98537-45-2Relevant articles and documents
5-HT2A/5-HT2C Receptor Pharmacology and Intrinsic Clearance of N-Benzylphenethylamines Modified at the Primary Site of Metabolism
Leth-Petersen, Sebastian,Petersen, Ida N.,Jensen, Anders A.,Bundgaard, Christoffer,B?k, Mathias,Kehler, Jan,Kristensen, Jesper L.
, p. 1614 - 1619 (2016/11/29)
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.
Ring-substituted β-methoxyphenethylamines: A new class of psychotomimetic agents active in man
Lemaire,Jacob III,Shulgin
, p. 575 - 577 (2007/10/02)
Four members of a new class of psychotomimetic agents have been synthesized and evaluated in man. These compounds, which incorporate a β-methoxy group onto a β-phenethylamine sidechain, are the first reported psychotomimetics which are structural analogues of the neurotransmitter noradrenaline. These substances are more potent than the corresponding phenethylamines (lacking a β-methoxy group) but less potent than the correspondingly substituted amphetamine derivatives.