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AB Cachelin and G Rust
Department of Pharmacology, University of Berne, Switzerland.
We have investigated the functional properties of four rat neuronal nicotinic acetylcholine receptor types expressed in Xenopus oocytes after injection of pairwise combinations of mRNA encoding alpha 2 or alpha 3 receptor subunits with mRNA encoding beta 2 or beta 4 receptor subunits. Current responses evoked by rapid application of cholinergic agonists (acetylcholine, nicotine, or 1,1-dimethyl-4- phenylpiperazinium) were recorded from voltage-clamped oocytes. Substituting BaCl2 for CaCl2 in the external solution increased the apparent Kd values of beta 4 subunit-containing receptors for acetylcholine but decreased the apparent Kd values of beta 2 subunit- containing receptors. Inhibition curves for the cholinergic antagonist (+)-tubocurarine were measured in BaCl2 medium at low agonist concentrations. (+)-Tubocurarine was a competitive antagonist of acetylcholine at neuronal nicotinic acetylcholine receptors that coexpressed the beta 2 subunit; the estimated Kb values were 3.6 microM (alpha 2 beta 2 receptors) and 390 nM (alpha 3 beta 2 receptors). In contrast, (+)-tubocurarine enhanced the peak responses evoked by low acetylcholine concentrations at alpha 2 beta 4 and alpha 3 beta 4 neuronal nicotinic acetylcholine receptors, without being a partial agonist. The maximal increase was observed at 5 microM and 10 microM (+)-tubocurarine for alpha 2 beta 4 and alpha 3 beta 4 receptors, respectively. Higher (+)-tubocurarine concentrations inhibited cholinergic responses, thus yielding a "bell-shaped" concentration- response curve.
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