Microsomal CatalyzedN-Hydroxylation of Guanfacine and Reduction ofN-Hydroxyguanfacine
作者:Bernd Clement、Mark Demesmaeker
DOI:10.1002/ardp.19973300907
日期:——
Guanfacine 1 is a well known centrally acting α2‐adrenoceptor agonist with antihypertensive activity. The drug belongs to the guanidine class of compounds. The N‐oxidative biotransformation of guanfacine was investigated in vitro in the presence of hepatic microsomal fractions from rabbits, pigs, and humans. The N‐hydroxylated derivative N‐hydroxyguanfacine 2 had to be synthesized as reference for