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BIBTEX RIS

Control of the binding of a vesamicol analog to the vesicular acetylcholine transporter

1999; Lippincott Williams & Wilkins; Volume: 10; Issue: 13 Linguagem: Inglês

10.1097/00001756-199909090-00016

1473-558X

Alessandra D. Clarizia, Marcus V. Gomez, Marco Aurélio Romano‐Silva, Stanley M. Parsons, Vânia F. Prado, Marco A. M. Prado,

Cholinesterase and Neurodegenerative Diseases

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.