223911-60-2Relevant academic research and scientific papers
Metabolism investigation leading to novel drug design: Orally active prostacyclin mimetics. Part 4
Hattori, Kouji,Takamura, Fujiko,Tanaka, Akira,Takasugi, Hisashi,Taniguchi, Kiyoshi,Nishio, Mie,Koyama, Satoshi,Seki, Jiro,Sakane, Kazuo
, p. 3284 - 3287 (2005)
A metabolism study of FR181157 (1) led to the discovery of new oxazole derivatives as active metabolites. The metabolite 6 with an epoxy ring exhibited high anti-aggregative potency with an IC50 of 5.8 nM and potent binding affinity for the human recombinant IP receptor with a Ki value of 6.1 nM and selectivity for human IP receptor over all other members of the human prostanoid receptor family.
