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Molecular Pharmacology

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Research ArticleArticle

Effects of Quinine, Quinidine, and Chloroquine on α9α10 Nicotinic Cholinergic Receptors

Jimena A. Ballestero, Paola V. Plazas, Sebastian Kracun, María E. Gómez-Casati, Julián Taranda, Carla V. Rothlin, Eleonora Katz, Neil S. Millar and A. Belén Elgoyhen
Molecular Pharmacology September 2005, 68 (3) 822-829; DOI: https://doi.org/10.1124/mol.105.014431
Jimena A. Ballestero
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Paola V. Plazas
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Sebastian Kracun
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María E. Gómez-Casati
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Julián Taranda
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Carla V. Rothlin
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Eleonora Katz
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Neil S. Millar
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A. Belén Elgoyhen
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Abstract

In this study, we report the effects of the quinoline derivatives quinine, its optical isomer quinidine, and chloroquine on α9α10-containing nicotinic acetylcholine receptors (nAChRs). The compounds blocked acetylcholine (ACh)-evoked responses in α9α10-injected Xenopus laevis oocytes in a concentration-dependent manner, with a rank order of potency of chloroquine (IC50 = 0.39 μM) > quinine (IC50 = 0.97 μM) ∼ quinidine (IC50 = 1.37 μM). Moreover, chloroquine blocked ACh-evoked responses on rat cochlear inner hair cells with an IC50 value of 0.13 μM, which is within the same range as that observed for recombinant receptors. Block by chloroquine was purely competitive, whereas quinine inhibited ACh currents in a mixed competitive and noncompetitive manner. The competitive nature of the blockage produced by the three compounds was confirmed by equilibrium binding experiments using [3H]methyllycaconitine. Binding affinities (Ki values) were 2.3, 5.5, and 13.0 μM for chloroquine, quinine, and quinidine, respectively. Block by quinine was found to be only slightly voltage-dependent, thus precluding open-channel block as the main mechanism of interaction of quinine with α9α10 nAChRs. The present results add to the pharmacological characterization of α9α10-containing nicotinic receptors and indicate that the efferent olivocochlear system that innervates the cochlear hair cells is a target of these ototoxic antimalarial compounds.

  • Received May 3, 2005.
  • Accepted June 13, 2005.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 68 (3)
Molecular Pharmacology
Vol. 68, Issue 3
1 Sep 2005
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Research ArticleArticle

Effects of Quinine, Quinidine, and Chloroquine on α9α10 Nicotinic Cholinergic Receptors

Jimena A. Ballestero, Paola V. Plazas, Sebastian Kracun, María E. Gómez-Casati, Julián Taranda, Carla V. Rothlin, Eleonora Katz, Neil S. Millar and A. Belén Elgoyhen
Molecular Pharmacology September 1, 2005, 68 (3) 822-829; DOI: https://doi.org/10.1124/mol.105.014431

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Research ArticleArticle

Effects of Quinine, Quinidine, and Chloroquine on α9α10 Nicotinic Cholinergic Receptors

Jimena A. Ballestero, Paola V. Plazas, Sebastian Kracun, María E. Gómez-Casati, Julián Taranda, Carla V. Rothlin, Eleonora Katz, Neil S. Millar and A. Belén Elgoyhen
Molecular Pharmacology September 1, 2005, 68 (3) 822-829; DOI: https://doi.org/10.1124/mol.105.014431
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