Prostaglandin

L-161982 is a selective EP4 receptor antagonist that inhibits PGE2-induced ERK phosphorylation and cell proliferation in HCA-7 cells and alleviates collagen-induced arthritis in mice.

Pranoprofen (Pyranoprofen) (INN) is a non-steroidal anti-inflammatory drug used in ophthalmology.

Phenylbutazone (Butazolidine) is a butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ankylosing spondylitis, rheumatoid arthritis, and reactive arthritis.

Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.

FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and COX (IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase, respectively).

AT56, a specific inhibitor of prostaglandin D2 synthase enzymatic activity, blunted adipogenic aldosterone effects.

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

Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a synthetic analogue of PGF2α with oxytocic properties, commonly used to restore uterine tone.

Saralasin acetate is a Non-selective angiotensin II antagonist.

Prostaglandin E2 (PGE2) is a natural hormone-like substance involved in various physiological functions, including the contraction and relaxation of smooth muscles, dilation and constriction of blood vessels, regulation of blood pressure, and modulation of inflammation. It can be used to induce neuropathic pain models.

Prostaglandin G/H synthase 1 inhibitor (CP 74006) is a selective D5D inhibitor with an IC(50) value of 20 nM.

16,16-Dimethyl prostaglandin E2 is an orally active vertebrate Hematopoietic stem cells homeostasis critical regulator. It can act through EP2/EP4 and has an interaction with the Wnt pathway.

Prostaglandin D2 (PGD2), a major prostaglandin produced actively in the brains of various mammals, is a potent endogenous sleep-promoting substance.

Prostaglandin E1 (Alprostadil) is the naturally occurring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Prostaglandin E1 is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

Prostaglandin K1 (compound 46) is a structurally modified prostanoid analog with an EC50 and Ki of 2800 nM for the EP1 receptor.

17-Phenyl trinor prostaglandin F2α glycinamide methyl ester is a derivative of Bimatoprost and functions as a prostaglandin analogue. This compound acts as an agonist for the human prostaglandin FP receptor. It exhibits ocular hypotensive effects and is utilized in research related to ocular hypertension and glaucoma.

Prostaglandin A3 is a non-enzymatic dehydration product of prostaglandin E3 (PGE3). It demonstrates significant affinity for canine EP2 and EP4 receptors with IC50 values of 120 nM and 20 nM, respectively. For human PPARγ, Prostaglandin A3 has a Ki value of 188 μM.

Prostaglandin F3α (PGF3α) is a bioactive lipid mediator derived from eicosapentaenoic acid (EPA) with anticancer and anti-inflammatory properties. It serves as a substrate for ABCC4 with a Km of 12.1 μM. Additionally, Prostaglandin F3α (PGF3α) is utilized in diabetes research.

16-Phenyl tetranor Prostaglandin F2α (16-Phenyl tetranor PGF2α) is a metabolically stable analogue of PGF2α. Compared to PGF2α, 16-Phenyl tetranor PGF2α exhibits reduced affinity (8.7%) for the FP receptor on ovine luteal cells.

20-ethyl Prostaglandin F2α (ICI 74205; 20-ethyl PGF2α) is an analog of PGF2α and is a metabolite of arachidonic acid.

15-deoxy-Δ-12,14-Prostaglandin J2 is a PPARγ agonist.

Bimatoprost is the Allergan trade name for 17-phenyl trinor prostaglandin F2α ethyl amide (17-phenyl trinor PGF2α ethyl amide), an F-series PG analog which has been approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group produces 15-keto-17-phenyl trinor PGF2α ethyl amide. 15-keto-17-phenyl trinor PGF2α ethyl amide is a potential metabolite of 17-phenyl trinor PGF2α ethyl amide when 17-phenyl trinor PGF2α ethyl amide is administered to intact animals. No pharmacological studies on 15-keto-17-phenyl trinor PGF2α ethyl amide have been reported.

PGBx is a mixture of oligomers of PGB1 with a molecular weight of 1,000-1,500. It has antioxidant and free radical trapping activity that was first studied in isolated mitochondria.1 PGBx has anti-inflammatory and cytoprotective activity which may be attributed to inhibition of the 14 kDa sPLA2.2,3 At a dose of 1 mg/kg, PGBx significantly reduces the incidence of ulcers in rats.2References1. Polis, B.D., Polis, E., and Kwong, S. Protection and reactivation of oxidative phosphorylation in mitochondria by a stable free-radical prostaglandin polymer (PGBΧ). Proceedings of the National Academy of Sciences of the United States of America 76, 1598-1602 (1979).2. Kumashiro, R., Devlin, T.M., Kholoussy, A.M., et al. Prostaglandin BΧ in the prevention of stress ulcers in rats. International Surgery 70, 247-250 (1985).3. Franson, R.C., Rosenthal, M.D., and Regelson, W. Mechanism(s) of cytoprotective and anti-inflammatory activity of PGB1 oligomers: PGBx has potent anti-phospholipase A2 and anti-oxidant activity. Prostaglandins, Leukotrienes and Essential Fatty Acids 43, 63-70 (1991). PGBx is a mixture of oligomers of PGB1 with a molecular weight of 1,000-1,500. It has antioxidant and free radical trapping activity that was first studied in isolated mitochondria.1 PGBx has anti-inflammatory and cytoprotective activity which may be attributed to inhibition of the 14 kDa sPLA2.2,3 At a dose of 1 mg/kg, PGBx significantly reduces the incidence of ulcers in rats.2 References1. Polis, B.D., Polis, E., and Kwong, S. Protection and reactivation of oxidative phosphorylation in mitochondria by a stable free-radical prostaglandin polymer (PGBΧ). Proceedings of the National Academy of Sciences of the United States of America 76, 1598-1602 (1979).2. Kumashiro, R., Devlin, T.M., Kholoussy, A.M., et al. Prostaglandin BΧ in the prevention of stress ulcers in rats. International Surgery 70, 247-250 (1985).3. Franson, R.C., Rosenthal, M.D., and Regelson, W. Mechanism(s) of cytoprotective and anti-inflammatory activity of PGB1 oligomers: PGBx has potent anti-phospholipase A2 and anti-oxidant activity. Prostaglandins, Leukotrienes and Essential Fatty Acids 43, 63-70 (1991).

Isoprostanes are produced by the non-enzymatic, free radical peroxidation of phospholipid-esterified arachidonic acid. They have been used as biomarkers of oxidative stress, but they also have been found to have potent biological activity. ent-8-iso-15(S)-Prostaglandin F2α (ent-8-iso-15(S)-PGF2α) is a potent vasoconstrictor of porcine retinal and brain microvessels with EC50 values of 15 and 24 nM, respectively. This isoprostane is about ten-fold more potent than 8-iso-PGF2α in a whole blood platelet aggregation inhibition assay.