Biological Activity
17-phenyl trinor Prostaglandin F2α-d4 (17-phenyl trinor PGF2α-d4) contains four deuterium atoms at the 3, 3', 4, and 4' positions. It is intended for use as an internal standard for the quantification of 17-phenyl trinor PGF2α by GC- or LC-mass spectrometry. 17-phenyl trinor PGF2α is a metabolically stable analog of PGF2α and is a potent agonist for the FP receptor. It binds to the FP receptor on ovine luteal cells with a relative potency of 756% compared to that of PGF2α.1 At the rat recombinant FP receptor expressed in CHO cells 17-phenyl trinor PGF2α inhibits PGF2α binding with a Ki of 1.1 nM.2 The isopropyl ester of 17-phenyl trinor PGF2α-d4 is slightly better than PGF2α isopropyl ester in reducing the intraocular pressure in the cat eye without any irritation.3
References
1.Balapure, A.K., Rexroad, C.E., Jr., Kawada, K., et al.Structural requirements for prostaglandin analog interaction with the ovine corpus luteum prostaglandin F2α receptorBiochem. Pharmacol.38(14)2375-2381(1989)
2.Lake, S., Gullberg, H., Wahlqvist, J., et al.Cloning of the rat and human prostaglandin F2α receptors and the expression of the rat prostaglandin F2α receptorFEBS Letters355317-325(1994)
3.Stjernschantz, J., and Resul, B.Phenyl substituted prostaglandin analogs for glaucoma treatmentDrugs of the Future17691-704(1992)
