Skip to main content
main-content

29.10.2018 | Psychiatry and Preclinical Psychiatric Studies - Review Article | Ausgabe 11/2018

Journal of Neural Transmission 11/2018

On the practical aspects of characterising monoamine oxidase inhibition in vitro

Zeitschrift:
Journal of Neural Transmission > Ausgabe 11/2018
Autor:
Andrew Holt

Abstract

The development of novel inhibitors of human monoamine oxidase enzymes with improved pharmacodynamic and pharmacokinetic profiles has, in the past, been hampered by limited access to enzyme, by assay protocols offering limited throughput, and by inappropriate analyses of kinetic data. More recently, high-level expression of human enzymes in yeast has facilitated thorough examinations of steady-state enzyme behaviour that have led to improvements in our understanding of the mathematical underpinnings of kinetic analyses of monoamine oxidases. However, with these improvements have come a realisation that to be useful, more data points across wider concentration ranges are required. In turn, many discontinuous assay approaches, such as those involving radiolabelled substrates or chromatographic separation of product from substrate, have been rendered somewhat obsolete. Justification for the use of a platereader-based approach to assess the effects of novel inhibitors on monamine oxidases is provided, along with details of experimental design optimised to address the unexpectedly complex kinetics followed by these enzymes. Potential sources of error are discussed, and comments provided on techniques that may enhance the quality of experimental data.

Bitte loggen Sie sich ein, um Zugang zu diesem Inhalt zu erhalten

★ PREMIUM-INHALT
e.Med Interdisziplinär

Mit e.Med Interdisziplinär erhalten Sie Zugang zu allen CME-Fortbildungen und Fachzeitschriften auf SpringerMedizin.de.

Jetzt e.Med zum Sonderpreis bestellen!

Sichern Sie sich jetzt Ihr e.Med-Abo und sparen Sie 50 %!

Weitere Produktempfehlungen anzeigen
Literatur
Über diesen Artikel

Weitere Artikel der Ausgabe 11/2018

Journal of Neural Transmission 11/2018 Zur Ausgabe

Neurology and Preclinical Neurological Studies - Review Article

The structure of monoamine oxidases: past, present, and future

Neurology and Preclinical Neurological Studies - Review Article

Kinetics, mechanism, and inhibition of monoamine oxidase

  1. Sie können e.Med Neurologie & Psychiatrie 14 Tage kostenlos testen (keine Print-Zeitschrift enthalten). Der Test läuft automatisch und formlos aus. Es kann nur einmal getestet werden.

  2. Sie können e.Med Neurologie 14 Tage kostenlos testen (keine Print-Zeitschrift enthalten). Der Test läuft automatisch und formlos aus. Es kann nur einmal getestet werden.