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Vol. 55, Issue 2, 248-254, February 1999
9 Nicotinic Acetylcholine Receptor Shares Pharmacological
Properties with Type A 
-Aminobutyric Acid, Glycine, and Type 3 Serotonin Receptors
Instituto de Investigaciones en Ingeniería Genética y
Biología Molecular, In the present study, we provide evidence that the 
9 nicotinic
acetylcholine receptor (nAChR) shares pharmacological properties with
members of the Cys-loop family of receptors. Thus, the type A
-aminobutyric acid receptor antagonist bicuculline, the glycinergic antagonist strychnine, and the type 3 serotonin receptor antagonist ICS-205,930 block ACh-evoked currents in 9-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 -aminobutyric acid nor glycine modified ACh-evoked
currents, serotonin blocked responses to ACh in a
concentration-dependent manner. The present results suggest that the
9 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 9 nAChR and the
cholinergic receptor present at the base of cochlear outer hair cells
have similar pharmacological properties.
Copyright © 1999 by The American Society for Pharmacology and Experimental Therapeutics
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