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

Producción científica: Chapter

15 Citas (Scopus)


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.

Idioma originalEnglish (US)
Título de la publicación alojadaHandbook of Experimental Pharmacology
EditorialSpringer Science and Business Media Deutschland GmbH
Número de páginas16
EstadoPublished - 2021

Serie de la publicación

NombreHandbook of Experimental Pharmacology
ISSN (versión impresa)0171-2004
ISSN (versión digital)1865-0325

ASJC Scopus subject areas

  • General Pharmacology, Toxicology and Pharmaceutics
  • Biochemistry


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