PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral antitumor activity.[1] At a 25 uM concentration, PGA2 blocks the cell cycle progression of NIH 3T3 cells at the G1 and G2 M phase .[2] It has also been shown to act as a vasodilator with natriuretic properties.[3]
17-phenyl trinor-13,14-dihydro ProstaglandinA2 is a synthetic analog of prostaglandin with relatively unexplored biological activity. Similarly structured, particularly in its lower side chain, to the PGF2α analog latanoprost, which is an approved glaucoma treatment, this compound presents an interesting subject for further pharmaceutical research and potential therapeutic applications.
16,16-dimethyl PGA2 is a metabolism-resistant analog of PGA2 with a prolonged in vivo half-life. It inhibits the proliferation of Sendai virus in cultured African green monkey kidney cells by >90% at a concentration of 4 μg ml. Daily infusion of 10 μg of 16,16-dimethyl PGA2 methyl ester into mice infected with influenza A virus increased survival by 40%. Similar treatment of mice inoculated with erythroleukemia cells delayed tumor growth and increased survival time.
Arbaprostil, a synthetic analog of prostaglandin E2 (PGE2) known as 15(R)-15-methyl prostaglandin E2, was developed for its cytoprotective activity. In the commercial production of bulk arbaprostil, one potential impurity is 15(R)-15-methyl ProstaglandinA2 (15(R)-15-methyl PGA2). The pharmacology and EP receptor binding affinity of 15(R)-15-methyl PGA2 have not been reported.
15(R)-Pinane thromboxane A2 is the (R)-epimer of pinane thromboxane A2 . 15(R)-PTA2 does not inhibit collagen-induced platelet aggregation (IC50s = 120-130 μM). It does not affect gastric tone in isolated rat gastric fundus when used at concentrations of 0.5 or 1.5 μg ml and is less effective than PTA2 at inhibiting prostaglandin-induced contraction of isolated rat stomach muscle.
L 888607 Racemate is a selective antagonist of prostaglandin D2 receptor subtype 1 (DP1) (Kis: 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively).
2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide is a compound known to inhibit stress-induced ulcers, effectively maintaining the levels of phospholipase A2 and prostaglandin E2 in rats subjected to water immersion-restrained stress-induced ulceration.
FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits glucose-induced increases in prostaglandin E2 production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.