title: Amphetamines, new psychoactive drugs and the monoamine transporter cycle.
abstract: In monoaminergic neurons, the vesicular transporters and the plasma membrane transporters operate in a relay. Amphetamine and its congeners target this relay to elicit their actions: most amphetamines are substrates, which pervert the relay to elicit efflux of monoamines into the synaptic cleft. However, some amphetamines act as transporter inhibitors. Both compound classes elicit profound psychostimulant effects, which render them liable to recreational abuse. Currently, a surge of new psychoactive substances occurs on a global scale. Chemists bypass drug bans by ingenuous structural variations, resulting in a rich pharmacology. A credible transport model must account for their distinct mode of action and link this to subtle differences in activity and undesired, potentially deleterious effects.
authors.affiliation: Institute of Pharmacology, Center for Physiology and Pharmacology, Medical University Vienna, Waehringerstrasse 13A, 1090 Vienna, Austria; Center for Addiction Research and Science (AddRess), Medical University Vienna, Waehringerstrasse 13A, 1090 Vienna, Austria. Electronic address: harald.sitte@meduniwien.ac.at.
authors.forename: Harald H
authors.initials: HH
authors.lastname: Sitte
authors.affiliation: Institute of Pharmacology, Center for Physiology and Pharmacology, Medical University Vienna, Waehringerstrasse 13A, 1090 Vienna, Austria.
authors.forename: Michael
authors.initials: M
authors.lastname: Freissmuth
mesh_terms: D000662:Amphetamines / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001692:Biological Transport; D006801:Humans; D050480:Plasma Membrane Neurotransmitter Transport Proteins / Q000378:metabolism*; D011619:Psychotropic Drugs / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000662:Amphetamines; D050480:Plasma Membrane Neurotransmitter Transport Proteins; D011619:Psychotropic Drugs
keywords: addiction; amphetamine; monoamine transporter; psychostimulant; regulation; reverse transport