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 muM PPZ and 20-30 muM TFP. Evidence is presented that this phenomenon is driven by the formation of nonfluorescent 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 noncompetitive 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.

Spinedi A., P.L. (1992). Phenothiazines inhibit acetylcholinesterase by concentration-dependent-type kinetics. A study with trifluoperazine and perphenazine. BIOCHEMICAL PHARMACOLOGY, 44(8), 1511-1514 [10.1016/0006-2952(92)90465-U].

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

SPINEDI, ANGELO;LULY, PAOLO;
1992

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 muM PPZ and 20-30 muM TFP. Evidence is presented that this phenomenon is driven by the formation of nonfluorescent 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 noncompetitive 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.
Pubblicato
Rilevanza internazionale
Articolo
Sì, ma tipo non specificato
Settore BIO/09
English
Con Impact Factor ISI
acetylcholinesterase; erythrocyte enzyme; fluorescent dye; perphenazine; phenothiazine derivative; trifluoperazine; article; cholinesterase inhibition; controlled study; drug concentration; enzyme kinetics; erythrocyte; fluorescence spectroscopy; human; human cell; micelle; priority journal; Acetylcholinesterase; Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Erythrocytes; Fluorescent Dyes; Human; Kinetics; Perphenazine; Support, Non-U.S. Gov't; Temperature; Trifluoperazine
Spinedi A., P.L. (1992). Phenothiazines inhibit acetylcholinesterase by concentration-dependent-type kinetics. A study with trifluoperazine and perphenazine. BIOCHEMICAL PHARMACOLOGY, 44(8), 1511-1514 [10.1016/0006-2952(92)90465-U].
Spinedi, A; Pacini, L; Limatola, C; Luly, P; Farias, Rn
Articolo su rivista
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2108/54839
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? ND
social impact