Sulprostone - CAS 60325-46-4
Category: Inhibitor
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Prostanoid Receptor
Sulprostone is a synthetic PGE2 analog that acts as a selective EP3 and EP1 receptor agonist (Ki = 0.6 and 21 nM, respectively). Sulprostone is a potent stimulator of uterine smooth muscle contractions with high abortifacient activity.
Brife Description:
EP3/EP1 receptor agonist
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1.Fibrinogen concentrate as a treatment for post-partum haemorrhage-induced coagulopathy: a study protocol for a randomized multicentre controlled trial. The FIbrinogen in haemorrhage of DELivery (FIDEL) trial.
Ducloy-Bouthors AS1, Mignon A2, Huissoud C3, Grouin JM4, Mercier FJ5. Anaesth Crit Care Pain Med. 2016 Mar 19. pii: S2352-5568(16)30016-9. doi: 10.1016/j.accpm.2015.10.011. [Epub ahead of print]
BACKGROUND: Postpartum haemorrhage (PPH) remains the leading cause for maternal mortality worldwide. Hypofibrinogenaemia has been identified as a major risk factor for progress towards severe PPH. The efficacy of fibrinogen concentrate supplementation in PPH has been shown in various clinical settings but the level of evidence is not sufficient to prove the benefit, evaluate the risks, and determine the value, timing and dose of fibrinogen supplementation in PPH. The FIDEL trial objective is to evaluate the impact of a therapeutic strategy based on the early administration of human fibrinogen concentrate compared to the current practice based on late administration in severe PPH patients requiring second line uterotonics.
2.PGE2 receptor EP3 inhibits water reabsorption and contributes to polyuria and kidney injury in a streptozotocin-induced mouse model of diabetes.
Hassouneh R1, Nasrallah R1, Zimpelmann J2, Gutsol A2, Eckert D1, Ghossein J1, Burns KD1,2, Hébert RL3. Diabetologia. 2016 Mar 19. [Epub ahead of print]
AIMS/HYPOTHESIS: The first clinical manifestation of diabetes is polyuria. The prostaglandin E2 (PGE2) receptor EP3 antagonises arginine vasopressin (AVP)-mediated water reabsorption and its expression is increased in the diabetic kidney. The purpose of this work was to study the contribution of EP3 to diabetic polyuria and renal injury.
3.The EP3 Agonist Sulprostone Enhances Platelet Adhesion But Not Thrombus Formation Under Flow Conditions.
Pasterk L1, Philipose S, Eller K, Marsche G, Heinemann A, Schuligoi R. Pharmacology. 2015;96(3-4):137-43. doi: 10.1159/000437143. Epub 2015 Jul 30.
Platelets express the EP2, EP3 and EP4 receptors. Prostaglandin (PG) E2 has a biphasic effect on platelets. Low concentrations of PGE2 enhance platelet aggregation through the activation of the EP3 receptors, while at high concentrations it attenuates aggregation via the EP4 receptor. Consequently, EP3 receptor inhibition was shown to inhibit artherothrombosis, but had no influence on bleeding time in vivo. In this study, we investigated the role of the EP3 receptor in adhesion and thrombus formation under flow conditions in vitro. The EP3 agonist sulprostone caused an increase in the adhesion of washed platelets to fibrinogen as well as to collagen under low shear stress, an effect that was blocked by the EP3 antagonist L-798106. In contrast, when whole blood was perfused over collagen-coated surfaces, sulprostone did not enhance binding and thrombus formation of platelets on collagen; at high concentrations it even attenuated this response.
4.Prostaglandins in the eye: Function, expression, and roles in glaucoma.
Doucette LP1, Walter MA1. Ophthalmic Genet. 2016 Apr 12:1-9. [Epub ahead of print]
Prostaglandins are small pro-inflammatory molecules derived from arachidonic acid that play roles in a multitude of biological processes including, but not limited to, inflammation, pain modulation, allergies, and bone formation. Prostaglandin analogues are the front-line medications for the treatment of glaucoma, a condition resulting in blindness due to the death of retinal ganglion cells. These drugs act by lowering intraocular pressure (IOP), a major risk factor for glaucoma. The currently used prostaglandin analogues (latanoprost, bimatoprost, tafluprost, and travoprost) mimic PGF2 and target one of the prostaglandin receptors (FP), though research into harnessing the other receptors using compounds like Sulprostone (EP3 receptor), or Iloprost (IP receptor) are currently ongoing. In this review, we summarize the research into each of the prostaglandin molecules (PGD2, PGE2, PGF2, PGI2, TXA2) and their respective receptors (DP, EP1, 2, 3, 4, FP, IP).
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CAS 60325-46-4 Sulprostone

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