Specific antagonists at the pyridine receptor: evidence from electrophysiological studies with acetylpyridines

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Abstract
The effect of structural isomers of acetylpyridine on the response of single pyridine-sensitive cells was investigated electrophysiologically. 4-Acetylpyridine was identified as a strong specific inhibitor of the response to pyrazine-carboxamide, the most effective stimulant. When 4-acetylpyridine was present in the concentration range from 5 × 10 -5 to 5 × 10 -2 mol/l, the dose-response curves were shifted to the right, the slope and the common saturation level remaining unchanged. This effect can be interpreted as a competitive inhibition. It was also consistent with competitive antagonism that the Schild plot of these data was linear with a slope close to 1 (0.90). Linear regression indicated an inhibition constant K 1 = 40 μmol. 2-Acetylpyridine had a less potent antagonistic effect and an agonistic effect only at high concentrations (>10 −3 mol/1).

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