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Cyclooxygenase metabolism of EPA to produce Prostaglandin E3 (PGE3) has been reported in biosynthetic preparations of ovine seminal vesicles1 and in the ocular tissues of primates.2 Prostaglandin A3 (PGA3) is an expected non-enzymatic dehydration product of this PGE3. PGA3 exhibits good affinity for the canine EP2 and EP4 receptors with IC50 values of 120 nM and 20 nM, respectively, in a radioligand binding assay.3,4 PGA3 has weak affinity for human PPARγ, with a Ki value of 188 µM.5
1
Lohmus, M., Vahemets, A., Järving, I., et al. Preparative separation of natural prostaglandins E. Preparative Chromatography1279-300(1991).
2
Kulkarni, P.S., Kaufman, P.L., and Srinivasan, B.D. Eicosapentaenoic acid metabolism in cynomolgus and rhesus conjunctiva and eyelid. J Ocul Pharmacol3349-356(1987).
3
Hibbs, T.A., Lu, B., Smock, S.L., et al. Molecular cloning and charcterization of the canine prostaglandin E receptor EP2 subtype. Prostaglandins Other Lipid Mediat57133-147(1999).
4
Castleberry, T.A., Lu, B., Smock, S.L., et al. Molecular cloning and functional charcterization of the canine prostaglandin E2 receptor EP4 subtype. Prostaglandins Other Lipid Mediat65167-187(2001).
5
Ferry, G., Bruneau, V., Beauverger, P., et al. Binding of prostaglandins to human PPARγ: Tool assessment and new natural ligands. Eur J Pharmacol41777-89(2001).
Lohmus, M., Vahemets, A., Järving, I., et al. Preparative separation of natural prostaglandins E. Preparative Chromatography1279-300(1991).
Ferry, G., Bruneau, V., Beauverger, P., et al. Binding of prostaglandins to human PPARγ: Tool assessment and new natural ligands. Eur J Pharmacol41777-89(2001).
Castleberry, T.A., Lu, B., Smock, S.L., et al. Molecular cloning and functional charcterization of the canine prostaglandin E2 receptor EP4 subtype. Prostaglandins Other Lipid Mediat65167-187(2001).
Hibbs, T.A., Lu, B., Smock, S.L., et al. Molecular cloning and charcterization of the canine prostaglandin E receptor EP2 subtype. Prostaglandins Other Lipid Mediat57133-147(1999).
Kulkarni, P.S., Kaufman, P.L., and Srinivasan, B.D. Eicosapentaenoic acid metabolism in cynomolgus and rhesus conjunctiva and eyelid. J Ocul Pharmacol3349-356(1987).