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Molecular Pharmacology

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Research ArticleArticle

The Novel α7β2-nicotinic Acetylcholine Receptor Subtype is Expressed in Mouse and Human Basal Forebrain: Biochemical and Pharmacological Characterisation

Milena Moretti, Michele Zoli, Andrew A George, Ronald J Lukas, Francesco Pistillo, Uve Maskos, Paul Whiteaker and Cecilia Gotti
Molecular Pharmacology July 8, 2014, mol.114.093377; DOI: https://doi.org/10.1124/mol.114.093377
Milena Moretti
1 CNR, Neuroscience Institute-Milano, Biometra University of Milan;
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Michele Zoli
2 Department of Biomedical, Metabolic and Neural Sciences, section of Physiology and Neurosciences, U;
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Andrew A George
3 Division of Neurobiology, Barrow Neurological Institute;
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Ronald J Lukas
4 Division of Neurobiology, Barrow Neurological Institute, Phoenix;
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Francesco Pistillo
5 CNR, Neuroscience Institute;
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Uve Maskos
6 Institut Pasteur, Paris, France;
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Paul Whiteaker
4 Division of Neurobiology, Barrow Neurological Institute, Phoenix;
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Cecilia Gotti
7 Neuroscience Institute
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Abstract

We examined α7β2-nicotinic acetylcholine receptor (α7β2-nAChR) expression in mammalian brain and compared pharmacological profiles of homomeric α7-nAChR and of α7β2-nAChR. α-Bugarotoxin affinity purification or immunoprecipitation with anti-α7 subunit antibodies (Abs) were used to isolate nAChR containing α7 subunits from rat or human brain samples. α7β2-nAChR were detected in forebrain, but not other tested regions, from both species, based on western blot analysis of isolates using β2 subunit-specific Abs. Abs specificity was confirmed in control studies using subunit-null mutant mice or cell lines heterologously expressing specific, human nAChR subtypes and subunits. Functional expression in Xenopus oocytes of concatenated pentameric (α7)5-, (α7)4(β2)1-, and (α7)3(β2)2-nAChR was confirmed using two-electrode voltage-clamp recording of responses to nicotinic ligands. Importantly pharmacological profiles were indistinguishable for concatenated (α7)5-nAChR or for homomeric α7-nAChR constituted from unlinked α7 subunits. Pharmacological profiles were similar for (α7)5-, (α7)4(β2)1-, and (α7)3(β2)2-nAChR except for diminished efficacy of nicotine (normalized to acetylcholine efficacy) at α7β2- vs. α7-nAChR. This study represents the first direct confirmation of α7β2-nAChR expression in human and mouse forebrain, supporting previous mouse studies that suggested relevance of α7β2-nAChR in Alzheimer's disease etiopathogenesis. These data also indicate that α7β2-nAChR subunit isoforms with different α7:β2 subunit ratios have similar pharmacological profiles to each other, and to α7 homopentameric nAChR. This supports the hypothesis that α7β2-nAChR agonist activation predominantly or entirely reflects binding to α7/α7 subunit interface sites.

  • Nicotinic cholinergic
  • Func. analysis receptor/ion channel mutants
  • Immunocytochemistry
  • Mutagenesis/Chimeric approaches
  • Receptor binding studies
  • Overexpression
  • Neurodegeneration
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 103 (6)
Molecular Pharmacology
Vol. 103, Issue 6
1 Jun 2023
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Research ArticleArticle

The Novel α7β2-nicotinic Acetylcholine Receptor Subtype is Expressed in Mouse and Human Basal Forebrain: Biochemical and Pharmacological Characterisation

Milena Moretti, Michele Zoli, Andrew A George, Ronald J Lukas, Francesco Pistillo, Uve Maskos, Paul Whiteaker and Cecilia Gotti
Molecular Pharmacology July 8, 2014, mol.114.093377; DOI: https://doi.org/10.1124/mol.114.093377

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Research ArticleArticle

The Novel α7β2-nicotinic Acetylcholine Receptor Subtype is Expressed in Mouse and Human Basal Forebrain: Biochemical and Pharmacological Characterisation

Milena Moretti, Michele Zoli, Andrew A George, Ronald J Lukas, Francesco Pistillo, Uve Maskos, Paul Whiteaker and Cecilia Gotti
Molecular Pharmacology July 8, 2014, mol.114.093377; DOI: https://doi.org/10.1124/mol.114.093377
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