Bath salts, mephedrone, and methylenedioxypyrovalerone as emerging illicit drugs that will need targeted therapeutic intervention.
Advances in pharmacology (San Diego, Calif.) 2014 DOI: 10.1016/b978-0-12-420118-7.00015-9 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Keywords | Bath salts Dopamine transporter Mdpv Mephedrone Methamphetamine Methcathinone Methylenedioxypyrovalerone Methylone Serotonin transporter Α-aminophenones |
| Key findings | Argues that synthetic cathinones are not a pharmacologically or mechanistically uniform class: individual agents act primarily via the dopamine, norepinephrine, and/or serotonin transporters by releasing or inhibiting reuptake of these neurotransmitters, producing effects that can resemble methamphetamine, cocaine, or Ecstasy. Until valid structure-activity relationships are established, each cathinone must be evaluated case by case, and treatment of intoxication remains largely palliative. |
Abstract
The term "synthetic cathinones" is fairly new, but, although the abuse of synthetic cathinones is a recent problem, research on cathinone analogs dates back >100 years. One structural element cathinone analogs have in common is an α-aminophenone moiety. Introduction of amine and/or aryl substituents affords a large number of agents. Today, >40 synthetic cathinones have been identified on the clandestine market and many have multiple "street names." Many cathinone analogs, although not referred to as such until the late 1970s, were initially prepared as intermediates in the synthesis of ephedrine analogs. The cathinones do not represent a pharmacologically or mechanistically homogeneous class of agents. Currently abused synthetic cathinones are derived from earlier agents and seem to produce their actions primarily via the dopamine, norepinephrine, and/or serotonin transporter; that is, they either release and/or inhibit the reuptake of one or more of these neurotransmitters. The actions of these agents can resemble those of central stimulants such as methamphetamine, cocaine, and/or empathogens such as 1-(3,4-methylenedioxyphenyl)-2-aminopropane (Ecstasy) and/or produce other effects. Side effects are primarily of a neurological and/or cardiovascular nature. The use of the "and/or" term is emphasized because synthetic cathinones represent a broad class of agents that produce a variety of actions; the agents cannot be viewed as being pharmacologically equivalent. Until valid structure-activity relationships are formulated for each behavioral/mechanistic action, individual synthetic cathinones remain to be evaluated on a case-by-case basis. Treatment of synthetic cathinone intoxication requires more "basic science" research. At this time, treatment is mostly palliative.
Citations in the library
Cited by 10
- Stereochemistry of mephedrone neuropharmacology: enantiomer‐specific behavioural and neurochemical effects in rats British Journal of Pharmacology September 26, 2014
- Effect fingerprinting of new psychoactive substances (NPS): What can we learn from in vitro data? Pharmacology & Therapeutics February 1, 2018
- Novel Psychoactive Substances—Recent Progress on Neuropharmacological Mechanisms of Action for Selected Drugs Frontiers in Psychiatry August 18, 2017
- Awash in a sea of ‘bath salts’: implications for biomedical research and public health Addiction July 1, 2014
- Eutylone and Its Structural Isomers Interact with Monoamine Transporters and Induce Locomotor Stimulation ACS Chemical Neuroscience March 9, 2021
and 5 more in the library
Cites 10
- Toxicokinetics of Amphetamines: Metabolism and Toxicokinetic Data of Designer Drugs, Amphetamine, Methamphetamine, and Their N-Alkyl Derivatives Therapeutic Drug Monitoring April 1, 2002
- Contrasting effects of d-methamphetamine, 3,4-methylenedioxymethamphetamine, 3,4-methylenedioxypyrovalerone, and 4-methylmethcathinone on wheel activity in rats Drug and Alcohol Dependence June 3, 2012
- Mephedrone, compared with MDMA (ecstasy) and amphetamine, rapidly increases both dopamine and 5-HT levels in nucleus accumbens of awake rats British Journal of Pharmacology May 26, 2011
- Pharmacological examination of trifluoromethyl ring-substituted methcathinone analogs. European Journal of Pharmacology November 21, 2012
- The designer methcathinone analogs, mephedrone and methylone, are substrates for monoamine transporters in brain tissue. Neuropsychopharmacology December 14, 2011
and 5 more in the library