NDLI: Correlating the Metabolic Stability of Psychedelic 5-HT$_{2A}$ Agonists with Anecdotal Reports of Human Oral Bioavailability

Content Provider	Springer Nature Link
Author	Leth Petersen, Sebastian Bundgaard, Christoffer Hansen, Martin Carnerup, Martin A. Kehler, Jan Kristensen, Jesper Langgaard
Copyright Year	2014
Abstract	2,5-Dimethoxyphenethylamines and their N-benzylated derivatives are potent 5-HT$_{2A}$ agonists with psychedelic effects in humans. The N-benzylated derivatives are among the most selective 5-HT$_{2A}$ agonists currently available and their usage as biochemical and brain imaging tools is increasing, yet very little is known about the relationships between the structure of the ligands and their pharmacokinetic profile. In order to evaluate the potential of these compounds for in vivo applications we have determined the microsomal stability of 11 phenethylamines and 27 N-benzylated derivatives thereof using human liver microsomes. We found that the N-benzylated phenethylamines have much higher intrinsic clearance than the parent phenethylamines. We hypothesize that their low hepatic stability renders them orally inactive due to first pass metabolism, which is supported by anecdotal data from recreational use of these compounds.
Starting Page	2018
Ending Page	2023
Page Count	6
File Format	PDF
ISSN	03643190
Journal	Neurochemical Research
Volume Number	39
Issue Number	10
e-ISSN	15736903
Language	English
Publisher	Springer US
Publisher Date	2014-02-12
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Phenethylamines N-benzylphenethylamines Microsomal stability 5-HT$_{2A}$ agonists Psychedelics Neurosciences Neurochemistry Biochemistry Cell Biology Neurology
Content Type	Text
Resource Type	Article
Subject	Medicine Biochemistry Cellular and Molecular Neuroscience

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Erratum to: Correlating the Metabolic Stability of Psychedelic 5-HT$_{2A}$ Agonists with Anecdotal Reports of Human Oral Bioavailability

Erratum to: Correlating the Metabolic Stability of Psychedelic 5-HT2A Agonists with Anecdotal Reports of Human Oral Bioavailability

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Correlating the Metabolic Stability of Psychedelic 5-HT$_{2A}$ Agonists with Anecdotal Reports of Human Oral Bioavailability

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