Tetrahydroaminoacridine inhibits human and rat brain monoamine oxidase

Abdu Adem, Sukhwinder S. Jossan, Lars Oreland

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44 Citations (Scopus)

Abstract

The inhibitory effects of 1,2,3,4-tetrahydro-9-aminoacridine (THA) on monoamine oxidase (MAO; EC 1.4.3.4) enzyme activities in human hippocampal and rat striatal homogenates have been studied. The activities of MAO-A and MAO-B were estimated radiochemically, in-vitro, in human hippocampus and rat striatum in the presence of various concentrations of THA with [2-14C]hydroxytryptamine binoxalate (100 μM) and β-[ethyl-14C]phenylethylamine hydrochloride (20 μM) as substrates for the respective enzyme form. THA was found to inhibit both MAO-A and MAO-B activities reversibly and competitively, with inhibition constants (Ki) of 12.5 μM and > 500 μM respectively, of the rat striatal enzymes. From this it can be extrapolated that at therapeutic tissue concentrations of THA (10-8 to 10-6 M), more than 20% of the MAO-A activity should be inhibited. Thus it is possible that inhibition of MAO may be involved in the therapeutic action of THA in Alzheimer's disease.

Original languageEnglish
Pages (from-to)313-317
Number of pages5
JournalNeuroscience Letters
Volume107
Issue number1-3
DOIs
Publication statusPublished - Dec 15 1989
Externally publishedYes

Keywords

  • Enzyme activity
  • Human brain
  • MAO-A
  • MAO-B
  • Monoamine oxidase
  • Tetrahydroaminoacridine

ASJC Scopus subject areas

  • General Neuroscience

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