11-deoxy Prostaglandin E₁ (11-deoxy PGE₁) is a synthetic analog of PGE₁. Early reports show that it is a selective agonist for the EP₂ receptor but effective at much higher concentrations than PGE₂.^1,2 However, later studies show that it is a non-selective agonist of EP receptors and stimulates cAMP release in Jurkat cells with an EC₅₀ of 0.25 µM.³ 11-deoxy PGE₁ also exhibits vasodepressor and bronchodilator responses in guinea pigs.⁴ 11-deoxy PGE₁ exhibits selectively for the murine EP₃ receptor and is essentially equipotent to PGE₁ at this receptor subtype. The K_i values for binding to the murine EP₁, EP₂, EP₃, and EP₄ receptors are 600, 45, 1.1, and 23 nM, respectively.⁵

1 Dong, Y.J., Jones, R.L., and Wilson, N.H. Prostaglandin E receptor subtypes in smooth muscle: Agonist activities of stable prostacyclin analogues. Br J Pharmacol 87 97-107 (1986).

2 Chen, J., and Woodward, D.F. Prostanoid-induced relaxation of precontracted cat ciliary muscle is mediated by EP₂ and DP receptors. Invest Ophthamol Vis Sci 33 3195-3201 (1992).

3 De Vries, G.W., Guarino, P., McLaughlin, A., et al. An EP receptor with a novel pharmacological profile in the T-cell line Jurkat. Br J Pharmacol 115 1231-1234 (1995).

4 Hall, D.W.R., and Jaitly, K.D. Structure-activity relationships in a series of 11-deoxy prostaglandins. Prostaglandins 11 573-587 (1976).

5 Kiriyama, M., Ushikubi, F., Kobayashi, T., et al. Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol 122 217-224 (1997).

Chen, J., and Woodward, D.F. Prostanoid-induced relaxation of precontracted cat ciliary muscle is mediated by EP₂ and DP receptors. Invest Ophthamol Vis Sci 33 3195-3201 (1992).

Mori, K., Tanaka, I., Kotani, M., et al. Gene expression of the human prostaglandin E receptor EP₄ subtype: Differential regulation in monocytoid and lymphoid lineage cells by phorbol ester. J Mol Med 74 333-336 (1996).

Kiriyama, M., Ushikubi, F., Kobayashi, T., et al. Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol 122 217-224 (1997).

Hall, D.W.R., and Jaitly, K.D. Structure-activity relationships in a series of 11-deoxy prostaglandins. Prostaglandins 11 573-587 (1976).

Protzman, C.E., and Woodward, D.F. Prostanoid-induced blood-aqueous barrier breakdown in rabbits involves the EP₂ receptor subtype. Invest Ophthamol Vis Sci 31 2463-2466 (1990).

Talpain, E., Armstrong, R.A., Coleman, R.A., et al. Characterization of the PGE receptor subtype mediating inhibition of superoxide production in human neutrophils. Br J Pharmacol 114 1459-1465 (1995).

Miledi, R., and Woodward, R.M. Membrane currents elicited by prostaglandins, atrial natriuretic factor and oxytocin in follicle-enclosed Xenopus oocytes. J Physiol 416 623-643 (1989).

De Vries, G.W., Guarino, P., McLaughlin, A., et al. An EP receptor with a novel pharmacological profile in the T-cell line Jurkat. Br J Pharmacol 115 1231-1234 (1995).

Dong, Y.J., Jones, R.L., and Wilson, N.H. Prostaglandin E receptor subtypes in smooth muscle: Agonist activities of stable prostacyclin analogues. Br J Pharmacol 87 97-107 (1986).

Jumblatt, M.M., and Paterson, C.A. Prostaglandin E₂ effects on corneal endothelial cyclic adenosine monophosphate synthesis and cell shape are mediated by a receptor of the EP₂ subtype. Invest Ophthamol Vis Sci 32 360-365 (1991).

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11-deoxy Prostaglandin E1 is available in the following screening library:

• Bio-active Lipid I Screening Library (96-Well)