Stable expression, pharmacologic properties and regulation of the human neuronal nicotinic acetylcholine alpha 4 beta 2 receptor.

Gopalakrishnan, M; Monteggia, L M; Anderson, D J; Molinari, E J; Piattoni-Kaplan, M; Donnelly-Roberts, D; Arneric, S P; Sullivan, J P

doi:10.1016/s0022-3565(25)12264-7

Cited by 181Nicotinic Acetylcholine Receptors StudyNeuroscience and Neuropharmacology ResearchReceptor Mechanisms and Signaling

Stable expression, pharmacologic properties and regulation of the human neuronal nicotinic acetylcholine alpha 4 beta 2 receptor.

Gopalakrishnan, M, Monteggia, L M, Anderson, D J, Molinari, E J, Piattoni-Kaplan, M, Donnelly-Roberts, D, Arneric, S P, Sullivan, J P·1996·The Journal of Pharmacology and Experimental Therapeutics

DOI 10.1016/s0022-3565(25)12264-7

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Abstract

(-)-Nicotine, the prototypical agonist for neuronal nicotinic acetylcholine receptors (nAChR) has been shown to bind with high affinity to the rodent and avian alpha 4 beta 2 nAChR subtype. This subtype may represent a primary molecular target for some of the beneficial central nervous system effects i.e., cognitive enhancement, anxiolysis, analgesia, neuroprotection, of (-)-nicotine and related ligands. However, a detailed study of the human alpha 4 beta 2 subunit combination has not yet been reported. In this study, we stably coexpressed the human neuronal alpha 4 and beta 2 nAChR subunits in human embryonic kidney (HEK) 293 cells and studied its pharmacological and regulatory properties. [3H]Cytisine bound to stably transfected cells with high affinity (KD value, 0.2 +/- 0.04 nM) and with a Bmax value of 1359 +/- 91 fmol/mg protein. A good correlation (r = 0.98) was observed between binding affinities in transfected cells and in native neuronal preparations for a series of nAChR ligands. 86Rb+ efflux studies showed that stably transfected cells express functional ion channels that are sensitive to blockade by dihydro-beta-erythroidine. (+/-)-Epibatidine, (-)-nicotine, 1,1-dimethyl-4-phenylpiperazinium, (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT-418), acetylcholine and (-)-cytisine stimulated 86Rb+ efflux with EC50 values of 0.02, 3.9, 2.5, 10, 44 and 38 microM, respectively. Treatment of transfected cells with (-)-nicotine for 7 days led to a significant increase in the density of [3H](-)-cytisine binding sites (EC50 = 0.56 microM) and a significant enhancement in the sensitivity of ACh. Specific binding or (-)-nicotine-evoked cation efflux was not detected in untransfected cells. Analysis of total cellular RNA from transfected, but not untransfected cells, showed the expected fragment sizes corresponding to the human alpha 4 and beta 2 subunit mRNA. These results demonstrate that stable expression of the human alpha 4 beta 2 nAChR subunit combination can give rise to functional ion channels that bind [3H](-)-cytisine with high affinity, exhibit homologous regulation and evoke agonist-induced cation flux with pharmacological properties consistent with native neuronal alpha 4 beta 2 nAChR.

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After chronic nicotine treatment, increased responses that reflect the higher receptor numbers are usually observed later.
“Subsequently, however, increased responses reflecting the increased receptors are usually found (Rowell and Wonnacott, 1990;Benwell et al., 1995;Gopalakrishnan et al., 1996Gopalakrishnan et al., , 1997;;Buisson and Bertrand, 2001;Avila et al., 2003)”
From Chronic Sazetidine-A at Behaviorally Active Doses Does Not Increase Nicotinic Cholinergic Receptors in Rodent Brain (2012) · cites this paper as Gopalakrishnan et al., 1996
α4β2 receptors exist in a mixed population whose nicotine EC50 values differ by 50- to 100-fold (~1 and ~100 μM).
“The α4β2 receptors exist in a mixed population whose nicotine EC50 values differ by 50- to 100-fold (70–73) (~1 and ~100 μM).”
From Nicotine is a selective pharmacological chaperone of acetylcholine receptor number and stoichiometry. Implications for drug discovery (2009) · cites this paper as [70]

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Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations alpha2beta4, alpha3beta4 and alpha4beta4 stably expressed in HEK293 cells.
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Janhunen, S. K., & Ahtee, L. (2006) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2006.09.008 · Cited by 81 · see citing works
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Fenster, C. P., Beckman, M. L., Parker, J. C., Sheffield, E. B., Whitworth, T. L., Quick, M. W., & Lester, R. A. J. (1999) · Molecular Pharmacology · doi:10.1016/s0026-895x(24)12167-0 · Cited by 81 · see citing works
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Sallette, J., Bohler, S., Benoit, P., Soudant, M., Pons, S., Le Novère, N., Changeux, J.-P., & Corringer, P. J. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m308260200 · Cited by 80 · see citing works
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Marks, M. J., Whiteaker, P., Calcaterra, J., Stitzel, J. A., Bullock, A. E., Grady, S. R., Picciotto, M. R., Changeux, J.-P., & Collins, A. C. (1999) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)38240-0 · Cited by 79 · see citing works
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Sullivan, J. P., Donnelly‐Roberts, D. L., Briggs, C. A., Anderson, D. J., Gopalakrishnan, M., Xue, I. C., Piattoni-Kaplan, M., Molinari, E. J., Campbell, J. E., McKenna, D. G., et al. (1997) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)37014-4 · Cited by 79 · see citing works
Agonist-Induced Up-Regulation of α4β2 Nicotinic Acetylcholine Receptors in M10 Cells: Pharmacological and Spatial Definition
Whiteaker, P., Sharples, C. G. V., & Wonnacott, S. (1998) · Molecular Pharmacology · doi:10.1016/s0026-895x(24)13263-4 · Cited by 152 · see citing works
Roles of nicotinic acetylcholine receptor β subunits in function of human α4‐containing nicotinic receptors
Wu, J., Liu, Q., Yu, K., Hu, J., Kuo, Y., Segerberg, M., John, P. A. S., & Lukas, R. J. (2006) · The Journal of Physiology · doi:10.1113/jphysiol.2006.114645 · Cited by 73 · see citing works
Changes in Conformation and Subcellular Distribution of α4β2 Nicotinic Acetylcholine Receptors Revealed by Chronic Nicotine Treatment and Expression of Subunit Chimeras
Harkness, P. C., & Millar, N. S. (2002) · The Journal of Neuroscience · doi:10.1523/jneurosci.22-23-10172.2002 · Cited by 74 · see citing works
Characterization of the recombinant human neuronal nicotinic acetylcholine receptors α3β2 and α4β2 stably expressed in HEK293 cells
Chavez-Noriega, L. E., Gillespie, A. J., Stauderman, K. A., Crona, J. H., Claeps, B. O., Elliott, K. J., Reid, R. T., Rao, T. S., Veliçelebi, G., Harpold, M. M., et al. (2000) · Neuropharmacology · doi:10.1016/s0028-3908(00)00134-9 · Cited by 73 · see citing works
Functional Deactivation of the Major Neuronal Nicotinic Receptor Caused by Nicotine and a Protein Kinase C-Dependent Mechanism
Eilers, H., Schaeffer, E., Bickler, P. E., & Forsayeth, J. (1997) · Molecular Pharmacology · doi:10.1124/mol.52.6.1105 · Cited by 71 · see citing works
Ligand Binding and Activation of Rat Nicotinic α4β2 Receptors Stably Expressed in HEK293 Cells
Sabey, K., Paradiso, K. G., Zhang, J., & Steinbach, J. H. (1999) · Molecular Pharmacology · doi:10.1124/mol.55.1.58 · Cited by 66 · see citing works
Nicotine produces selective degeneration in the medial habenula and fasciculus retroflexus
Carlson, J. L., Noguchi, K., & Ellison, G. D. (2001) · Brain Research · doi:10.1016/s0006-8993(01)02570-7 · Cited by 65 · see citing works
Different nicotinic acetylcholine receptor subtypes mediating striatal and prefrontal cortical [3H]dopamine release
Cao, Y., Surowy, C. S., & Puttfarcken, P. S. (2004) · Neuropharmacology · doi:10.1016/j.neuropharm.2004.09.005 · Cited by 65 · see citing works
Pharmacological Comparison of Transient and Persistent [3H]Dopamine Release from Mouse Striatal Synaptosomes and Response to Chronic l-Nicotine Treatment
Grady, S. R., Grun, E. U., Marks, M. J., & Collins, A. C. (1997) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)36799-0 · Cited by 65 · see citing works
The nicotinic acetylcholine receptor partial agonist varenicline and the treatment of drug dependence: A review
Crunelle, C. L., Miller, M. L., Booij, J., & van den Brink, W. (2009) · European Neuropsychopharmacology · doi:10.1016/j.euroneuro.2009.11.001 · Cited by 63 · see citing works
Effects of neuronal nicotinic acetylcholine receptor allosteric modulators in animal behavior studies
Pandya, A. A., & Yakel, J. L. (2013) · Biochemical Pharmacology · doi:10.1016/j.bcp.2013.05.018 · Cited by 62 · see citing works
An uncontrolled trial of cytisine (Tabex) for smoking cessation: Table 1
Zatoński, W. A., Cedzyńska, M., Tutka, P., & West, R. (2006) · Tobacco Control · doi:10.1136/tc.2006.016097 · Cited by 61 · see citing works
Phantasmidine: An Epibatidine Congener from the Ecuadorian Poison Frog Epipedobates anthonyi
Fitch, R. W., Spande, T. F., Garraffo, H. M., Yeh, H. J. C., & Daly, J. W. (2010) · Journal of Natural Products · doi:10.1021/np900727e · Cited by 55 · see citing works
Modulatory Mechanism of the Endogenous Peptide Catestatin on Neuronal Nicotinic Acetylcholine Receptors and Exocytosis
Herrero, C. J., Alés, E., Pintado, A. J., López, M. G., García‐Palomero, E., Mahata, S. K., O’Connor, D. T., Garcı́a, A. G., & Montiel, C. (2002) · Journal of Neuroscience · doi:10.1523/jneurosci.22-02-00377.2002 · Cited by 55 · see citing works
Ibogaine: A Potent Noncompetitive Blocker of Ganglionic/Neuronal Nicotinic Receptors
Badio, B., Padgett, W. L., & Daly, J. W. (1997) · Molecular Pharmacology · doi:10.1124/mol.51.1.1 · Cited by 53 · see citing works
Characterization of Human Recombinant Neuronal Nicotinic Acetylcholine Receptor Subunit Combinations α2β4, α3β4 and α4β4 Stably Expressed in HEK293 Cells
Stauderman, K. A., Mahaffy, L. S., AKONG, M., Veliçelebi, G., Chavez-Noriega, L. E., Crona, J. H., Johnson, E. C., Elliott, K. J., Gillespie, A. J., Reid, R. T., et al. (1998) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)37270-2 · Cited by 90 · see citing works
Cholinergic drugs potentiate human nicotinic α4β2 acetylcholine receptors by a competitive mechanism
Smulders, C., Zwart, R., Bermúdez, I., van Kleef, R. G. D. M., Groot‐Kormelink, P. J., & Vijverberg, H. P. M. (2005) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2004.12.037 · Cited by 52 · see citing works
Pharmacology of Nicotinic Receptors in PreBötzinger Complex That Mediate Modulation of Respiratory Pattern
Shao, X. M., & Feldman, J. L. (2002) · Journal of Neurophysiology · doi:10.1152/jn.2002.88.4.1851 · Cited by 52 · see citing works
Functional characterization of mouse α4β2 nicotinic acetylcholine receptors stably expressed in HEK293T cells
Karadsheh, M. S., Shah, M. S., Tang, X., Macdonald, R. L., & Stitzel, J. A. (2004) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.2004.02801.x · Cited by 52 · see citing works
Allosteric Modulator Desformylflustrabromine Relieves the Inhibition of α2β2 and α4β2 Nicotinic Acetylcholine Receptors by β-Amyloid1–42 Peptide
Pandya, A. A., & Yakel, J. L. (2011) · Journal of Molecular Neuroscience · doi:10.1007/s12031-011-9509-3 · Cited by 47 · see citing works
Allosteric modulators of the α4β2 subtype of neuronal nicotinic acetylcholine receptors
Pandya, A. A., & Yakel, J. L. (2011) · Biochemical Pharmacology · doi:10.1016/j.bcp.2011.04.020 · Cited by 44 · see citing works
Chaperone protein 14‐3‐3 and protein kinase A increase the relative abundance of low agonist sensitivity human α4β2 nicotinic acetylcholine receptors in Xenopus oocytes
Exley, R. A., Moroni, M., Sasdelli, F., Houlihan, L. M., Lukas, R. J., Sher, E., Zwart, R., & Bermúdez, I. (2006) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.2006.03915.x · Cited by 43 · see citing works
Study of the calcium dynamics of the human α4β2, α3β4 and α1β1γδ nicotinic acetylcholine receptors
Michelmore, S., Croskery, K., Nozulak, J., Hoyer, D., Longato, R., Weber, A., Bouhelal, R., & Feuerbach, D. (2002) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-002-0589-z · Cited by 42 · see citing works
Recent developments in neuronal nicotinic acetylcholine receptor antagonists
Dwoskin, L. P., Xu, R., Ayers, J. T., & Crooks, P. A. (2000) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.10.10.1561 · Cited by 42 · see citing works
Characterization of nicotinic acetylcholine receptor-mediated [3H]-dopamine release from rat cortex and striatum
Puttfarcken, P. S., Jacobs, I. C., & Faltynek, C. R. (2000) · Neuropharmacology · doi:10.1016/s0028-3908(00)00131-3 · Cited by 41 · see citing works
Acetylcholine receptor extracellular domain determines sensitivity to nicotine-induced inactivation
Kuryatov, A., Olale, F., Choi, C. H., & Lindstrom, J. M. (2000) · European Journal of Pharmacology · doi:10.1016/s0014-2999(00)00027-3 · Cited by 41 · see citing works
Cytisine-like alkaloids from Ormosia hosiei Hemsl. & E.H. Wilson
Pouny, I., Batut, M., Vendier, L., David, B., Yi, S., Sautel, F., Arimondo, P. B., & Massiot, G. (2014) · Phytochemistry · doi:10.1016/j.phytochem.2014.07.022 · Cited by 39 · see citing works
Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT1a receptor antagonist
Pandya, A. A., & Yakel, J. L. (2013) · Neuropharmacology · doi:10.1016/j.neuropharm.2013.01.004 · Cited by 39 · see citing works
Progress and challenges in the study of α6-containing nicotinic acetylcholine receptors
Letchworth, S. R., & Whiteaker, P. (2011) · Biochemical Pharmacology · doi:10.1016/j.bcp.2011.06.022 · Cited by 39 · see citing works

Regulation of Human α4β2 Neuronal Nicotinic Acetylcholine Receptors by Cholinergic Channel Ligands and Second Messenger Pathways
Gopalakrishnan, M., Molinari, E. J., & Sullivan, J. P. (1997) · Molecular Pharmacology · doi:10.1124/mol.52.3.524 · Cited by 127 · see citing works
Characterization of Human α4β2-Nicotinic Acetylcholine Receptors Stably and Heterologously Expressed in Native Nicotinic Receptor-Null SH-EP1 Human Epithelial Cells
Eaton, J. B., Peng, J., Schroeder, K. M., George, A. A., Fryer, J. D., Krishnan, C., Buhlman, L. M., Kuo, Y.-P., Steinlein, O. K., & Lukas, R. J. (2003) · Molecular Pharmacology · doi:10.1124/mol.64.6.1283 · Cited by 117 · see citing works
Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations alpha2beta4, alpha3beta4 and alpha4beta4 stably expressed in HEK293 cells.
Stauderman, K. A., Mahaffy, L. S., Akong, M., Veliçelebi, G., Chavez-Noriega, L. E., Crona, J. H., Johnson, E. C., Elliott, K. J., Gillespie, A., Reid, R. T., et al. (1998) · PubMed · doi:10.7270/q28g8j7q · Cited by 86 · see citing works
The Comparative Pharmacology and Up-Regulation of Rat Neuronal Nicotinic Receptor Subtype Binding Sites Stably Expressed in Transfected Mammalian Cells
Xiao, Y., & Kellar, K. J. (2004) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.104.066787 · Cited by 148 · see citing works
Human α4β2 Neuronal Nicotinic Acetylcholine Receptor in HEK 293 Cells: A Patch-Clamp Study
Buisson, B., Gopalakrishnan, M., Arnerić, S. P., Sullivan, J. P., & Bertrand, D. (1996) · Journal of Neuroscience · doi:10.1523/jneurosci.16-24-07880.1996 · Cited by 183 · see citing works

Authors: Gopalakrishnan, M., Monteggia, L. M., Anderson, D. J., Molinari, E. J., Piattoni-Kaplan, M., Donnelly-Roberts, D., Arneric, S. P., & Sullivan, J. P.
Affiliations: Abbott (United States) (US)
ORCID: Gopalakrishnan, M
Monteggia, L M
Sullivan, J P
Venue: The Journal of Pharmacology and Experimental Therapeutics
Publisher: Elsevier BV
Published: 1996-01
Volume: 276
Issue: 1
Pages: 289-297
ISSN: 0022-3565 (ISSN-L)
DOI: 10.1016/s0022-3565(25)12264-7
OpenAlex: W2238918217
Cited by: 178
References: 0
Citations by year: 2024: 1 · 2023: 1 · 2022: 2 · 2021: 1 · 2020: 2 · 2017: 4 · 2016: 6 · 2015: 2 · 2014: 2 · 2013: 7 · 2012: 3
FWCI: 6.18
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Journal of Pharmacology and Experimental Therapeutics (publishedVersion)
PubMed (publishedVersion)
PubMed
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords: neuronal nicotinic acetylcholine receptors, alpha4beta2 nAChR, nicotine, 86Rb efflux, ion channel function, receptor desensitization, receptor resensitization, receptor internalization, receptor trafficking
MeSH terms: Quinolizidine Alkaloids, Alkaloids, Animals, Azocines, Base Sequence, Cells, Cultured, Humans, Kidney, Kinetics, Male, Molecular Sequence Data, Neurons, Nicotine, Quinolizines, Receptors, Nicotinic, RNA, Messenger, Stereoisomerism, Transfection, Tritium, Up-Regulation, Rats, Sprague-Dawley, DNA, Complementary, Nicotinic Agonists, Rats

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Stable expression, pharmacologic properties and regulation of the human neuronal nicotinic acetylcholine alpha 4 beta 2 receptor.

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