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Molecular Pharmacology

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Research ArticleArticle

Four Pharmacologically Distinct Subtypes of α4β2 Nicotinic Acetylcholine Receptor Expressed in Xenopus laevisOocytes

Ruud Zwart and Henk P. M. Vijverberg
Molecular Pharmacology December 1998, 54 (6) 1124-1131; DOI: https://doi.org/10.1124/mol.54.6.1124
Ruud Zwart
Research Institute of Toxicology, Utrecht University, Utrecht, The Netherlands
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Henk P. M. Vijverberg
Research Institute of Toxicology, Utrecht University, Utrecht, The Netherlands
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Abstract

Nicotinic receptors generally are presumed to consist of two α and three non-α subunits. We varied the relative levels of expression of the neuronal nicotinic α4 and β2 receptor subunits inXenopus laevis oocytes by nuclear injection of cDNAs coding for these subunits in α:β ratios of 9:1, 1:1, and 1:9. The sensitivities of the receptors to acetylcholine andd-tubocurarine were investigated in voltage-clamp experiments. For receptors expressed at the 9:1 and 1:1 α:β ratios, the EC50 value of acetylcholine is ∼60 μm. For the majority of the receptors expressed at the 1:9 α:β ratio, the sensitivity to acetylcholine is enhanced 30-fold. No evidence for more than one type of acetylcholine binding site in a single receptor is obtained. The sensitivity to d-tubocurarine decreases with decreasing α:β ratio. IC50 values ofd-tubocurarine are 0.2, 0.5, and 2 μm for the 9:1, 1:1, and 1:9 α:β ratios, respectively. At the 1:9 α:β ratio, additional receptors with an IC50 value of 163 μm d-tubocurarine are expressed. At least two components with distinct sensitivities tod-tubocurarine are required to account for the shift in IC50. The combined agonist and antagonist effects reveal four distinct subtypes of α4β2 nicotinic receptors. The results imply that the subunit stoichiometry of heteromeric α4β2 acetylcholine receptors is not restricted to 2α:3β.

Footnotes

    • Received May 18, 1998.
    • Accepted September 14, 1998.
  • Send reprint requests to: Dr. R. Zwart, Research Institute of Toxicology, Utrecht University, P.O. Box 80.176, NL-3508 TD Utrecht, The Netherlands. E-mail: r.zwart{at}ritox.vet.uu.nl

  • This work was financially supported by Netherlands Organization for Scientific Research (NWO) Grant 903–42-011.

  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 54 (6)
Molecular Pharmacology
Vol. 54, Issue 6
1 Dec 1998
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Research ArticleArticle

Four Pharmacologically Distinct Subtypes of α4β2 Nicotinic Acetylcholine Receptor Expressed in Xenopus laevisOocytes

Ruud Zwart and Henk P. M. Vijverberg
Molecular Pharmacology December 1, 1998, 54 (6) 1124-1131; DOI: https://doi.org/10.1124/mol.54.6.1124

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Research ArticleArticle

Four Pharmacologically Distinct Subtypes of α4β2 Nicotinic Acetylcholine Receptor Expressed in Xenopus laevisOocytes

Ruud Zwart and Henk P. M. Vijverberg
Molecular Pharmacology December 1, 1998, 54 (6) 1124-1131; DOI: https://doi.org/10.1124/mol.54.6.1124
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