Structure-Activity Relationship of Synthetic Cathinones: An Updated Review

Núria Nadal-Gratacós*, Martalu D. Pazos, David Pubill, Jorge Camarasa, Elena Escubedo, Xavier Berzosa, Raúl López-Arnau

*Corresponding author for this work

Research output: Indexed journal article Reviewpeer-review

1 Citation (Scopus)

Abstract

The escalating prevalence of new psychoactive substances (NPSs) poses a significant public health challenge, evidenced by the vast chemical diversity, with over 500 substances reported annually to the United Nations Office on Drugs and Crime-Early Warning Advisory (UNODC-EWA) in the past five years. Among NPSs, synthetic cathinones are gaining a lot of popularity among users. Notably, synthetic cathinones accounted for approximately 50% of the total quantity of NPSs reported as seized by EU Member States in 2021. Preliminary data from UNODC indicates that a total of 209 synthetic cathinones have been reported to date. As their popularity grows, studying the structure-activity relationship (SAR) of synthetic cathinones is essential. SAR studies elucidate how structural features impact biological effects, aiding in toxicity prediction, regulatory compliance, and forensic identification. Additionally, SAR studies play a pivotal role in guiding drug policies, aiding authorities in categorizing and regulating newly emerging synthetic cathinones, mitigate public health risks and offer valuable insights into potential therapeutic applications. Thus, our Review consolidates recent findings on the effects of different substitutions in the chemical scaffold of synthetic cathinones on their mechanism of action as well as pharmacological and toxicological effects of synthetic cathinones, thus enhancing understanding of the SAR of synthetic cathinones’ pharmacology and potential implications.

Original languageEnglish
Pages (from-to)2588-2603
Number of pages16
JournalACS Pharmacology and Translational Science
Volume7
Issue number9
DOIs
Publication statusPublished - 13 Sept 2024

Keywords

  • cytotoxicity
  • new psychoactive substances
  • psychostimulant
  • reward
  • structure−activity relationship
  • synthetic cathinones

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