Prostaglandin E1-d4 (Synonyms: Alprostadild4, PGE1d4)

Prostaglandin E₁-d₄ (PGE₁-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 PGE₁ by GC- or LC-mass spectrometry. PGE₁ is the theoretical cyclooxygenase metabolite of dihomo-γ-linolenic acid (DGLA), but it is virtually undetectable in the plasma of normal humans or other animals.¹ Its pharmacology includes vasodilation, hypotension, and anti-platelet activities. The IC₅₀ of PGE₁ for the inhibition of ADP-induced human platelet aggregation is 40 nM.^2,3 The vasorelaxant and anti-hypertensive effects of PGE₁ are used to treat male erectile dysfunction and to provide emergency vasodilation of the patent ductus arteriosus in infants whose cardiac anomalies require pulmonary shunting for survival.^4,5 In human males, the intracavernosal effective dose range for PGE₁ is 2 to 80 µg, and the transurethral range is 125 to 1,000 µg.⁴

1.Cawello, W., Schweer, H., Dietrich, B., et al.Pharmacokinetics of prostaglandin E1 and its main metabolites after intracavernous injection and short-term infusion of prostaglandin E1 in patients with erectile dysfunctionJournal of Urology1581403-1407(1997) 2.Kobzar, G., Mardla, V., JÄrving, I., et al.Antiaggregating potency of E-type prostaglandins in human and rabbit plateletsProceedings of the Estonian Academy of Sciences.Chemistry40179-180(1991) 3.Okada, F., Nukada, T., Yamauchi, Y., et al.The hypotensive effect of prostaglandin E1 on hypertensive cases of various typesProstaglandins799-106(1974) 4.Padma-Nathan, H., Hellstrom, W.J.G., Kaiser, F.E., et al.Treatment of men with erectile dysfunction with transurethral alprostadilNew England Journal of Medicine3361-7(1997) 5.Olley, P.M., and Coceani, F.Prostaglandins and the ductus arteriosusAnnual Reviews of Medicine32375-3785(1981)