78622-22-7Relevant academic research and scientific papers
Microsomal catalyzed N-hydroxylation of guanfacine and reduction of N-hydroxyguanfacine
Clement, Bernd,Demesmaeker, Mark
, p. 303 - 306 (2007/10/03)
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 the identification of the metabolite. The corresponding in vitro retroreduction of N-hydroxyguanfacine 2 was also investigated using the same set of enzyme sources. A new HPLC analytical method was developed in order to isolate and quantify the metabolites. A complete metabolic cycle involving the oxidative metabolism of guanfacine could only be observed in the presence of microsomal fractions from rabbit livers, whereas enzyme sources of all species under investigation catalyzed the N-reduction of N-hydroxyguanfacine 2.
Synthesis and properties of the tremor-inducing N-carbamoylacetamidine derivative LON-954 and some related compounds
Bream,Picard,White
, p. 175 - 179 (2007/10/02)
The synthesis of N-carbamoyl-2-(2,6-dichlorophenyl)acetamidine hydrochloride (LON-954; compound 5) and of some related N-carbamoyl-amidines is reported and structure-activity relationships within this series are discussed. The tremorogenic action of LON-9
