amiflamine
Sign in to saveAlso known as FLA-336
Amiflamine (developmental code name FLA-336), also known '(S)-2-methyl-4-(dimethylamino)amphetamine', is a reversible inhibitor of monoamine oxidase A (MAO-A), thereby being a RIMA, and, to a lesser extent, semicarbazide-sensitive amine oxidase (SSAO) inhibitor, as well as a serotonin releasing agent (SRA). It is a derivative of the phenethylamine and amphetamine families. The (+)-enantiomer is the active stereoisomer.
Research
51 papers- Relationship of N-demethylation of amiflamine and its metabolite to debrisoquine hydroxylation polymorphism.Clinical pharmacology and therapeutics · 1984
- Pressor response of oral tyramine in healthy men given amiflamine and placebo.Clinical pharmacology and therapeutics · 1986
- Selective inhibition by amiflamine of monoamine oxidase type A in rat brain, liver and duodenum.Naunyn-Schmiedeberg's archives of pharmacology · 1984
- Effects of amiflamine and related compounds on the accumulation of biogenic monoamines in rat brain slices in vitro and ex vivo in relation to their behavioural effects.Acta pharmacologica et toxicologica · 1985
- Effect of repeated amiflamine administration on serotonergic and noradrenergic neurotransmission: electrophysiological studies in the rat CNS.Naunyn-Schmiedeberg's archives of pharmacology · 1986
via PubMed
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Encyclopedic overview
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Amiflamine (developmental code name FLA-336), also known '(S)-2-methyl-4-(dimethylamino)amphetamine', is a reversible inhibitor of monoamine oxidase A (MAO-A), thereby being a RIMA, and, to a lesser extent, semicarbazide-sensitive amine oxidase (SSAO) inhibitor, as well as a serotonin releasing agent (SRA). It is a derivative of the phenethylamine and amphetamine families. The (+)-enantiomer is the active stereoisomer.
Amiflamine shows preference for inhibiting MAO-A in serotonergic relative to noradrenergic and dopaminergic neurons. In other words, at low doses, it can be used to selectively inhibit MAO-A enzymes in serotonin cells, whereas at higher doses it loses its selectivity. This property is attributed to amiflamine's higher affinity for the serotonin transporter over the norepinephrine and dopamine transporters, as transporter-mediated carriage is required for amiflamine to enter monoaminergic neurons.
Excerpted from Wikipedia’s “amiflamine” article, available under the CC BY-SA 4.0 licence.