5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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.
Originalsprog | Engelsk |
---|---|
Tidsskrift | A C S Chemical Neuroscience |
Sider (fra-til) | 1-6 |
Antal sider | 6 |
ISSN | 1948-7193 |
DOI | |
Status | Udgivet - 26 aug. 2016 |
ID: 164969052