5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism

Research output: Contribution to journalJournal articleResearchpeer-review

Sebastian Leth-Petersen, Ida Nymann Petersen, Anders A Jensen, Christoffer Bundgaard, Mathias Bæk, Jan Kehler, Jesper L Kristensen

The toxic hallucinogen 25B-NBOMe is very rapidly degraded by human liver microsomes and has low oral bioavailability. Herein we report on the synthesis, microsomal stability and 5-HT2A/5-HT2C receptor profile of novel analogs of 25B-NBOMe modified at the primary site of metabolism. Although microsomal stability could be increased while maintaining potent 5-HT2 receptor agonist properties, all analogs had an intrinsic clearance above 1.3 L/kg/h predictive of high first-pass metabolism.

Original languageEnglish
JournalA C S Chemical Neuroscience
Pages (from-to)1-6
Number of pages6
ISSN1948-7193
DOIs
Publication statusPublished - 26 Aug 2016

ID: 164969052