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Effects of Synthetic Cathinones on Brain Neurotransmitters

  • Krystyna Gołembiowska
  • Katarzyna Kamińska
Chapter
Part of the Current Topics in Neurotoxicity book series (Current Topics Neurotoxicity, volume 12)

Abstract

Synthetic cathinones are the β-keto analogs of amphetamines and synthetic derivatives of cathinone naturally present in the khat plant (Catha edulis). There is very little data on pharmacology of cathinone derivatives. Like amphetamines, cathinones exert their stimulant effects via increasing synaptic concentrations of dopamine (DA), noradrenaline (NA), and serotonin (5-HT), albeit at various potencies. These compounds interact with plasma membrane transporters for DA, NA, and 5-HT. Some designer cathinones target monoamine transporters like substrates, such as amphetamine, while others are their blockers, like cocaine. Substrates, but not blockers, stimulate non-exocytotic release of neurotransmitters by reversing the normal direction of the transporter flux. Blockers of transport proteins are capable of increasing the extracellular level of neurotransmitters by preventing their reuptake after release from monoaminergic neurons. This chapter provides an overview of effects of synthetic cathinones on brain neurotransmitter levels. In vivo microdialysis studies demonstrated that administration of cathinones produced a potent and dose-dependent increase in the extracellular DA and 5-HT levels in the rat nucleus accumbens, frontal cortex, and striatum. It appears that certain synthetic cathinones potently affect extracellular levels of brain monoaminergic neurotransmitters, which may contribute to psychostimulatory, entactogenic, and hallucinogenic effect of these drugs and brings about the risk of addiction.

Keywords

Dopamine Serotonin Release Microdialysis 

Notes

Acknowledgements

Supported by the National Science Centre (NCN), Cracow, Poland (grant no 2013/09/B/NZ7/04104).

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Copyright information

© Springer International Publishing AG, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Institute of PharmacologyPolish Academy of SciencesKrakówPoland

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