logo
Welcome Guest! To enable all features please Login or Register.

Notification

Icon
Error

Login


Options
View
Go to last post Go to first unread
goon2019  
#1 Posted : Thursday, July 04, 2019 11:01:12 PM(UTC)
goon2019

Rank: Advanced Member

Groups: Registered
Joined: 5/8/2019(UTC)
Posts: 1,470
China
Location: beijing

Grapiprant (Synonyms: CJ-023423; RQ-00000007; AAT-007)


Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). Target: prostaglandin receptor in vitro: Grapiprant is a novel pharmacologically active ingredient, acts as a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). [1] in vivo: Grapiprant is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis. [1] Results suggested the safety of long-term oral administration of grapiprant to dogs. Efficacy of grapiprant in the treatment of dogs with osteoarthritis needs to be evaluated in other studies. [2]

CJ-023,423 is also effective in models of acute and chronic inflammatory pain. CJ-023,423 significantly reduces mechanical hyperalgesia in the carrageenan model. Furthermore, CJ-023,423 significantly reverses complete Freund's adjuvant-induced chronic inflammatory pain response. Taken together, the present data indicate that CJ-023,423, a highly potent and selective antagonist of both human and rat EP(4) receptors, produces antihyperalgesic effects in animal models of inflammatory pain. Thus, specific blockade of the EP(4) receptor signaling may represent a novel therapeutic approach for the treatment of inflammatory pain.
Users browsing this topic
Guest
Forum Jump  
You cannot post new topics in this forum.
You cannot reply to topics in this forum.
You cannot delete your posts in this forum.
You cannot edit your posts in this forum.
You cannot create polls in this forum.
You cannot vote in polls in this forum.