Limit of detection: 80% B/B₀: 2.6 pg/ml · Sensitivity: 50% B/B₀: 15.5 pg/ml · 17-phenyl trinor Prostaglandin F_2α (17-phenyl trinor PGF_2α) is a metabolically stable analog of PGF_2α 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 PGF_2α.¹ At the rat recombinant FP receptor expressed in CHO cells, 17-phenyl trinor PGF_2α inhibits PGF_2α binding with a K_i value of 1.1 nM.² In human and animal models of glaucoma, FP receptor agonist activity corresponds very closely with intraocular hypotensive activity. 17-phenyl trinor PGF_2α ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost.³ Whether 17-phenyl trinor PGF_2α ethyl amide is a prodrug analogous to prostaglandin ester prodrugs such as latanoprost is currently controversial. There is some evidence that unmetabolized 17-phenyl trinor PGF_2α is a weak FP receptor agonist.⁴ 17-phenyl trinor PGF_2α is converted by an amidase enzymatic activity in the bovine and human cornea to yield the corresponding free acid, with a conversion rate of about 40 µg/g corneal tissue/24 hours.⁵ Cayman’s 17-phenyl trinor PGF_2α EIA is a sensitive detection method for measuring both the free acid and ethyl amide forms of 17-phenyl trinor PGF_2α. The assay is most appropriate for use when only one of the two forms is present. Samples containing mixtures of both the ethyl amide and free acid should be purified and the two compounds separated prior to EIA analysis.

1 Balapure, A.K., Rexroad, C.E., Kawada, K., et al. Structural requirements for prostaglandin analog interaction with the ovine corpus luteum prostaglandin F_2α receptor. Biochem Pharmacol 38 2375-2381 (1989).

2 Lake, S., Gullberg, H., Wahlqvist, J., et al. Cloning of the rat and human prostaglandin F_2α receptors and the expression of the rat prostaglandin F_2α receptor. FEBS Lett 355 317-325 (1994).

3 Woodward, D.F., Krauss, A.H., Chen, J., et al. The pharmacology of Bimatoprost (Lumigan^™). Surv Ophthalmol 45 S337-S345 (2001).

4 Sharif, N.A., Williams, G.W., and Kelly, C.R. Bimatoprost and its free acid are prostaglandin FP receptor agonists. Eur J Pharmacol 432 211-213 (2001).

5 Maxey, K.M., Johnson, J., Camras, C.B., et al. The hydrolysis of bimatoprost in corneal tissue generates a potent prostanoid FP receptor agonist. Surv Ophthalmol 47(4) 34-40 (2002).

Lake, S., Gullberg, H., Wahlqvist, J., et al. Cloning of the rat and human prostaglandin F_2α receptors and the expression of the rat prostaglandin F_2α receptor. FEBS Lett 355 317-325 (1994).

Balapure, A.K., Rexroad, C.E., Kawada, K., et al. Structural requirements for prostaglandin analog interaction with the ovine corpus luteum prostaglandin F_2α receptor. Biochem Pharmacol 38 2375-2381 (1989).

Maxey, K.M., Johnson, J., Camras, C.B., et al. The hydrolysis of bimatoprost in corneal tissue generates a potent prostanoid FP receptor agonist. Surv Ophthalmol 47(4) 34-40 (2002).

Woodward, D.F., Krauss, A.H., Chen, J., et al. The pharmacology of Bimatoprost (Lumigan^™). Surv Ophthalmol 45 S337-S345 (2001).

Sharif, N.A., Williams, G.W., and Kelly, C.R. Bimatoprost and its free acid are prostaglandin FP receptor agonists. Eur J Pharmacol 432 211-213 (2001).

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