SC-51089
Prostaglandin E (EP1) antagonist / Prostaglandin E2 (EP1 receptor) antagonist (pA2=6.5, guinea pig ileum muscle strip assay )1,4. Possesses analgesic activity in vivo (rodent ED50= 6.8 mg/kg)1,2,4. Does not inhibit COX11 and does not block PGE1 induced hyperalgesia3.
Biochemicals & reagents
146033-02-5
1) Hallinan et al. (1993), N-substituted dibenzoxazepines as analgesic PGE2 antagonists; J. Med. Chem., 36 3293 2) Malmberg et al. (1994), Antinociceptive effect of spinally delivered prostaglandin E receptor antagonists in the formalin test on rat; Neurosci. Lett., 173 193 3) Khasar et al. (1994), Comparison of prostaglandin E1- and prostaglandin E2 hyperalgesia in the rat; Neuroscience, 62 345 4) Hallinan et al. (1996), Aminoacetyl moiety as a potential surrogate for diacylhydrazine group of SC-51089, a potent PGE2 antagonist, and its analogs; J. Med. Chem., 39 609
RT
TARGET: GPCR -- PATHWAY: Lipid signaling -- DISEASE AREA: Inflammation