SC-51089 is a selective antagonist of prostaglandin E2, which displays specificity towards the EP1 receptor subtype. Studies indicate that SC-51089 can induce nociceptive behaviors in rats as a result of its antagonistic effects on prostaglandin E2. This compound contains a diacylhydrazine moiety, which has often been observed to release hydrazine. Alternate studies suggest that SC-51089 can be metabolized by rat and human hepatocytes, however different metabolic products are produced. For instance, SC-51089 undergoes aromatic hydroxylation with consequent glucuronidation and sulphation in human hepatocytes, while oxidative N-dealkylation with opening of the oxazepine ring and consequent glucuronidation in observed in rat hepatocytes. SC-51089 is an inhibitor of EP2 and EP3.
1. Hallinan, E.A., et al. 1993. J. Med. Chem. 36: 3293-3299. PMID: 7901416 2. Malmberg, A.B., et al. 1994. Neurosci. Lett. 173: 193-196. PMID: 7936413 3. Khasar, S.G., et al. 1994. Neuroscience. 62: 345-350. PMID: 7830882 4. Lee, K., et al. 1994. Xenobiotica. 24: 25-36. PMID: 8165819 5. Hallinan, E.A., et al. 1996. J. Med. Chem. 39: 609-613. PMID: 8558534
Soluble in water, DMSO (25 mg/ml), methanol, and 1:1 ethanol:PBS (pH 7.2) (~0.5 mg/ml).
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