The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors

Carla V. Rothlin, Eleonora Katz, Miguel Verbitsky, A. Belén Elgoyhen

Research output: Contribution to journalArticle

Abstract

In the present study, we provide evidence that the α9 nicotinic acetylcholine receptor (nAChR) shares pharmacological properties with members of the Cys-loop family of receptors. Thus, the type A γ-aminobutyric acid receptor antagonist bicuculline, the glycinergic antagonist strychnine, and the type 3 serotonin receptor antagonist ICS-205,930 block ACh-evoked currents in α9-injected Xenopus laevis oocytes with the following rank order of potency: strychnine > ICS-205,930 > bicuculline. Block by antagonists was reflected in an increase in the acetylcholine (ACh) EC50 value, with no changes in agonist maximal response or Hill coefficient, which suggests a competitive type of block. Moreover, whereas neither γ-aminobutyric acid nor glycine modified ACh-evoked currents, serotonin blocked responses to ACh in a concentration-dependent manner. The present results suggest that the α9 nAChR must conserve in its primary structure some residues responsible for ligand binding common to other Cys-loop receptors. In addition, it adds further evidence that the α9 nAChR and the cholinergic receptor present at the base of cochlear outer hair cells have similar pharmacological properties.

Original languageEnglish (US)
Pages (from-to)248-254
Number of pages7
JournalMolecular Pharmacology
Volume55
Issue number2
StatePublished - 1999
Externally publishedYes

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Aminobutyrates
Receptors, Serotonin, 5-HT3
tropisetron
Nicotinic Receptors
Glycine
Acetylcholine
Cysteine Loop Ligand-Gated Ion Channel Receptors
Pharmacology
Strychnine
Bicuculline
Outer Auditory Hair Cells
Serotonin Antagonists
Xenopus laevis
Cholinergic Receptors
Oocytes
Serotonin
Ligands

ASJC Scopus subject areas

  • Pharmacology

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The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors. / Rothlin, Carla V.; Katz, Eleonora; Verbitsky, Miguel; Belén Elgoyhen, A.

In: Molecular Pharmacology, Vol. 55, No. 2, 1999, p. 248-254.

Research output: Contribution to journalArticle

Rothlin, Carla V. ; Katz, Eleonora ; Verbitsky, Miguel ; Belén Elgoyhen, A. / The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors. In: Molecular Pharmacology. 1999 ; Vol. 55, No. 2. pp. 248-254.
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