|Systematic (IUPAC) name|
|Mol. mass||192.30 g/mol|
Amiflamine (FLA-336) is a reversible inhibitor of monoamine oxidase A (MAO-A), thereby being a RIMA, and, to a lesser extent, semicarbazide-sensitive amine oxidase (SSAO), as well as a serotonin releasing agent (SRA). It is a derivative of the phenethylamine and amphetamine chemical classes. The (+)-enantiomer is the active stereoisomer.
Amiflamine is unique among MAOIs in that it 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.
- Ask AL, Högberg K, Schmidt L, Kiessling H, Ross SB (April 1982). "(+)-4-Dimethylamino-2,alpha-dimethylphenethylamine (FLA 336(+)), a selective inhibitor of the A form of monoamine oxidase in the rat brain".
- Fowler CJ, Eriksson M, Thorell G, Magnusson O (October 1984). "Stereoselective inhibition of monoamine oxidase and semicarbazide-sensitive amine oxidase by 4-dimethylamino-2,alpha-dimethylphenethylamine (FLA 336)". Naunyn-Schmiedeberg's Archives of Pharmacology 327 (4): 279–84.
- Morikawa F, Ueda T, Arai Y, Kinemuchi H (1986). "Inhibition of monoamine oxidase A-form and semicarbazide-sensitive amine oxidase by selective and reversible monoamine oxidase-A inhibitors, amiflamine and FLA 788(+)". Pharmacology 32 (1): 38–45.
- Ask AL, Fagervall I, Huang RB, Ross SB (June 1989). "Release of 3H-5-hydroxytryptamine by amiflamine and related phenylalkylamines from rat occipital cortex slices". Naunyn-Schmiedeberg's Archives of Pharmacology 339 (6): 684–9.
- Fowler CJ, Magnusson O, Ross SB (1984). "Intra- and extraneuronal monoamine oxidase". Blood Vessels 21 (3): 126–31.
- Ask AL, Fagervall I, Ross SB (September 1983). "Selective inhibition of monoamine oxidase in monoaminergic neurons in the rat brain". Naunyn-Schmiedeberg's Archives of Pharmacology 324 (2): 79–87.