Format

Send to

Choose Destination
Trends Pharmacol Sci. 2015 Jan;36(1):41-50. doi: 10.1016/j.tips.2014.11.006. Epub 2014 Dec 23.

Amphetamines, new psychoactive drugs and the monoamine transporter cycle.

Author information

1
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.
2
Institute of Pharmacology, Center for Physiology and Pharmacology, Medical University Vienna, Waehringerstrasse 13A, 1090 Vienna, Austria.

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.

KEYWORDS:

addiction; amphetamine; monoamine transporter; psychostimulant; regulation; reverse transport

PMID:
25542076
PMCID:
PMC4502921
DOI:
10.1016/j.tips.2014.11.006
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Elsevier Science Icon for PubMed Central
Loading ...
Support Center