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  • Title: Control of the binding of a vesamicol analog to the vesicular acetylcholine transporter.
    Author: Clarizia AD, Gomez MV, Romano-Silva MA, Parsons SM, Prado VF, Prado MA.
    Journal: Neuroreport; 1999 Sep 09; 10(13):2783-7. PubMed ID: 10511440.
    Abstract:
    4-Aminobenzovesamicol was used to test whether activation of protein kinase C protects the vesicular acetylcholine transporter from interaction with vesamicol-like drugs. The essentially irreversible vesamicol analog inhibits the release of newly synthesized [3H]acetylcholine from stimulated hippocampal slices. Prior activation of protein kinase C with a phorbol ester prevented the inhibition of [3H]acetylcholine release, but activation of protein kinase C after the exposure to the irreversible analog did not prevent the effect of the drug. Binding of 4-aminobenzovesamicol in hippocampal synaptosomes, assayed using [3H]vesamicol and back-titration, was decreased by activation of protein kinase C prior to analog exposure but not by activation subsequent to exposure. We propose that phosphorylation of the vesicular acetylcholine transporter prevents the binding of vesamicol-like drugs.
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