Possible Interaction: Norepinephrine and Phenethylamines

“They have marked effects on the metabolism of over 15 different monoamines, including major brain neurotransmitters norepinephrine , dopamine, and serotonin) and on that of many other amines, which may act as co-transmitters, false transmitters, amine-releasing agents, or neuromodulators (e.g., tryptamine, tyramine, octopamine, and phenylethylamine).”

“ Phenylethylamine administration influences other neurotransmitters such as dopamine, norepinephrine and 5-hydroxytryptamine.”

“These trace amines, including phenethylamine , phenylethanolamine, tyramine and octopamine, are derived from phenylalanine and tyrosine, which are normally metabolized in the liver, and may interfere with neural transmission of noradrenaline and dopamine in the central and peripheral nervous systems [l].”

“The phenethylamine derivatives , 4-fluoroamphetamine, 2-methylamino-3,4-methylene-dioxy-propiophenone (methylone), 1-(1,3-benzodioxol-5-yl)-2-butanamine (BDB), and N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), had strong inhibitory effects on the re-uptake of dopamine, 5-HT and norepinephrine.”

“A neurotoxin, 5‐amino‐2,4‐dihydroxy‐α‐methylphenylethylamine , microinjected into the vicinity of the supraoptic nucleus, selectively depleted the noradrenaline contents of the nucleus and blocked the Fos expression in the supraoptic nucleus after the unconditioned or conditioned fear stimulus.”

“Dopamine, tyramine, 3-methyltyramine, and phenylethylamine also inhibited the activity while no particular effects were obtained by adrenaline, noradrenaline , tyrosine, and DOPA.”

“ Norepinephrine uptake could be inhibited by various phenethylamines and indoleamines following the rank order: reserpine > harmaline > 5‐hydroxytryptamine > dopamine > norepinephrine.”

“ Noradrenaline and related amines, e.g. metaraminol, are transported in adrenergic nerves by a carrier-mediated process that is inhibited by a number of phenethylamine derivatives including amphetamine (Iversen, 1967).”

“Some phenethylamine and tryptamine derivatives accelerated the efflux of [3H]noradrenaline , the most potent compounds studied /I-phenethylamine and amphetamine (Paton, 1973b, c; Paton & Pasternak, 1974).”

“The ability and … of a given phenethylamine derivative to accelerate … efflux of cytoplasmic noradrenaline is probably determined by such factors as the lipid solubility of the amine, the affinity of the amine … the uptake and efflux site(s) for noradrenaline, and competition for any reserpine-resistant intraneuronal binding sites.”

“There was a dissociation between the abilities of phenylethylamines to block the extra-and intraneuronal uptake of norepinephrine.”