pge1

Limaprost (17α,20-dimethyl-δ2-PGE1) is an analog of PGE1 with structural modifications intended to give it a prolonged half-life and greater potency.It is a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost (17α,20-dimethyl-δ2-PGE1) can be used for pain relief, has antianginal effects, and has potential for ischaemic symptoms treatment.

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.

15-epi-PGE1 (15R-Prostaglandin E1; 15-Epiprostaglandin E1), a stereoisomer of PGE1, exhibits reduced biological activity [2]. This compound acts as a non-competitive inhibitor of human placental 15-Hydroxyprostaglandin dehydrogenase (15-PGDH), with an inhibitory concentration 50 (IC50) value of 170 μM [1].

Alprostadil sodium is a prostaglandin receptor ligand with Ki values of 36, 10, 1.1, 2.1, and 33 nM for EP1, EP2, EP3, EP4, and IP, respectively, in mice.It induces vasodilatation and inhibits platelet aggregation, and it can be used as a vasodilator for the study of peripheral vascular disease.

13,14-Dihydro-15(R)-Prostaglandin E1 (13,14-dihydro-15(R)-PGE1) is an analog of 13,14-dihydro-PGE1 characterized by its R-configured hydroxyl group at the C-15 position [1].

Tetranor-Prostaglandin E1 (tetranor-PGE1), a metabolite of PGE1 and PGE2, undergoes formation through β-oxidation.

15(R),19(R)-Hydroxy prostaglandin E1 is a dihydroxy metabolite/stereoisomer of Prostaglandin E1. It is found in the semen of certain mammals, particularly primates.

ADP-β-S (trisodium) is an analog of ADP and acts as a partial agonist. It can induce human platelet aggregation and inhibit PGE1-stimulated adenylate cyclase.

Anti-inflammatory agent 78 (compound L-37) is a potent anti-inflammatory agent. It effectively inhibits PGE2, PGE1, COX-2, and COX-1. Additionally, Anti-inflammatory agent 78 suppresses the release of NO in LPS-stimulated RAW 264.7 cell lines.

3-Methoxy Limaprost is a derivative of Limaprost, which is a prostaglandin E1 (PGE1) analog. Limaprost functions as a potent orally active vasodilator.

Alprostadil ethyl ester is a biochemical used in the treatment of scleroderma.

SC 31391 is a PGE1 analog.

13,14-dihydro-15-keto Prostaglandin E1 inhibits ADP-induced platelet aggregation in human isolated platelet-rich plasma (IC50=14.8 μg/mL) and is a PGE1 metabolite.

15(S)-15-methyl PGE2 is a potent, metabolically stable analog of PGE2. It is a potent gastric antisecretory and antiulcer compound. 15(S)-15-methyl PGE2 binds to human myometrium with twice the affinity of PGE2 and is ten times more potent than PGE1 in contracting uterine smooth muscle.

8-iso Prostaglandin A1 (8-iso PGA1) is an isoprostane and a member in a large family of prostanoids of non-cyclooxygenase origin. It occurs as a common minor impurity in most commercial preparations of PGE1. The biological activity of 8-iso PGA1 has not been studied in depth or reported in the literature.

8-iso Prostaglandin F2β (8-iso PGF2β) is an isomer of PGF2α of non-enzymatic origin. It is one of 64 possible isomers of PGF2α which can be produced by free radical peroxidation of arachidonic acid. 8-iso PGF2β exhibits very weak contraction of human umbilical vein artery and does not promote aggregation of human whole blood. However, 8-iso PGF2β moderately contracts both the canine and porcine pulmonary vein, although the effect is much weaker than that exhibited by other isoprostanes such as 8-iso PGE1, 8-iso PGE2, or 8-iso PGF2α. 8-iso-15-keto PGF2β is a potential metabolite of 8-iso PGF2β via the 15-hydroxy PG dehydrogenase pathway. There are no published reports on the formation or biological activity of 8-iso-15-keto PGF2β.

Prostaglandin A1 (PGA1) was first isolated as a dehydration product of the PGE1 compounds found in human semen. 15-keto PGA1 is a metabolite of PGA1, produced by 15-hydroxy PG dehydrogenase. It can be produced from PGA1 in pig lung, trachea, aorta, and pulmonary artery tissue preparations. 15-keto PGA1, given at a concentration of 6 μM, causes vasoconstriction of rabbit lung that is comparable to that induced by angiotensin II.

16,16-dimethyl Prostaglandin E1 is a PGE1 (T1626) analog that induces bronchoconstriction and vascular smooth muscle contraction and inhibits indomethacin-induced cell elongation.

6-keto Prostaglandin E1 is a bioactive derivative of PGE1 that plays a role in antiplatelet aggregation and depolymerization.

13,14-dihydro Prostaglandin E1 (13,14-dihydro PGE1) is a biologically active metabolite of PGE1 with comparable potency to the parent compound. It is an inhibitor of ADP-induced platelet aggregation in human PRP and washed platelets with IC50 values of 31 and 21 nM, respectively. 13,14-dihydro PGE1 is a slightly more potent inhibitor of ADP-induced human platelet aggregation than PGE1 which has an IC50 value of 40 nM. Also, 13,14-dihydro PGE1 was shown to activate adenylate cyclase in NCB-20 hybrid cells with a Kact value of 668 nM.

8,11,14-Eicosatrienoic acid, also known as dihomo-γ-linolenic acid , is a polyunsaturated fatty acid (PUFA) produced from γ-linolenic acid by the action of fatty acid elongases. It can be metabolized by the cyclooxygenase pathway to produce 1-series prostaglandins (PGs) (e.g., PGE1). (±)14(15)-EpEDE is an EpEDE acid formed from 8,11,14-eicosatrienoic acid. This monoepoxide can be generated from the PUFA, in vitro, by the action of a strong oxidizing agent. Alternatively, this compound may be produced, in vivo, by epoxidation of the PUFA by cytochrome P450 epoxygenases. The biological properties of this compound are poorly understood.

The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells. KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.

tetranor-PGEM is the major urinary metabolite of PGE1 and PGE2, and is used as a marker of PGE2 biosynthesis.[1],[2] About 15% of an infused dose of PGE2 appears as this metabolite in the urine of humans. Normal healthy males excrete 7-40 μg of tetranor-PGEM over a 24-hour period.[1]

MRS2395 is a dipivaloyl derivative and a potent antagonist of the P2Y12 receptor. MRS2395 inhibited ADP-induced platelet activation (Ki: 3.6 μM). MRS2395 enhances platelet dense granule release in response to TRAP-6.