Description
Prostaglandin F
2α ethyl amide (PGF
2α-
NEt) is an analog of PGF
2α in which the C-
1 carboxyl group has been modified to an N-
ethyl amide. PG esters have been shown to have ocular hypotensive activity. PG N-
ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that PG ethyl amides are not converted to the free acids
in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-
ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. PGF
2α-
NEt would be expected to show the typical intraocular effects of PGF
2α free acid, but with the much slower hydrolysis pharmacokinetics of the PG N-
amides.
