Designer psychostimulants: pharmacology and differences.
More than 200 novel psychoactive drugs have been reported in Europe, with 73 added in 2012 and additional compounds encountered every week in 2013. Many of these are "designer psychostimulants" which aim to mimic the subjective effects of amphetamines, cocaine or 3,4-methylenedioxymethylamphetamine (MDMA; "Ecstasy"). Several drugs are based on the beta-ketoamphetamine cathinone chemical structure, others include aminoindanes, aminotetralins, piperazines, amphetamine analogues and pipradrol derivatives. Although a detailed analysis of the pharmacology of these novel drugs is largely lacking, a number of scientific studies have been reported in 2011-2013 and these are reviewed. All of the novel psychostimulants activate monoamine systems in the brain - with differing dopamine (DA) v serotonin (5-HT) preferences. Those activating principally DA systems are amphetamine-like stimulants, such as naphyrone, desoxypipradrol, 3,4-methylenedioxypyrovalerone (MDPV), and benzylpiperazine while those preferentially activating 5-HT mechanisms are MDMA-like or cocaine-like stimulants, such as mephedrone, methylone and other substituted cathinones, aminoindanes, aminotetralins and piperazines. The ability of mephedrone and other novel psychostimulants to substitute for methylamphetamine or cocaine in drug discrimination tests in rats, and the ability of mephedrone to induce conditioned place preference and to sustain self-administration behaviour suggests that this and other cocaine/methylamphetamine-like drugs have dependence liability. This article is part of the Special Issue entitled 'CNS Stimulants'.
Department of Pharmacology, University of Oxford, Mansfield Road, OX1 3QT, UK. Electronic address: les.iversen@pharm.ox.ac.uk.
Leslie
L
Iversen
Forensic Adviser, Advisory Council on the Misuse of Drugs (ACMD) Secretariat, 2 Marsham Street, London SW1P 4DP, UK.
Michael
M
White
LGC Forensics, Queens Road, Teddington, London TW11 0LY, UK.
Ric
R
Treble
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D000697:Central Nervous System Stimulants / Q000737:chemistry / Q000494:pharmacology*; D015198:Designer Drugs / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D011619:Psychotropic Drugs / Q000737:chemistry / Q000494:pharmacology*
D000697:Central Nervous System Stimulants; D015198:Designer Drugs; D011619:Psychotropic Drugs
Amphetamine; Cathinones; Cocaine; Ecstasy; Mephedrone; Monoamine transporters