Monoamine Transporter and Receptor Interaction Profiles of Synthetic Cathinones

  • Linda D. Simmler
Part of the Current Topics in Neurotoxicity book series (Current Topics Neurotoxicity, volume 12)


Cathinones are amphetamine-type substances with a β-keto substitution, typically emerging as drugs of abuse among novel psychoactive substances (NPS). In vitro screenings have been useful in characterizing pharmacological profiles of cathinone NPS and in obtaining fast estimates of mechanisms of action, potencies, and potential toxicity. Pharmacological targets of cathinone psychostimulants are dopamine, serotonin, and noradrenaline re-uptake transporters (DAT, SERT, and NET, respectively), as well as monoamine receptors. However, there are considerable differences among cathinones with respect to potencies and relative activity at monoaminergic targets. Foremost, cathinones act on NET, DAT, and/or SERT as inhibitors, usually also inducing reverse transport of monoamines. For many cathinones, it is difficult to predict pharmacological profiles, and consequently to anticipate acute effects, doses, and toxicity, based solely on their chemical structures. In vitro screening and pharmacological classification are therefore essential in providing translationally valuable information promptly after new cathinone derivatives emerge among drug users. This chapter provides an overview of the pharmacological profiles of NPS cathinones, which have been characterized in in vitro screenings.


Affinity Cathinone DAT Dopamine NET Noradrenaline Monoamines Pharmacological profiles Release Serotonin SERT Synthetic cathinones Uptake 



The author would like to thank Dr. Shannon L. Wolfman for proofreading the manuscript. The author is supported by the Swiss National Science Foundation (PZ00P3_174178).


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© Springer International Publishing AG, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Department of Basic NeurosciencesUniversity of GenevaGenevaSwitzerland

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