ONO-8130 is an orally bioavailable antagonist of the prostaglandin E₂ (PGE₂) receptor EP₁ (K_i = 1.9 nM)^1,2 It exerts a more than 1,000-fold selectivity for EP₁ compared with other EP receptors.² ONO-8130 suppresses pain associated with cyclophosphamide-induced cystitis in mice at 0.3-30 mg/kg.¹ It also blocks PGE₂-induced contraction and eliminates spontaneous tone of guinea pig trachea tested in tissue organ baths.²

≥98%

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1.Miki, T.,Matsunami, M.,Nakamura, S., et al. ONO-8130, a selective prostanoid EP₁ receptor antagonist, relieves bladder pain in mice with cyclophosphamide-induced cystitis. Pain 152(6), 1373-1381 (2011).

2.Säfholm, J.,Dahlén, S.E.,Delin, I., et al. PGE₂ maintains the tone of the guinea pig trachea through a balance between activation of contractile EP₁ receptors and relaxant EP₂ receptors. British Journal of Pharmacology 168, 794-806 (2013).