5-HT2A/5-HT2C Receptor Pharmacology and Intrinsic Clearance of N-Benzylphenethylamines Modified at the Primary Site of Metabolism.
ACS Chem Neurosci
; 7(11): 1614-1619, 2016 11 16.
Article
en En
| MEDLINE
| ID: mdl-27564969
ABSTRACT
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 analogues 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 analogues had an intrinsic clearance above 1.3 L/kg/h predictive of high first-pass metabolism.
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Banco de datos:
MEDLINE
Asunto principal:
Fenetilaminas
/
Agonistas del Receptor de Serotonina 5-HT2
Límite:
Humans
Idioma:
En
Revista:
ACS Chem Neurosci
Año:
2016
Tipo del documento:
Article
País de afiliación:
Dinamarca