Prostaglandin F2α (PGF2α) drives luteolysis and smooth muscle contraction by activating the FP receptor. Stable, lipophilic analogs of PGF2α are used to modulate luteolysis and treat glaucoma. 16-phenoxy tetranor Prostaglandin F2α (16-phenoxy tetranor PGF2α) is a metabolically stable form of PGF2α containing a 16-phenoxy group at the ω-terminus. It binds to the FP receptor on ovine luteal cells with much greater affinity (440%) than PGF2α. 16-phenoxy tetranor PGF2α methyl ester is a lipophilic analog of 16-phenoxy tetranor PGF2α. Methyl esters of PGs serve as prodrugs, as they are efficiently hydrolyzed in certain tissues to generate the bioactive free acid.
Prostaglandin F2α (PGF2α), acting through the FP receptor, causes smooth muscle contraction and exhibits potent luteolytic activity. 17-trifluoromethylphenyl trinor PGF2α is an analog of PGF2α that shares the meta-trifluoromethyl group of travoprost with the 17-phenyl trinor modification of latanoprost. It is anticipated to be a potent and selective agonist of the FP receptor, with potential applications in glaucoma and luteolysis. 17-trifluoromethylphenyl trinor PGF2α methyl ester is a lipophilic analog of 17-trifluoromethylphenyl trinor PGF2α. Methyl esters of PGs serve as prodrugs, as they are efficiently hydrolyzed in certain tissues to generate the bioactive free acid.
15(S)-15-methyl Prostaglandin F2α (15(S)-15-methyl PGF2α) has been shown to have potent uterine stimulant and abortifacient properties when administered intramuscularly to induce labor. 15(S)-15-methyl PGF2α isopropyl ester is a lipophilic analog of 15(S)-15-methyl PGF2α methyl ester, which may be hydrolyzed in vivo to the fully active free acid.
(+)-Cloprostenol is a synthetic analog of prostaglandin F2α (PGF2α). It is an FP receptor agonist and a potent luteolytic agent in rats and hamsters. It is 200 times and 100 times more potent than PGF2α in terminating pregnancy in hamsters and rats, respectively, without the side effects associated with PGF2α. Cloprostenol is also used in veterinary medicine as a luteolytic agent for the induction of estrus and the treatment of reproductive disorders in cattle, swine, and horses. (+)-Cloprostenol methyl ester is a more lipid soluble form of cloprostenol, which may be more amenable for certain formulations.
Prostaglandin F2α (PGF2α) drives luteolysis and smooth muscle contraction by activating the FP receptor. Bimatoprost methyl ester is a lipophilic analog of 17-phenyl trinor PGF2α, a potent agonist for the FP receptor. 17-phenyl trinor PGF2α binds the FP receptor on ovine luteal cells with a relative potency of 756% compared to that of PGF2α. Esters of PGs serve as prodrugs, as they are efficiently hydrolyzed in certain tissues to generate the bioactive free acid.