PMID: 7088264Apr 1, 1982Paper

Selective inhibition of the A form of monoamine oxidase by 4-dimethylamino-alpha-methylphenylalkylamine derivatives in the rat

Neuropharmacology
A L AskS B Ross

Abstract

The inhibitory effects on monoamine oxidase (MAO) of some dimethylamino-alpha-phenylalkylamine derivatives were examined in a rat brain mitochondrial preparation in vitro and in rat brain slices following oral administration. In the in vitro assay the compounds were shown to be selective inhibitors of the A form of MAO, being 100-600 times more potent in inhibiting the deamination of [14C]5-hydroxytryptamine than that of [14C]phenetylamine. Using an ex vivo brain slice technique it was found that the new compounds were reversible and very selective inhibitors of type A MAO in the rat brain and the most potent compounds (FLA 405, 314, 336 and 558) were equipotent with clorgyline. The compounds increased the monoamine concentrations in whole rat brain, particularly that of 5-hydroxytryptamine, in the same dose range which produced MAO inhibition. Some of the new compounds, e.g. FLA 336 and FLA 717, caused only weak potentiation of the vaso-pressor effect of orally administered tyramine.

Citations

Aug 1, 1984·Naunyn-Schmiedeberg's Archives of Pharmacology·A L Ask
Mar 26, 1985·European Journal of Pharmacology·N A GarrickD L Murphy
Jun 1, 1985·Journal of Pharmacological Methods·A Morinan, H M Garratt
Jan 1, 1983·Biochemical Pharmacology·M S BenedettiC J Fowler
Apr 1, 1986·Cell Biochemistry and Function·B A Callingham
Feb 11, 2020·Frontiers in Pharmacology·Miguel Reyes-ParadaBruce K Cassels
Jun 15, 1987·The Medical Journal of Australia·B Jarrott, F J Vajda

Related Concepts

Deamination
Intropin
Organum Vasculosum Laminae Terminalis
Mitochondria
Monoamine Oxidase
RIMA (Reversible Inhibitor of Monoamine Oxidase A)
Norepinephrine, (+, -)-Isomer
Phenethylamines
August Rats
Hydroxytryptamine

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