prostaglandin a2

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]

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.

8-iso Prostaglandin A2 is an isoprostane produced by the nonenzymatic oxidation of arachidonic acid.

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 Prostaglandin A2 (15(R)-15-methyl PGA2). The pharmacology and EP receptor binding affinity of 15(R)-15-methyl PGA2 have not been reported.

17-phenyl trinor-13,14-dihydro Prostaglandin A2 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.

17-Phenyl trinor prostaglandin A2 is a synthetic analog of prostaglandin [1].

LCB-2853 is a potent thromboxane A2 prostaglandin H2 (TXA2 PGH2) receptor antagonist with antiplatelet aggregation, antivasospasm, and antithrombotic effects.

AZ-1355 is a novel dibenzoxepine derivative with lipid-lowering properties.

Terbogrel is an oral thromboxane A2 receptor antagonist (IC50 is about 10 nM) and thromboxane A2 synthase inhibitor (IC50 is about 10 nM). Terbogrel is an antiplatelet compound that inhibits platelet aggregation and is a potential compound for the prevention of blood clots.

Ketoprofen (RP-19583) is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. It inhibits cyclo-oxygenase I and II, decreasing the formation of prostaglandin and thromboxane precursors. This reduction in prostaglandin synthesis, mediated by prostaglandin synthase, is responsible for its therapeutic effects. Additionally, Ketoprofen decreases thromboxane A2 formation via thromboxane synthase, inhibiting platelet aggregation.

Etodolac (AY-24236) inhibits the activity of cyclooxygenase I and II, thereby preventing the formation of prostaglandin which is involved in the induction of pain, fever, and inflammation. Etodolac is a pyranocarboxylic acid and non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic activities. It also inhibits platelet aggregation by blocking platelet cyclooxygenase and the subsequent formation of thromboxane A2.

Ozagrel (Domenan) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

Ozagrel hydrochloride (OKY-046 HCl) is a selective thromboxane A(2) synthetase inhibitor used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

p-Hydroxycinnamic acid (NSC-59260) can inhibit platelet activity, with IC50s of 371 μM, 126 μM for thromboxane B2 production and lipopolysaccharide-induced prostaglandin E2 generation, respectively.

2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide inhibits stress-induced ulcers by maintaining phospholipase A2 and prostaglandin E2 levels in rats subjected to water immersion-restrained stress-induced ulceration.

Bromoenol lactone ((6E)-Bromoenol lactone) is a selective calcium-dependent phospholipase A2 (iPLA2β) and serine protease inhibitor that attenuates nicotine-induced breast cancer cell proliferation and migration, inhibits voltage-gated Ca2+ and transient receptor potential classical channels, and inhibits carrageenan-induced prostaglandin production and hyperalgesia in rat hind paws.

L 888607 Racemate is a selective antagonist of the prostaglandin D2 receptor subtype 1 (DP1) with Ki values of 132 nM and 17 nM for DP1 and the thromboxane A2 receptor (TP), respectively.

ONO-RS-082 is a Ca2+-independent phospholipase A2 inhibitor.

Arachidonic acid leelamide is a phospholipase A2 inhibitor. Phospholipase A is a hydrolase responsible for the release of arachidonic acid from the sn2 position of phospholipids. The released arachidonic acid is then converted to mediators of inflammation

L-670,596 is a thromboxane A2/prostaglandin endoperoxide receptor antagonist.

Ono 1301 is a prostaglandin I2 mimetic coumpound with inhibitory activity against thromboxane A2 synthase. Ono 1301 suppresses pancreatic fibrosis in the DBTC-induced CP model by inhibiting monocyte activity not only with induction of HGF but also by Ono

Ono-3708 is a potent antagonist of the thromboxane A2 prostaglandin endoperoxide receptor in vitro and in vivo.

SQ 26655 is an antagonist of thromboxane A2/prostaglandin H2.

Thromboxane A2, as an unstable intermediate between the prostaglandin endoperoxides and thromboxane B2, is a potent inducer of platelet aggregation and causes vasoconstriction.