Phenothiazines inhibit acetylcholinesterase by concentration-dependent-type kinetics. A study with trifluoperazine and perphenazine

Angelo Spinedi, Laura Pacini, Cristina Limatola, Paolo Luly, Ricardo N. Farias

Research output: Contribution to journalArticle

Abstract

The properties of perphenazine (PPZ) and trifluoperazine (TFP) as fluorescent dyes were exploited to calculate their critical micellar concentrations. The relative fluorescence quantum yield of the two amphiphiles was dependent on their concentration, abruptly decreasing above 30-40 μM PPZ and 20-30 μM TFP. Evidence is presented that this phenomenon is driven by the formation of non-fluorescent drug aggregates. The type of inhibition kinetics displayed by PPZ and TFP on human erythrocyte acetylcholinesterase (AChE) was also dependent on drug concentration, turning from non-competitive to a "mixed" inhibition type at concentrations at which PPZ and TFP were demonstrated to undergo micelle formation. Results support the notion that phenothiazines may interact with AChE both as monomers and micellar aggregates, producing different inhibitory effects.

Original languageEnglish
Pages (from-to)1511-1514
Number of pages4
JournalBiochemical Pharmacology
Volume44
Issue number8
DOIs
Publication statusPublished - Oct 20 1992

ASJC Scopus subject areas

  • Pharmacology

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