Cetiedil, a Drug That Inhibits Acetylcholine Release in Torpedo Electric Organ

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Abstract
The effects of cetiedil, a vasodilatator substance with reported anticholinergic properties, were examined on cholinergic pesynaptic functions at the nerve electroplaque junction of Torpedo marmorata using either synaptosomes or slice soft intact tissues. Cetiedil abolished the calcium-dependent release of acetycholine (ACh) triggered by depolarization or by addition of A23187 ionophore, a finding localizing the site of cation downstream from the calcium entry step. In addition, a direct effect on the release process itself was indicated by the observation that cetiedil blocks the release of ACh mediated by a recently isolated presynaptic membrane protein, the mediatophore, reconstituted into ACh-containing proteoliposomes. In all three preparations, ACh release was inhibited by cetiedil with a Ki of 5-8 .mu.M. Under the conditions used in these release experiments, the synthesis of ACh and its compartmentation within the nerve terminal were not modified. However, the drug was able to reduce high-affinity choline uptake and vesicular ACh incorporation when it was given together with the radioactive precursor, a result showing that cetiedil has a broad inhibitory action on cholinergic uptake processes.

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