grapiprant

Description: Grapiprant (formerly known as CJ-023, 423, RQ-00000007, or AAT-007) is a selective and potent EP4 receptor antagonist. It has potential antihyperalgesic properties. In vitro, CJ-023, 423 inhibits (3)H-labeled PGE(2) binding to both human and rat EP(4) receptors with K(i) of 13 +/- 4 and 20 +/- 1 nM, respectively. CJ-023, 423 is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. It also inhibits PGE(2)-evoked elevation in intracellular cAMP at the human and rat EP(4) receptors with pA(2) of 8.3 +/- 0.03 and 8.2 +/- 0.2 nM, respectively. In vivo, oral administration of CJ-023, 423 significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE(2) (ED(50) = 12.8 mg/kg).

References: JCI Insight. 2018 Feb 8; 3(3). pii: 97843; J Pharm Biomed Anal. 2016 Jan 25; 118:251-8.