2-[4-[イソプロピル(5,6-ジフェニルピラジン-2-イル)アミノ]ブトキシ]酢酸 化学特性,用途語,生産方法
説明
Prostacyclin (PGI
2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-
coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets. The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation. MRE-
269 is the active form of the prodrug NS-
304. It is a potent and selective agonist for the human IP receptor with a K
i value of 20 nM. In contrast to PGI
2, which has a half-
life of 30 seconds to a few minutes
in vivo, plasma concentrations of MRE-
269 remain near peak levels for more than eight hours in rats and dogs. Unlike the PGI
2 analogues, beraprost and iloprost, MRE-
269 lacks high affinity for the EP
3 receptor. As a result, MRE-
269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced
via EP
3-
mediated vasoconstriction.
使用
MRE-269 an orally available and long-acting prostacyclin receptor agonist prodrug. MRE-269 is used for the treatment of pulmonary arterial hypertension. MRE-269 is an active metabolite of Selexipag (S253150).
定義
ChEBI: A member of the class of pyrazines that is {4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetic acid carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. The active metabolite of selexipag, an orphan drug used for the treatm
nt of pulmonary arterial hypertension.
2-[4-[イソプロピル(5,6-ジフェニルピラジン-2-イル)アミノ]ブトキシ]酢酸 上流と下流の製品情報
原材料
準備製品