PMID: 9170145Apr 1, 1997Paper

Tryptamine: a possible endogenous substrate for CYP2D6

Pharmacogenetics
C MartínezJ Benítez

Abstract

The fact that CYP2D6 is not only expressed in liver but also in brain and the clinical association of this cytochrome with Parkinson's disease suggests the possibility of existence of some endogenous substrate, and among these perhaps one or more neurotransmitters could be metabolized by CYP2D6. In this study we explored such a possibility by studying the modulation of CYP2D6 activity by several neurotransmitters. Our findings confirm the occurrence of a competitive inhibition of dextromethorphan O-demethylation in the presence of tryptamine, with a Ki value of 44.6 microM. Tryptamine was metabolized in human liver microsomes by an enzyme activity with a K(m) of 3.6 +/- 0.9 microM. Such activity is NADPH dependent and is inhibited by quinidine and CYP2D6-specific substrates. The product of the reaction is tryptophol. These results suggest that tryptamine may be an endogenous substrate of CYP2D6.

Citations

Jul 30, 2008·Amino Acids·M SamuelssonC Nordin
Apr 30, 2005·Pharmacogenetics and Genomics·Nikolaos A PatsopoulosJohn P A Ioannidis
Jul 1, 1998·Environmental Health Perspectives·M A Rossing
Aug 11, 2004·Clinical Pharmacokinetics·Guillermo GervasiniJulio Benitez
Jan 1, 2014·European Journal of Pharmacology·Xiaoshuang WangJiang Yue
Mar 12, 2013·ISRN Pharmacology·Guillermo GervasiniJulio Benitez
May 9, 2002·Drug Metabolism Reviews·Slobodan Rendic
Jul 25, 2006·Expert Opinion on Drug Metabolism & Toxicology·James J CaliDavid Liu
Jul 9, 2004·Drug Metabolism Reviews·Ai-Ming YuFrank J Gonzalez
Jul 16, 2009·Drug Metabolism Reviews·Alan BoobisKeith Tipton
Sep 3, 2004·Journal of Clinical Pharmacology·Kiman KimHartmut Derendorf
Dec 25, 2004·Drug Metabolism and Pharmacokinetics·Yoshihiko FunaeToyoko Hiroi
Dec 24, 2002·The Journal of Pharmacy and Pharmacology·Władysława A DanielJ Wójcikowski
Oct 30, 2003·The Pharmacogenomics Journal·A LLerenaA De La Rubia
Jan 23, 2003·The Journal of Pharmacology and Experimental Therapeutics·Ai-Ming YuFrank J Gonzalez

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