TY - CHAP
T1 - The Interaction of Organic Cation Transporters 1-3 and PMAT with Psychoactive Substances
AU - Maier, Julian
AU - Niello, Marco
AU - Rudin, Deborah
AU - Daws, Lynette C.
AU - Sitte, Harald H.
N1 - Publisher Copyright:
© 2021, The Author(s), under exclusive license to Springer Nature Switzerland AG.
PY - 2021
Y1 - 2021
N2 - 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.
AB - 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.
KW - Amphetamine
KW - Ketamine
KW - New psychoactive substances
KW - Opioids
KW - Stress-addiction axis
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U2 - 10.1007/164_2021_469
DO - 10.1007/164_2021_469
M3 - Chapter
C2 - 33993413
AN - SCOPUS:85118421313
T3 - Handbook of Experimental Pharmacology
SP - 199
EP - 214
BT - Handbook of Experimental Pharmacology
PB - Springer Science and Business Media Deutschland GmbH
ER -