L channels by insulin-like growth factor-1 is required for neuronal survival. J Neurosci 19:1940-1951
31. Smith CC, McMahon LL (2006) Estradiol-induced increase in the magnitude of long-term potentiation is prevented by blocking NR2B-containing receptors. J Neurosci 26:8517-8522
32. Hurst RS, Hajos M, Raggenbass M, Wall TM, Higdon NR, Lawson JA, Rutherford-Root KL, Berkenpas MB, Hoffmann WE, Piotrowski DW, Groppi VE, Allaman G, Ogier R, Bertrand S, Bertrand D, Arneric SP (2005) A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci 25:4396-4405
33. Timmermann DB, Gronlien JH, Kohlhaas KL, Nielsen EO, Dam E, Jorgensen TD, Ahring PK, Peters D, Holst D, Christensen JK, Malysz J, Briggs CA, Gopalakrishnan M, Olsen GM (2007) An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J Pharmacol Exp Ther 323:294-307
34. Gusev AG, Uteshev VV (2010) Physiological concentrations of choline activate native alpha7-containing nicotinic acetylcholine receptors in the presence of PNU-120596 [1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3- yl)-urea]. J Pharmacol Exp Ther 332:588-598
35. Kalappa BI, Gusev AG, Uteshev VV (2010) Activation of functional alpha7-containing nAChRs in hippocampal CA1 pyramidal neurons by physiological levels of choline in the presence of PNU-120596. PLoS One 5:e13964
36. Malysz J, Gronlien JH, Anderson DJ, Hakerud M, Thorin-Hagene K, Ween H, Wetterstrand C, Briggs CA, Faghih R, Bunnelle WH, Gopalakrishnan M (2009) In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl- 1H-pyrrol-1-yl)benzenesulfonami de (A-867744), exhibiting unique pharmacological profile. J Pharmacol Exp Ther 330:257-267
37. Dinklo T, Shaban H, Thuring JW, Lavreysen H, Stevens KE, Zheng L, Mackie C, Grantham C, Vandenberk I, Meulders G, Peeters L, Verachtert H, De Prins E, Lesage AS (2011) Characterization of 2-[[4-fl uoro-3-(trifl uoromethyl)phenyl] amino]-4-(4-pyridinyl)-5-thiazoleme thanol (JNJ-1930942), a novel positive allosteric modulator of the {alpha}7 nicotinic acetylcholine receptor. J Pharmacol Exp Ther 336:560-574
38. Choi DW (1988) Calcium-mediated neurotoxicity: relationship to specific channel types and role in ischemic damage. Trends Neurosci 11:465-469
39. Mennerick S, Zorumski CF (2000) Neural activity and survival in the developing nervous system. Mol Neurobiol 22:41-54
40. Tymianski M, Charlton MP, Carlen PL, Tator CH (1993) Source specificity of early calcium neurotoxicity in cultured embryonic spinal neurons. J Neurosci 13:2085-2104
41. Brandt SK, Weatherly ME, Ware L, Linn DM, Linn CL (2011) Calcium preconditioning triggers neuroprotection in retinal ganglion cells. Neuroscience 172:387-397
42. Soriano FX, Papadia S, Hofmann F, Hardingham NR, Bading H, Hardingham GE (2006) Preconditioning doses of NMDA promote neuroprotection by enhancing neuronal excitability. J Neurosci 26:4509-4518
43. Asomugha CO, Linn DM, Linn CL (2010) ACh receptors link two signaling pathways to neuroprotection against glutamate-induced excitotoxicity in isolated RGCs. J Neurochem 112:214-226
44. Ogita K, Okuda H, Yamamoto Y, Nishiyama N, Yoneda Y (2003) In vivo neuroprotective role of NMDA receptors against kainate-induced excitotoxicity in murine hippocampal pyramidal neurons. J Neurochem 85:1336-1346
45. Nakazawa H, Murphy TH (1999) Activation of nuclear calcium dynamics by synaptic stimulation in cultured cortical neurons. J Neurochem 73:1075-1083
46. Hardingham GE, Arnold FJ, Bading H (2001) A calcium microdomain near NMDA receptors: on switch for ERK-dependent synapse-to-nucleus communication. Nat Neurosci 4:565-566
47. Pokorska A, Vanhoutte P, Arnold FJ, Silvagno F, Hardingham GE, Bading H (2003) Synaptic activity induces signalling to CREB without increasing global levels of cAMP in hippocampal neurons. J Neurochem 84:447-452
48. Uteshev VV, Knot HJ (2005) Somatic Ca(2+) dynamics in response to choline-mediated excitation in histaminergic tuberomammillary neurons. Neuroscience 134:133-143
49. Papadia S, Soriano FX, Leveille F, Martel MA, Dakin KA, Hansen HH, Kaindl A, Sifringer M, Fowler J, Stefovska V, McKenzie G, Craigon M, Corriveau R, Ghazal P, Horsburgh K, Yankner BA, Wyllie DJ, Ikonomidou C, Hardingham GE (2008) Synaptic NMDA receptor activity boosts intrinsic antioxidant defenses. Nat Neurosci 11:476-487
50. Hardingham GE, Bading H (2010) Synaptic versus extrasynaptic NMDA receptor signalling: implications for neurodegenerative disorders. Nat Rev Neurosci 11:682-696
51. Hardingham GE, Bading H (2003) The Yin and Yang of NMDA receptor signalling. Trends Neurosci 26:81-89
52. Tovar KR, Westbrook GL (2002) Mobile NMDA receptors at hippocampal synapses. Neuron 34:255-264
53. Borgdorff AJ, Choquet D (2002) Regulation of AMPA receptor lateral movements. Nature 417:649-653
54. Fernandes CC, Berg DK, Gomez-Varela D (2010) Lateral mobility of nicotinic acetylcholine receptors on neurons is determined by receptor composition, local domain, and cell type. J Neurosci 30:8841-8851
55. Okubo Y, Sekiya H, Namiki S, Sakamoto H, Iinuma S, Yamasaki M, Watanabe M, Hirose K, Iino M (2010) Imaging extrasynaptic glutamate dynamics in the brain. Proc Natl Acad Sci USA 107:6526-6531
56. Uteshev VV, Pennefather PS (1997) Analytical description of the activation of multi-state receptors by continuous neurotransmitter signals at brain synapses. Biophys J 72:1127-1134
57. Rusakov DA, Wuerz A, Kullmann DM (2004) Heterogeneity and specificity of presynaptic Ca2+ current modulation by mGluRs at individual hippocampal synapses. Cereb Cortex 14:748-758
58. Zheng K, Scimemi A, Rusakov DA (2008) Receptor actions of synaptically released glutamate: the role of transporters on the scale from nanometers to microns. Biophys J 95:4584-4596
59. Asztely F, Erdemli G, Kullmann DM (1997) Extrasynaptic glutamate spillover in the hippocampus: dependence on temperature and the role of active glutamate uptake. Neuron 18: 281-293
60. Kullmann DM (2000) Spillover and synaptic cross talk mediated by glutamate and GABA in the mammalian brain. Prog Brain Res 125:339-351
61. Uteshev VV, Pennefather PS (1996) A mathematical description of miniature postsynaptic current generation at central nervous system synapses. Biophys J 71:1256-1266
62. Traynelis SF, Wollmuth LP, McBain CJ, Menniti FS, Vance KM, Ogden KK, Hansen KB, Yuan H, Myers SJ, Dingledine R (2010) Glutamate receptor ion channels: structure, regulation, and function. Pharmacol Rev 62:405-496
63. Lester RA, Jahr CE (1992) NMDA channel behavior depends on agonist affi nity. J Neurosci 12:635-643
64. Clements AM, Westbrook GL (1991) Activation kinetics reveal the number of glutamate and glycine binding sites on the N -methyl-D-aspartate receptor. Neuron 7:605-613
65. Herman MA, Jahr CE (2007) Extracellular glutamate concentration in hippocampal slice. J Neurosci 27:9736-9741
66. Rossi DJ, Oshima T, Attwell D (2000) Glutamate release in severe brain ischaemia is mainly by reversed uptake. Nature 403:316-321
67. Camacho A, Massieu L (2006) Role of glutamate transporters in the clearance and release of glutamate during ischemia and its relation to neuronal death. Arch Med Res 37:11-18
68. Groc L, Heine M, Cousins SL, Stephenson FA, Lounis B, Cognet L, Choquet D (2006) NMDA receptor surface mobility depends on NR2A-2B subunits. Proc Natl Acad Sci USA 103:18769-18774
69. Groc L, Bard L, Choquet D (2009) Surface Trafficking of N-methyl-D-aspartate receptors: physiological and pathological perspectives. Neuroscience 158:4-18
70. Lipton SA (2007) Pathologically activated therapeutics for neuroprotection. Nat Rev Neurosci 8:803-808
71. Chen HS, Pellegrini JW, Aggarwal SK, Lei SZ, Warach S, Jensen FE, Lipton SA (1992) Open-channel block of N-methyl-D-aspartate (NMDA) responses by memantine: therapeutic advantage against NMDA receptor-mediated neurotoxicity. J Neurosci 12:4427-4436
72. Aracava Y, Pereira EF, Maelicke A, Albuquerque EX (2005) Memantine blocks alpha7*nicotinic acetylcholine receptors more potently than n-methyl-D-aspartate receptors in rat hippocampal neurons. J Pharmacol Exp Ther 312:1195-1205
73. Maskell PD, Speder P, Newberry NR, Bermudez I (2003) Inhibition of human alpha 7 nicotinic acetylcholine receptors by open channel blockers of N-methyl-D-aspartate receptors. Br J Pharmacol 140:1313-1319
74. Kotermanski SE, Johnson JW (2009) Mg2+ imparts NMDA receptor subtype selectivity to the Alzheimer's drug memantine. J Neurosci 29:2774-2779
75. Aarsland D, Ballard C, Walker Z, Bostrom F, Alves G, Kossakowski K, Leroi I, Pozo-Rodriguez F, Minthon L, Londos E (2009) Memantine in patients with Parkinson's disease dementia or dementia with Lewy bodies: a double-blind, placebo-controlled, multicentre trial. Lancet Neurol 8:613-618
76. Atri A, Shaughnessy LW, Locascio JJ, Growdon JH (2008) Long-term course and effectiveness of combination therapy in Alzheimer disease. Alzheimer Dis Assoc Disord 22:209-221
77. Leroi I, Overshott R, Byrne EJ, Daniel E, Burns A (2009) Randomized controlled trial of memantine in dementia associated with Parkinson's disease. Mov Disord 24:1217-1221
78. Levin OS, Batukaeva LA, Smolentseva IG, Amosova NA (2009) Efficacy and safety of memantine in Lewy body dementia. Neurosci Behav Physiol 39:597-604
79. Parsons CG, Danysz W, Quack G (1999) Memantine is a clinically well tolerated N-methyl-D-aspartate (NMDA) receptor antagonist-a review of preclinical data. Neuropharmacology 38:735-767
80. Plosker GL, Lyseng-Williamson KA (2005) Memantine: a pharmacoeconomic review of its use in moderate-to-severe Alzheimer's disease. Pharmacoeconomics 23:193-206
81. Reisberg B, Doody R, Stoffl er A, Schmitt F, Ferris S, Mobius HJ (2003) Memantine in moderate-to-severe Alzheimer's disease. N Engl J Med 348:1333-1341
82. Creeley CE, Wozniak DF, Nardi A, Farber NB, Olney JW (2008) Donepezil markedly potentiates memantine neurotoxicity in the adult rat brain. Neurobiol Aging 29:153-167
83. Schugens MM, Egerter R, Daum I, Schepelmann K, Klockgether T, Loschmann PA (1997) The NMDA antagonist memantine impairs classical eyeblink conditioning in humans. Neurosci Lett 224:57-60
84. Swerdlow NR, van Bergeijk DP, Bergsma F, Weber E, Talledo J (2009) The effects of memantine on prepulse inhibition. Neuropsychopharmacology 34:1854-1864
85. Vercelletto M , Boutoleau-Bretonniere C, Volteau C, Puel M, Auriacombe S, Sarazin M, Michel BF, Couratier P, Thomas-Anterion C, Verpillat P, Gabelle A, Golfi er V, Cerato E, Lacomblez L (2011) Memantine in behavioral variant frontotemporal dementia: negative results. J Alzheimers Dis 23:749-759
86. Schneider LS, Insel PS, Weiner MW (2011) Treatment with cholinesterase inhibitors and memantine of patients in the Alzheimer's Disease neuroimaging initiative. Arch Neurol 68:58-66
87. Aarts M, Liu Y, Liu L, Besshoh S, Arundine M, Gurd JW, Wang YT, Salter MW, Tymianski M (2002) Treatment of ischemic brain damage by perturbing NMDA receptor-PSD-95 protein interactions. Science 298:846-850
88. Hogg RC, Raggenbass M, Bertrand D (2003) Nicotinic acetylcholine receptors: from structure to brain function. Rev Physiol Biochem Pharmacol 147:1-46
89. Corringer PJ, Le Novere N, Changeux JP (2000) Nicotinic receptors at the amino acid level. Annu Rev Pharmacol Toxicol 40:431-458
90. Castro NG, Albuquerque EX (1995) à-Bungarotoxin-sensitive hippocampal nicotinic receptor channel has a high calcium permeability. Biophys J 68:516-524
91. Fucile S (2004) Ca2+ permeability of nicotinic acetylcholine receptors. Cell Calcium 35:1-8
92. Seguela P, Wadiche J, Dinely-Miller K, Dani JA, Patrick JW (1993) Molecular cloning, functional properties and distribution of rat brain alpha 7: a nicotinic cation channel highly permeable to calcium. J Neurosci 13(2):596-604
93. Sands SB, Costa ACS, Patrick JW (1993) Barium permeability of neuronal nicotinic acetylcholine receptor alpha 7 expressed in Xenopus oocytes. Biophys J 65:2614-2621
94. Vernino S, Amador M, Luetje CW, Patrick J, Dani JA (1992) Calcium modulation and high calcium permeability of neuronal nicotinic acetylcholine receptors. Neuron 8:127-134
95. Bertrand D, Galzi JL, Devillers-Thiery A, Bertrand S, Changeux JP (1993) Mutations at two distinct sites within the channel domain M2 alter calcium permeability of neuronal alpha 7 nicotinic receptor. Proc Natl Acad Sci USA 90:6971-6975
96. Nutter TJ, Adams DJ (1995) Monovalent and divalent cation permeability and block of neuronal nicotinic receptor channels in rat parasympathetic ganglia. J Gen Physiol 105:701-723
97. Uteshev VV (2010) Evaluation of Ca2+ permeability of nicotinic acetylcholine receptors in hypothalamic histaminergic neurons. Acta Biochim Biophys Sin (Shanghai) 42:8-20
98. Meyer EM, Tay ET, Zoltewicz JA, Papke RL, Meyers C, King M, Fiebre CMd (1998) Neuroprotective and memory-related actions of novel à7 nicotinic agents with different mixed agonist/antagonist properties. J Pharmacol Exp Ther 284:1026-1032
99. Role LW, Berg DK (1996) Nicotinic receptors in the development and modulation of CNS synapses. Neuron 16:1077-1085
100. Dajas-Bailador F, Wonnacott S (2004) Nicotinic acetylcholine receptors and the regulation of neuronal signalling. Trends Pharmacol Sci 25:317-324
101. Thomsen MS, Hansen HH, Timmerman DB, Mikkelsen JD (2010) Cognitive improvement by activation of alpha7 nicotinic acetylcholine receptors: from animal models to human pathophysiology. Curr Pharm Des 16:323-343
102. Albuquerque EX, Pereira EF, Mike A, Eisenberg HM, Maelicke A, Alkondon M (2000) Neuronal nicotinic receptors in synaptic functions in humans and rats: physiological and clinical relevance. Behav Brain Res 113:131-141
103. Fucile S, Renzi M, Lax P, Eusebi F (2003) Fractional Ca(2+) current through human neuronal alpha7 nicotinic acetylcholine receptors. Cell Calcium 34:205-209
104. El-Hajj RA, McKay SB, McKay DB (2007) Pharmacological and immunological Identification of native alpha7 nicotinic receptors: evidence for homomeric and heteromeric alpha7 receptors. Life Sci 81:1317-1322
105. Khiroug SS, Harkness PC, Lamb PW, Sudweeks SN, Khiroug L, Millar NS, Yakel JL (2002) Rat nicotinic ACh receptor alpha7 and beta2 subunits co-assemble to form functional heteromeric nicotinic receptor channels. J Physiol 540:425-434
106. Listerud M, Brussaard AB, Devay P, Colman DR, Role LW (1991) Functional contribution of neuronal AChR subunits revealed by antisense oligonucleotides. Science 254:1518-1521
107. Palma E, Maggi L, Barabino B, Eusebi F, Ballivet M (1999) Nicotinic acetylcholine receptors assembled from the alpha7 and beta3 subunits. J Biol Chem 274:18335-18340
108. Ramirez-Latorre J, Yu CR, Qu X, Perin F, Karlin A, Role L (1996) Functional contributions of alpha5 subunit to neuronal acetylcholine receptor channels. Nature 380:347-351
109. Sudweeks SN, Yakel JL (2000) Functional and molecular characterization of neuronal nicotinic ACh receptors in rat CA1 hippocampal neurons. J Physiol 527(Pt 3):515-528
110. Virginio C, Giacometti A, Aldegheri L, Rimland JM, Terstappen GC (2002) Pharmacological properties of rat alpha 7 nicotinic receptors expressed in native and recombinant cell systems. Eur J Pharmacol 445:153-161
111. Yu CR, Role LW (1998) Functional contribution of the alpha5 subunit to neuronal nicotinic channels expressed by chick sympathetic ganglion neurones. J Physiol 509(Pt 3):667-681
112. Yu CR, Role LW (1998) Functional contribution of the alpha7 subunit to multiple subtypes of nicotinic receptors in embryonic chick sympathetic neurones. J Physiol 509(Pt 3):651-665
113. Patrick J , Sequela P, Vernino S, Amador M, Luetje C, Dani JA (1993) Functional diversity of neuronal nicotinic acetylcholine receptors. Prog Brain Res 98:113-120
114. Levin ED (2002) Nicotinic receptor subtypes and cognitive function. J Neurobiol 53:633-640
115. Marini AM, Rabin SJ, Lipsky RH, Mocchetti I (1998) Activity-dependent release of brainderived neurotrophic factor underlies the neuroprotective effect of N-methyl-D-aspartate. J Biol Chem 273:29394-29399
116. Valera E, Sanchez-Martin FJ, Ferrer-Montiel AV, Messeguer A, Merino JM (2008) NMDAinduced neuroprotection in hippocampal neurons is mediated through the protein kinase A and CREB (cAMP-response element-binding protein) pathway. Neurochem Int 53:148-154
117. Akaike A, Takada-Takatori Y, Kume T, Izumi Y (2010) Mechanisms of neuroprotective effects of nicotine and acetylcholinesterase inhibitors: role of alpha4 and alpha7 receptors in neuroprotection. J Mol Neurosci 40:211-216
118. Lester HA, Dibas MI, Dahan DS, Leite JF, Dougherty DA (2004) Cys-loop receptors: new twists and turns. Trends Neurosci 27:329-336
119. Fucile S, Palma E, Martinez-Torres A, Miledi R, Eusebi F (2002) The single-channel properties of human acetylcholine alpha 7 receptors are altered by fusing alpha 7 to the green fluorescent protein. Proc Natl Acad Sci USA 99:3956-3961
120. Mike A, Castro NG, Albuquerque EX (2000) Choline and acetylcholine have similar kinetic properties of activation and desensitization on the alpha7 nicotinic receptors in rat hippocampal neurons. Brain Res 882:155-168
121. Shao Z, Yakel JL (2000) Single channel properties of neuronal nicotinic ACh receptors in stratum radiatum interneurons of rat hippocampal slices. J Physiol 527(Pt 3):507-513
122. Ascher P, Bregestovski P, Nowak L (1988) N -methyl-D-aspartate-activated channels of mouse central neurones in magnesium-free solutions. J Physiol 399:207-226
123. Uteshev VV, Meyer EM, Papke RL (2002) Activation and inhibition of native neuronal alphabungarotoxin-sensitive nicotinic ACh receptors. Brain Res 948:33-46
124. Uteshev VV, Meyer EM, Papke RL (2003) Regulation of neuronal function by choline and 4OH-GTS-21 through alpha 7 nicotinic receptors. J Neurophysiol 89:1797-1806
125. Alkondon M, Reinhardt S, Lobron C, Hermsen B, Maelicke A, Albuquerque EX (1994) Diversity of nicotinic acetylcholine receptors in rat hippocampal neurons. II. The rundown and inward rectifi cation of agonist-elicited whole cell currents and Identification of receptor subunits by in situ hybridization. J Pharmacol Exp Ther 271:494-506
126. Jahr CE, Stevens CF (1993) Calcium permeability of the N-methyl-D-aspartate receptor channel in hippocampal neurons in culture. Proc Natl Acad Sci USA 90:11573-11577
127. Iino M, Ozawa S, Tsuzuki K (1990) Permeation of calcium through excitatory amino acid receptor channels in cultured rat hippocampal neurons. J Physiol 424:151-165
128. Mayer ML, Westbrook GL (1987) Permeation and block of N -methyl-D-aspartic acid receptor channels by divalent cations in mouse cultured central neurons. J Physiol 394:501
129. Lyford LK, Lee JW, Rosenberg RL (2002) Low-affi nity Ca(2+) and Ba(2+) binding sites in the pore of alpha7 nicotinic acetylcholine receptors. Biochim Biophys Acta 1559:69-78
130. Conroy WG, Liu Z, Nai Q, Coggan JS, Berg DK (2003) PDZ-containing proteins provide a functional postsynaptic scaffold for nicotinic receptors in neurons. Neuron 38:759-771
131. Ehlers MD, Heine M, Groc L, Lee MC, Choquet D (2007) Diffusional trapping of GluR1 AMPA receptors by input-specific synaptic activity. Neuron 54:447-460
132. Mielke JG, Mealing GA (2009) Cellular distribution of the nicotinic acetylcholine receptor alpha7 subunit in rat hippocampus. Neurosci Res 65:296-306
133. Hardingham GE, Fukunaga Y, Bading H (2002) Extrasynaptic NMDARs oppose synaptic NMDARs by triggering CREB shut-off and cell death pathways. Nat Neurosci 5:405-414
134. Zhang Z, Coggan JS, Berg DK (1996) Synaptic currents generated by neuronal acetylcholine receptors sensitive to alpha-bungarotoxin. Neuron 17:1231-1240
135. Frazier CJ, Buhler AV, Weiner JL, Dunwiddie TV (1998) Synaptic potentials mediated via alpha-bungarotoxin-sensitive nicotinic acetylcholine receptors in rat hippocampal interneurons. J Neurosci 18:8228-8235
136. Hefft S, Hulo S, Bertrand D, Muller D (1999) Synaptic transmission at nicotinic acetylcholine receptors in rat hippocampal organotypic cultures and slices. J Physiol 515(Pt 3): 769-776
137. Hatton GI, Yang QZ (2002) Synaptic potentials mediated by alpha 7 nicotinic acetylcholine receptors in supraoptic nucleus. J Neurosci 22:29-37
138. Kem WR (2000) The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21). Behav Brain Res 113:169-181
139. Uteshev VV, Stevens DR, Haas HL (1996) Alpha-Bungarotoxin-sensitive nicotinic responses in rat tuberomammillary neurons. Pflugers Arch 432:607-613
140. Alkondon M, Pereira EF, Almeida LE, Randall WR, Albuquerque EX (2000) Nicotine at concentrations found in cigarette smokers activates and desensitizes nicotinic acetylcholine receptors in CA1 interneurons of rat hippocampus. Neuropharmacology 39:2726-2739
141. Fujii S, Ji Z, Sumikawa K (2000) Inactivation of alpha7 ACh receptors and activation of nonalpha7 ACh receptors both contribute to long term potentiation induction in the hippocampal CA1 region. Neurosci Lett 286:134-138
142. Ferchmin PA, Perez D, Eterovic VA, de Vellis J (2003) Nicotinic receptors differentially regulate N-methyl-D-aspartate damage in acute hippocampal slices. J Pharmacol Exp Ther 305:1071-1078
143. Hu M, Gopalakrishnan M, Li J (2009) Positive allosteric modulation of alpha7 neuronal nicotinic acetylcholine receptors: lack of cytotoxicity in PC12 cells and rat primary cortical neurons. Br J Pharmacol 158:1857-1864
144. Briggs CA, Gronlien JH, Curzon P, Timmermann DB, Ween H, Thorin-Hagene K, Kerr P, Anderson DJ, Malysz J, Dyhring T, Olsen GM, Peters D, Bunnelle WH, Gopalakrishnan M (2009) Role of channel activation in cognitive enhancement mediated by alpha7 nicotinic acetylcholine receptors. Br J Pharmacol 158:1486-1494
145. Leon SF, Suwazono S, Takenaga S, Arimura K, Osame M (1997) The effects of tobacco smoking on the short, middle, and long latency responses of the blink reflex in humans. J Clin Neurophysiol 14:144-149
146. Woodruff-Pak DS, Green JT, Coleman-Valencia C, Pak JT (2000) A nicotinic cholinergic agonist (GTS-21) and eyeblink classical conditioning: acquisition, retention, and relearning in older rabbits. Exp Aging Res 26:323-336
147. Woodruff-Pak DS (2003) Mecamylamine reversal by nicotine and by a partial alpha7 nicotinic acetylcholine receptor agonist (GTS-21) in rabbits tested with delay eyeblink classical conditioning. Behav Brain Res 143:159-167
148. Brown KL, Comalli DM, Biasi MD, Woodruff-Pak DS (2010) Trace eyeblink conditioning is impaired in alpha7 but not in beta2 nicotinic acetylcholine receptor knockout mice. Front Behav Neurosci 4:166
149. Hernandez CM, Kayed R, Zheng H, Sweatt JD, Dineley KT (2010) Loss of alpha7 nicotinic receptors enhances beta-amyloid oligomer accumulation, exacerbating early-stage cognitive decline and septohippocampal pathology in a mouse model of Alzheimer's disease. J Neurosci 30:2442-2453
150. Ren K, King MA, Liu J, Siemann J, Altman M, Meyers C, Hughes JA, Meyer EM (2007) The alpha7 nicotinic receptor agonist 4OH-GTS-21 protects axotomized septohippocampal cholinergic neurons in wild type but not amyloid-overexpressing transgenic mice. Neuroscience 148:230-237
151. Jonnala RR, Buccafusco JJ (2001) Relationship between the increased cell surface alpha7 nicotinic receptor expression and neuroprotection induced by several nicotinic receptor agonists. J Neurosci Res 66:565-572
152. Hu M, Schurdak ME, Puttfarcken PS, El Kouhen R, Gopalakrishnan M, Li J (2007) High content screen microscopy analysis of A beta 1-42-induced neurite outgrowth reduction in rat primary cortical neurons: neuroprotective effects of alpha 7 neuronal nicotinic acetylcholine receptor ligands. Brain Res 1151:227-235
153. Qi XL, Nordberg A, Xiu J, Guan ZZ (2007) The consequences of reducing expression of the alpha7 nicotinic receptor by RNA interference and of stimulating its activity with an alpha7 agonist in SH-SY5Y cells indicate that this receptor plays a neuroprotective role in connection with the pathogenesis of Alzheimer's disease. Neurochem Int 51:377-383
154. Wang HY, Li W, Benedetti NJ, Lee DH (2003) Alpha 7 nicotinic acetylcholine receptors mediate beta-amyloid peptide-induced tau protein phosphorylation. J Biol Chem 278: 31547-31553
155. Dineley KT, Westerman M, Bui D, Bell K, Ashe KH, Sweatt JD (2001) Beta-amyloid activates the mitogen-activated protein kinase cascade via hippocampal alpha7 nicotinic acetylcholine receptors: in vitro and in vivo mechanisms related to Alzheimer's disease. J Neurosci 21:4125-4133
156. Dineley KT, Bell KA, Bui D, Sweatt JD (2002) Beta -Amyloid peptide activates alpha 7 nicotinic acetylcholine receptors expressed in Xenopus oocytes. J Biol Chem 277: 25056-25061
157. Dineley KT (2007) Beta-amyloid peptide-nicotinic acetylcholine receptor interaction: the two faces of health and disease. Front Biosci 12:5030-5038
158. Clifford PM, Siu G, Kosciuk M, Levin EC, Venkataraman V, D'Andrea MR, Nagele RG (2008) Alpha7 nicotinic acetylcholine receptor expression by vascular smooth muscle cells facilitates the deposition of Abeta peptides and promotes cerebrovascular amyloid angiopathy. Brain Res 1234:158-171
159. Soderman A, Thomsen MS, Hansen HH, Nielsen EO, Jensen MS, West MJ, Mikkelsen JD (2008) The nicotinic alpha7 acetylcholine receptor agonist ssr180711 is unable to activate limbic neurons in mice overexpressing human amyloid-beta1-42. Brain Res 1227:240-247
160. Wang HY, Stucky A, Liu J, Shen C, Trocme-Thibierge C, Morain P (2009) Dissociating betaamyloid from alpha 7 nicotinic acetylcholine receptor by a novel therapeutic agent, S 24795, normalizes alpha 7 nicotinic acetylcholine and NMDA receptor function in Alzheimer's disease brain. J Neurosci 29:10961-10973
161. Martin SE, de Fiebre NE, de Fiebre CM (2004) The alpha7 nicotinic acetylcholine receptorselective antagonist, methyllycaconitine, partially protects against beta-amyloid1-42 toxicity in primary neuron-enriched cultures. Brain Res 1022:254-256
162. Dziewczapolski G, Glogowski CM, Masliah E, Heinemann SF (2009) Deletion of the alpha 7 nicotinic acetylcholine receptor gene improves cognitive defi
163. Nagele RG, D'Andrea MR, Anderson WJ, Wang HY (2002) Intracellular accumulation of beta-amyloid(1-42) in neurons is facilitated by the alpha 7 nicotinic acetylcholine receptor in Alzheimer's disease. Neuroscience 110:199-211
164. Wang HY, Lee DH, D'Andrea MR, Peterson PA, Shank RP, Reitz AB (2000) Beta-Amyloid(1-42) binds to alpha7 nicotinic acetylcholine receptor with high affi nity. Implications for Alzheimer's disease pathology. J Biol Chem 275:5626-5632
165. D'Andrea MR, Nagele RG (2006) Targeting the alpha 7 nicotinic acetylcholine receptor to reduce amyloid accumulation in Alzheimer's disease pyramidal neurons. Curr Pharm Des 12:677-684
166. Jenden DJ, Scremin OU, Roch M, Li G (1996) The influence of aging on whole body choline release and clearance. Life Sci 58:2003-2009
167. Guan ZZ, Zhang X, Ravid R, Nordberg A (2000) Decreased protein levels of nicotinic receptor subunits in the hippocampus and temporal cortex of patients with Alzheimer's disease. J Neurochem 74:237-243
168. Nordberg A (2001) Nicotinic receptor abnormalities of Alzheimer's disease: therapeutic implications. Biol Psychiatry 49:200-210
169. Sarter M, Parikh V (2005) Choline transporters, cholinergic transmission and cognition. Nat Rev Neurosci 6:48-56
170. Martin LF, Freedman R (2007) Schizophrenia and the alpha7 nicotinic acetylcholine receptor. Int Rev Neurobiol 78:225-246
171. Leonard S, Breese C, Adams C, Benhammou K, Gault J, Stevens K, Lee M, Adler L, Olincy A, Ross R, Freedman R (2000) Smoking and schizophrenia: abnormal nicotinic receptor expression. Eur J Pharmacol 393:237-242
172. Freedman R, Adams CE, Leonard S (2000) The alpha7-nicotinic acetylcholine receptor and the pathology of hippocampal interneurons in schizophrenia. J Chem Neuroanat 20: 299-306
173. Stevens KE, Freedman R, Collins AC, Hall M, Leonard S, Marks MJ, Rose GM (1996) Genetic correlation of inhibitory gating of hippocampal auditory evoked response and alpha-bungarotoxin-binding nicotinic cholinergic receptors in inbred mouse strains. Neuropsychopharmacology 15:152-162
174. Felix R, Levin ED (1997) Nicotinic antagonist administration into the ventral hippocampus and spatial working memory in rats. Neuroscience 81:1009-1017
175. Wevers A, Witter B, Moser N, Burghaus L, Banerjee C, Steinlein OK, Schutz U, de Vos RA, Steur EN, Lindstrom J, Schroder H (2000) Classical Alzheimer features and cholinergic dysfunction: towards a unifying hypothesis? Acta Neurol Scand Suppl 176:42-48
176. Freedman R, Hall M, Adler LE, Leonard S (1995) Evidence in postmortem brain tissue for decreased numbers of hippocampal nicotinic receptors in schizophrenia. Biol Psychiatry 38:22-33
177. Perry EK, Morris CM, Court JA, Cheng A, Fairbairn AF, McKeith IG, Irving D, Brown A, Perry RH (1995) Alteration in nicotine binding sites in Parkinson's disease. Lewy body dementia and Alzheimer's disease: possible index of early neuropathology. Neuroscience 64:385-395
178. Nordberg A, Winblad B (1986) Reduced number of [3H]nicotine and [3H]acetylcholine binding sites in the frontal cortex of Alzheimer brains. Neurosci Lett 72:115-119
179. Shimohama S, Taniguchi T, Fujiwara M, Kameyama M (1986) Changes in nicotinic and muscarinic cholinergic receptors in Alzheimer-type dementia. J Neurochem 46:288-293
180. London ED, Ball MJ, Waller SB (1989) Nicotinic binding sites in cerebral cortex and hippocampus in Alzheimer's dementia. Neurochem Res 14:745-750
181. Takeuchi H, Yanagida T, Inden M, Takata K, Kitamura Y, Yamakawa K, Sawada H, Izumi Y, Yamamoto N, Kihara T, Uemura K, Inoue H, Taniguchi T, Akaike A, Takahashi R, Shimohama S (2009) Nicotinic receptor stimulation protects nigral dopaminergic neurons in rotenoneinduced Parkinson's disease models. J Neurosci Res 87:576-585
182. Kaneko S, Maeda T, Kume T, Kochiyama H, Akaike A, Shimohama S, Kimura J (1997) Nicotine protects cultured cortical neurons against glutamate-induced cytotoxicity via alpha7-neuronal receptors and neuronal CNS receptors. Brain Res 765:135-140
183. Meyer EM, King MA, Meyers C (1998) Neuroprotective effects of 2,4-dimethoxybenzylidene anabaseine (DMXB) and tetrahydroaminoacridine (THA) in neocortices of nucleus basalis lesioned rats. Brain Res 786:252-254
184. Li Y, Meyer EM, Walker DW, Millard WJ, He YJ, King MA (2002) Alpha7 nicotinic receptor activation inhibits ethanol-induced mitochondrial dysfunction, cytochrome c release and neurotoxicity in primary rat hippocampal neuronal cultures. J Neurochem 81:853-858
185. Verbois SL, Scheff SW, Pauly JR (2003) Chronic nicotine treatment attenuates alpha 7 nicotinic receptor defi cits following traumatic brain injury. Neuropharmacology 44:224-233
186. Buccafusco JJ, Beach JW, Terry AV Jr, Doad GS, Sood A, Arias E, Misawa H, Masai M, Fujii T, Kawashima K (2004) Novel analogs of choline as potential neuroprotective agents. J Alzheimers Dis 6:S85-S92
187. Fucile S, Renzi M, Lauro C, Limatola C, Ciotti T, Eusebi F (2004) Nicotinic cholinergic stimulation promotes survival and reduces motility of cultured rat cerebellar granule cells. Neuroscience 127:53-61
188. Rosa AO, Egea J, Gandia L, Lopez MG, Garcia AG (2006) Neuroprotection by nicotine in hippocampal slices subjected to oxygen-glucose deprivation: involvement of the alpha7 nAChR subtype. J Mol Neurosci 30:61-62
189. Guseva MV, Hopkins DM, Scheff SW, Pauly JR (2008) Dietary choline supplementation improves behavioral, histological, and neurochemical outcomes in a rat model of traumatic brain injury. J Neurotrauma 25:975-983
190. Buccafusco JJ, Letchworth SR, Bencherif M, Lippiello PM (2005) Long-lasting cognitive improvement with nicotinic receptor agonists: mechanisms of pharmacokinetic-pharmacodynamic discordance. Trends Pharmacol Sci 26:352-360
191. Buccafusco JJ, Terry AV Jr, Decker MW, Gopalakrishnan M (2007) Profile of nicotinic acetylcholine receptor agonists ABT-594 and A-582941, with differential subtype selectivity, on delayed matching accuracy by young monkeys. Biochem Pharmacol 74:1202-1211
192. Kitagawa H, Takenouchi T, Azuma R, Wesnes KA, Kramer WG, Clody DE, Burnett AL (2003) Safety, pharmacokinetics, and effects on cognitive function of multiple doses of GTS-21 in healthy, male volunteers. Neuropsychopharmacology 28:542-551
193. Leiser SC, Bowlby MR, Comery TA, Dunlop J (2009) A cog in cognition: how the alpha 7 nicotinic acetylcholine receptor is geared towards improving cognitive defi cits. Pharmacol Ther 122:302-311
194. Olincy A, Stevens KE (2007) Treating schizophrenia symptoms with an alpha7 nicotinic agonist, from mice to men. Biochem Pharmacol 74:1192-1201
195. Arendash GW, Sengstock GJ, Sanberg PR, Kem WR (1995) Improved learning and memory in aged rats with chronic administration of the nicotinic receptor agonist GTS-21. Brain Res 674:252-259
196. Meyer EM, Tay ET, Papke RL, Meyers C, Huang G, de Fiebre CM (1997) Effects of 3-[2,4-dimethoxybenzylidene]anabaseine (DMXB) on rat nicotinic receptors and memoryrelated behaviors. Brain Res 768:49-56
197. Ross RG, Stevens KE, Proctor WR, Leonard S, Kisley MA, Hunter SK, Freedman R, Adams CE (2010) Research review: cholinergic mechanisms, early brain development, and risk for schizophrenia. J Child Psychol Psychiatry 51:535-549
198. Olincy A, Harris JG, Johnson LL, Pender V, Kongs S, Allensworth D, Ellis J, Zerbe GO, Leonard S, Stevens KE, Stevens JO, Martin L, Adler LE, Soti F, Kem WR, Freedman R (2006) Proof-of-concept trial of an alpha7 nicotinic agonist in schizophrenia. Arch Gen Psychiatry 63:630-638
199. Martin EJ, Panikar KS, King MA, Deyrup M, Hunter B, Wang G, Meyer E (1994) Cytoprotective actions of 2,4-dimethoxybenzylidene anabaseine in differentiated PC12 cells and septal cholinergic cells. Drug Dev Res 31:134-141
200. Briggs CA, Anderson DJ, Brioni JD, Buccafusco JJ, Buckley MJ, Campbell JE, Decker MW, Donnelly-Roberts D, Elliot RL, Gopalakrishnan M, Holladay MW, Hui Y, Jackson W, Kim DJB, Marsh KC, O'Neill AO, Pendergast MA, Ryther KB, Sullivan JP, Arneric SP (1997) Functional characterization of the novel nicotinic receptor ligand GTS-21 in vitro and in vivo. Pharmacol Biochem Behav 57:231-241
201. Van Kampen M, Selbach K, Schneider R, Schiegel E, Boess F, Schreiber R (2004) AR-R 17779 improves social recognition in rats by activation of nicotinic alpha7 receptors. Psychopharmacology 172:375-383
202. Woodruff-Pak DS, Li Y, Kem WR (1994) A nicotinic agonist (GTS-21), eyeblink classical conditioning, and nicotinic receptor binding in rabbit brain. Brain Res 645:309-317
203. Wishka DG, Walker DP, Yates KM, Reitz SC, Jia S, Myers JK, Olson KL, Jacobsen EJ, Wolfe ML, Groppi VE, Hanchar AJ, Thornburgh BA, Cortes-Burgos LA, Wong EH, Staton BA, Raub TJ, Higdon NR, Wall TM, Hurst RS, Walters RR, Hoffmann WE, Hajos M, Franklin S, Carey G, Gold LH, Cook KK, Sands SB, Zhao SX, Soglia JR, Kalgutkar AS, Arneric SP, Rogers BN (2006) Discovery of N-[(3R)-1- azabicyclo[2.2.2]oct-3-yl]furo[2,3-c] pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive defi cits in schizophrenia: synthesis and structure-activity relationship. J Med Chem 49:4425-4436
204. Bitner RS, Bunnelle WH, Decker MW, Drescher KU, Kohlhaas KL, Markosyan S, Marsh KC, Nikkel AL, Browman K, Radek R, Anderson DJ, Buccafusco J, Gopalakrishnan M (2010) In vivo pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107: preclinical considerations in Alzheimer's disease. J Pharmacol Exp Ther 334:875-886
205. Bitner RS, Bunnelle WH, Anderson DJ, Briggs CA, Buccafusco J, Curzon P, Decker MW, Frost JM, Gronlien JH, Gubbins E, Li J, Malysz J, Markosyan S, Marsh K, Meyer MD, Nikkel AL, Radek RJ, Robb HM, Timmermann D, Sullivan JP, Gopalakrishnan M (2007) Broad-spectrum efficacy across cognitive domains by alpha7 nicotinic acetylcholine receptor agonism correlates with activation of ERK1/2 and CREB phosphorylation pathways. J Neurosci 27:10578-10587
206. Boess FG, De Vry J, Erb C, Flessner T, Hendrix M, Luithle J, Methfessel C, Riedl B, Schnizler K, van der Staay FJ, van Kampen M, Wiese WB, Koenig G (2007) The novel alpha7 nicotinic acetylcholine receptor agonist N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-7-[2-(methoxy)phenyl]-1-benzofuran-2- carboxamide improves working and recognition memory in rodents. J Pharmacol Exp Ther 321:716-725
207. Pichat P, Bergis OE, Terranova JP, Urani A, Duarte C, Santucci V, Gueudet C, Voltz C, Steinberg R, Stemmelin J, Oury-Donat F, Avenet P, Griebel G, Scatton B (2007) SSR180711, a novel selective alpha7 nicotinic receptor partial agonist: (II) efficacy in experimental models predictive of activity against cognitive symptoms of schizophrenia. Neuropsychopharmacology 32:17-34
208. Tatsumi R, Fujio M, Takanashi S, Numata A, Katayama J, Satoh H, Shiigi Y, Maeda J, Kuriyama M, Horikawa T, Murozono T, Hashimoto K, Tanaka H (2006) (R)-3-(3-methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5 -oxazolidin]-2 -one, a novel and potent alpha7 nicotinic acetylcholine receptor partial agonist displays cognitive enhancing properties. J Med Chem 49:4374-4383
209. Ren K, Thinschmidt J, Liu J, Ai L, Papke RL, King MA, Hughes JA, Meyer EM (2007) Alpha7 Nicotinic receptor gene delivery into mouse hippocampal neurons leads to functional receptor expression, improved spatial memory-related performance, and tau hyperphosphorylation. Neuroscience 145:314-322
210. Banerjee C, Nyengaard JR, Wevers A, de Vos RA, Jansen Steur EN, Lindstrom J, Pilz K, Nowacki S, Bloch W, Schroder H (2000) Cellular expression of alpha7 nicotinic acetylcholine receptor protein in the temporal cortex in Alzheimer's and Parkinson's disease-a stereological approac. Neurobiol Dis 7:666-672
211. Loughead J, Ray R, Wileyto EP, Ruparel K, Sanborn P, Siegel S, Gur RC, Lerman C (2010) Effects of the alpha4beta2 partial agonist varenicline on brain activity and working memory in abstinent smokers. Biol Psychiatry 67:715-721
212. Furey ML, Pietrini P, Haxby JV, Alexander GE, Lee HC, VanMeter J, Grady CL, Shetty U, Rapoport SI, Schapiro MB, Freo U (1997) Cholinergic stimulation alters performance and task-specific regional cerebral blood flow during working memory. Proc Natl Acad Sci USA 94:6512-6516
213. Kirrane RM, Mitropoulou V, Nunn M, Silverman J, Siever LJ (2001) Physostigmine and cognition in schizotypal personality disorder. Schizophr Res 48:1-5
214. Koller G, Satzger W, Adam M, Wagner M, Kathmann N, Soyka M, Engel R (2003) Effects of scopolamine on matching to sample paradigm and related tests in human subjects. Neuropsychobiology 48:87-94
215. Green A, Ellis KA, Ellis J, Bartholomeusz CF, Ilic S, Croft RJ, Phan KL, Nathan PJ (2005) Muscarinic and nicotinic receptor modulation of object and spatial n-back working memory in humans. Pharmacol Biochem Behav 81:575-584
216. Ellis JR, Ellis KA, Bartholomeusz CF, Harrison BJ, Wesnes KA, Erskine FF, Vitetta L, Nathan PJ (2006) Muscarinic and nicotinic receptors synergistically modulate working memory and attention in humans. Int J Neuropsychopharmacol 9:175-189
217. Dunbar G, Kuchibhatla R, Lee G (2011) A randomized double-blind study comparing 25 and 50 mg TC-1734 (AZD3480) with placebo, in older subjects with age-associated memory impairment. J Psychopharmacol 25:1020-1029
218. Farlow MR, Salloway S, Tariot PN, Yardley J, Moline ML, Wang Q, Brand-Schieber E, Zou H, Hsu T, Satlin A (2010) Effectiveness and tolerability of high-dose (23 mg/d) versus standard-dose (10 mg/d) donepezil in moderate to severe Alzheimer's disease: a 24-week, randomized, double-blind study. Clin Ther 32:1234-1251
219. Alva G, Cummings JL (2008) Relative tolerability of Alzheimer's disease treatments. Psychiatry (Edgmont) 5:27-36
220. Lopez-Hernandez GY, Thinschmidt JS, Morain P, Trocme-Thibierge C, Kem WR, Soti F, Papke RL (2009) Positive modulation of alpha7 nAChR responses in rat hippocampal interneurons to full agonists and the alpha7-selective partial agonists, 4OH-GTS-21 and S 24795. Neuropharmacology 56:821-830
221. Papke RL, Bencherif M, Lippiello P (1996) An evaluation of neuronal nicotinic acetylcholine receptor activation by quaternary nitrogen compounds indicates that choline is selective for the alpha 7 subtype. Neurosci Lett 213:201-204
222. Alkondon M, Pereira EF, Cortes WS, Maelicke A, Albuquerque EX (1997) Choline is a selective agonist of alpha7 nicotinic acetylcholine receptors in the rat brain neurons. Eur J Neurosci 9:2734-2742
223. Bertrand N, Ishii H, Spatz M (1996) Cerebral ischemia in young and adult gerbils: effects on cholinergic metabolism. Neurochem Int 28:293-297
224. Jope RS, Gu X (1991) Seizures increase acetylcholine and choline concentrations in rat brain regions. Neurochem Res 16:1219-1226
225. Parikh V, Sarter M (2006) Cortical choline transporter function measured in vivo using choline-sensitive microelectrodes: clearance of endogenous and exogenous choline and effects of removal of cholinergic terminals. J Neurochem 97:488-503
226. Rao AM, Hatcher JF, Dempsey RJ (2000) Lipid alterations in transient forebrain ischemia: possible new mechanisms of CDP-choline neuroprotection. J Neurochem 75:2528-2535
227. Scremin OU, Jenden DJ (1991) Time-dependent changes in cerebral choline and acetylcholine induced by transient global ischemia in rats. Stroke 22:643-647
228. Papke RL, Papke JKP (2002) Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis. Br J Pharmacol 137:49-61
229. Klein J, Koppen A, Loffelholz K (1998) Regulation of free choline in rat brain: dietary and pharmacological manipulations. Neurochem Int 32:479-485
230. Faghih R, Gfesser GA, Gopalakrishnan M (2007) Advances in the discovery of novel positive allosteric modulators of the alpha7 nicotinic acetylcholine receptor. Recent Patents CNS Drug Discov 2:99-106
231. Roncarati R, Seredenina T, Jow B, Jow F, Papini S, Kramer A, Bothmann H, Dunlop J, Terstappen GC (2008) Functional properties of alpha7 nicotinic acetylcholine receptors coexpressed with RIC-3 in a stable recombinant CHO-K1 cell line. Assay Drug Dev Technol 6:181-193
232. Barron SC, McLaughlin JT, See JA, Richards VL, Rosenberg RL (2009) The allosteric modulator of {alpha}7 nicotinic receptors, PNU-120596, causes conformational changes in the extracellular ligand binding domain similar to acetylcholine. Mol Pharmacol 76:253-263
233. Young GT, Zwart R, Walker AS, Sher E, Millar NS (2008) Potentiation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site. Proc Natl Acad Sci USA 105:14686-14691
234. Gronlien JH, Hakerud M, Ween H, Thorin-Hagene K, Briggs CA, Gopalakrishnan M, Malysz J (2007) Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes. Mol Pharmacol 72:715-724
235. Bertrand D, Bertrand S, Cassar S, Gubbins E, Li J, Gopalakrishnan M (2008) Positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor: ligand interactions with distinct binding sites and evidence for a prominent role of the M2-M3 segment. Mol Pharmacol 74:1407-1416
236. Disterhoft JF, Oh MM (2007) Alterations in intrinsic neuronal excitability during normal aging. Aging Cell 6:327-336
237. Kaczorowski CC, Disterhoft JF (2009) Memory defi cits are associated with impaired ability to modulate neuronal excitability in middle-aged mice. Learn Mem 16:362-366
238. Gilbert D, Lecchi M, Arnaudeau S, Bertrand D, Demaurex N (2009) Local and global calcium signals associated with the opening of neuronal alpha7 nicotinic acetylcholine receptors. Cell Calcium 45:198-207
239. De Rosa MJ, Dionisio L, Agriello E, Bouzat C, Esandi Mdel C (2009) Alpha 7 nicotinic acetylcholine receptor modulates lymphocyte activation. Life Sci 85:444-449
240. Hao J, Simard AR, Turner GH, Wu J, Whiteaker P, Lukas RJ, Shi FD (2010) Attenuation of CNS infl ammatory responses by nicotine involves alpha7 and non-alpha7 nicotinic receptors. Exp Neurol 227:110-119
241. Kawashima K, Fujii T (2003) The lymphocytic cholinergic system and its contribution to the regulation of immune activity. Life Sci 74:675-696
242. Koval L, Lykhmus O, Zhmak M, Khruschov A, Tsetlin V, Magrini E, Viola A, Chernyavsky A, Qian J, Grando S, Komisarenko S, Skok M (2011) Differential involvement of alpha-4beta2, alpha7 and alpha9alpha10 nicotinic acetylcholine receptors in B lymphocyte activation in vitro. Int J Biochem Cell Biol 43:516-524
243. Mashkina AP, Cizkova D, Vanicky I, Boldyrev AA (2010) NMDA receptors are expressed in lymphocytes activated both in vitro and in vivo. Cell Mol Neurobiol 30:901-907
244. Mashkina AP, Tyulina OV, Solovyova TI, Kovalenko EI, Kanevski LM, Johnson P, Boldyrev AA (2007) The excitotoxic effect of NMDA on human lymphocyte immune function. Neurochem Int 51:356-360
245. Nizri E, Hamra-Amitay Y, Sicsic C, Lavon I, Brenner T (2006) Anti-infl ammatory properties of cholinergic up-regulation: a new role for acetylcholinesterase inhibitors. Neuropharmacology 50:540-547
246. Nizri E, Irony-Tur-Sinai M, Lory O, Orr-Urtreger A, Lavi E, Brenner T (2009) Activation of the cholinergic anti-infl ammatory system by nicotine attenuates neuroinflammation via suppression of Th1 and Th17 responses. J Immunol 183:6681-6688
247. Sharma G, Vijayaraghavan S (2002) Nicotinic receptor signaling in nonexcitable cells. J Neurobiol 53:524-534
248. Skok MV, Grailhe R, Agenes F, Changeux JP (2007) The role of nicotinic receptors in B-lymphocyte development and activation. Life Sci 80:2334-2336
249. Wang H, Yu M, Ochani M, Amella CA, Tanovic M, Susarla S, Li JH, Yang H, Ulloa L, Al-Abed Y, Czura CJ, Tracey KJ (2003) Nicotinic acetylcholine receptor alpha7 subunit is an essential regulator of inflammation. Nature 421:384-388
250. Yawata I, Takeuchi H, Doi Y, Liang J, Mizuno T, Suzumura A (2008) Macrophage-induced neurotoxicity is mediated by glutamate and attenuated by glutaminase inhibitors and gap junction inhibitors. Life Sci 82:1111-1116
251. Catassi A, Paleari L, Servent D, Sessa F, Dominioni L, Ognio E, Cilli M, Vacca P, Mingari M, Gaudino G, Bertino P, Paolucci M, Calcaterra A, Cesario A, Granone P, Costa R, Ciarlo M, Alama A, Russo P (2008) Targeting alpha7-nicotinic receptor for the treatment of pleural mesothelioma. Eur J Cancer 44:2296-2311
252. Catassi A, Servent D, Paleari L, Cesario A, Russo P (2008) Multiple roles of nicotine on cell proliferation and inhibition of apoptosis: implications on lung carcinogenesis. Mutat Res 659:221-231
253. Davis R, Rizwani W, Banerjee S, Kovacs M, Haura E, Coppola D, Chellappan S (2009) Nicotine promotes tumor growth and metastasis in mouse models of lung cancer. PLoS One 4:e7524
254. Egleton RD, Brown KC, Dasgupta P (2008) Nicotinic acetylcholine receptors in cancer: multiple roles in proliferation and inhibition of apoptosis. Trends Pharmacol Sci 29:151-158
255. North WG, Gao G, Memoli VA, Pang RH, Lynch L (2010) Breast cancer expresses functional NMDA receptors. Breast Cancer Res Treat 122:307-314
256. Paleari L, Catassi A, Ciarlo M, Cavalieri Z, Bruzzo C, Servent D, Cesario A, Chessa L, Cilli M, Piccardi F, Granone P, Russo P (2008) Role of alpha7-nicotinic acetylcholine receptor in human non-small cell lung cancer proliferation. Cell Prolif 41:936-959
257. Tachibana N, Shirakawa T, Ishii K, Takahashi Y, Tanaka K, Arima K, Yoshida T, Ikeda S (2010) Expression of various glutamate receptors including N-methyl-D-aspartate receptor (NMDAR) in an ovarian teratoma removed from a young woman with anti-NMDAR encephalitis. Intern Med 49:2167-2173
258. Oh MM, Wu WW, Power JM, Disterhoft JF (2006) Galantamine increases excitability of CA1 hippocampal pyramidal neurons. Neuroscience 137:113-123
259. Lynch G, Palmer LC, Gall CM (2011) The likelihood of cognitive enhancement. Pharmacol Biochem Behav 99:116-129