The Interaction of Organic Cation Transporters 1-3 and PMAT with Psychoactive Substances

Julian Maier, Marco Niello, Deborah Rudin, Lynette C. Daws, Harald H. Sitte

Research output: Chapter in Book/Report/Conference proceedingChapter

13 Scopus citations


Organic cation transporters 1-3 (OCT1-3, SLC22A1-3) and the plasma membrane monoamine transporter (PMAT, SLC29A4) play a major role in maintaining monoaminergic equilibrium in the central nervous system. With many psychoactive substances interacting with OCT1-3 and PMAT, a growing literature focuses on characterizing their properties via in vitro and in vivo studies. In vitro studies mainly aim at characterizing compounds as inhibitors or substrates of murine, rat, and human isoforms. The preponderance of studies has put emphasis on phenylalkylamine derivatives, but ketamine and opioids have also been investigated. Studies employing in vivo (knockout) models mostly concentrate on the interaction of psychoactive substances and OCT3, with an emphasis on stress and addiction, pharmacokinetics, and sensitization to psychoactive drugs. The results highlight the importance of OCT3 in the mechanism of action of psychoactive compounds. Concerning in vivo studies, a veritable research gap concerning OCT1, 2, and PMAT exists. This review provides an overview and summary of research conducted in this field of research.

Original languageEnglish (US)
Title of host publicationHandbook of Experimental Pharmacology
PublisherSpringer Science and Business Media Deutschland GmbH
Number of pages16
StatePublished - 2021

Publication series

NameHandbook of Experimental Pharmacology
ISSN (Print)0171-2004
ISSN (Electronic)1865-0325


  • Amphetamine
  • Ketamine
  • New psychoactive substances
  • Opioids
  • Stress-addiction axis

ASJC Scopus subject areas

  • General Pharmacology, Toxicology and Pharmaceutics
  • Biochemistry


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