Potent, highly selective and orally available agonist for the PGI2 receptor (IP receptor); nonprostanoid IP receptor agonist
Selexipag is a potent, highly selective and orally available nonprostanoid agonist for the PGI2 receptor (IP receptor). Selexipag is readily hydrolyzed to the active metabolite ACT-333679 (MRE-269), which is also a potent and selective agonist at IP receptors. In contrast to the prostacyclin analogs iloprost and beraprost, selexipag and metabolite ACT-333679 does not contract gastric fundus up to mM concentrations.
2-{4-[(5,6-Diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), an Orally Available and Long-Acting Prostacyclin Receptor Agonist Prodrug
Journal of Pharmacology and Experimental Therapeutics, 322, 1181-1188 (2007)
A long-acting and highly selective prostacyclin receptor agonist prodrug, 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responses of its active form, {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid (MRE-269), on rat pulmonary artery
Journal of Pharmacology and Experimental Therapeutics, 326(3), 691-699 (2008)
The Journal of pharmacology and experimental therapeutics, 335(1), 249-255 (2010-07-28)
Selexipag [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide] is an orally available prostacyclin (PGI(2)) receptor (IP receptor) agonist that is chemically distinct from PGI(2) and is in clinical development for the treatment of pulmonary arterial hypertension. Selexipag is highly selective for the human IP receptor in
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