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Prostaglandin Receptor

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Prostaglandin Receptor Prostaglandin receptor, a sub-family of cell surface seven-transmembrane receptors, are the G-protein-coupled receptors. There are currently ten known prostaglandin receptors on various cell types. Prostaglandins bind to a subfamily of cell surface seven-transmembrane receptors, G-protein-coupled receptors. These receptors are named: DP1-2-DP1, DP2 receptors, EP1-4-EP1, EP2, EP3, EP4 receptors, FP-FP, IP1-2-IP1, IP2 receptors, TP-TP receptor. The prostaglandins are a group of hormone-like lipid compounds that are derived enzymatically from fatty acids and have important functions in the animalbody. There are currently ten known prostaglandin receptors on various cell types. www.MedChemExpress.com 1 Prostaglandin Receptor Inhibitors, Agonists, Antagonists, Activators & Modulators (+)-Cloprostenol (-)-Curine (D-Cloprostenol) Cat. No.: HY-107381 Cat. No.: HY-N2569 (+)-Cloprostenol is a prostaglandin F2α (PGF2α) (-)-Curine is an orally active analogue, and shows selective agonistic activity bisbenzylisoquinoline alkaloid isolated from at the prostaglandin receptor. Chondrodendron platyphyllum. (-)-Curine presents anti-inflammatory and analgesic effects at nontoxic doses, at least in part, resulting from the inhibition of prostaglandin E2 production. Purity: 98.05% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg 16,16-Dimethyl prostaglandin E2 2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide (16,16-dimethyl PGE2) Cat. No.: HY-106420 Cat. No.: HY-100287 16,16-Dimethyl prostaglandin E2 (16,16-dimethyl 2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) PGE2) is an orally active vertebrate sulfide is a compound that inhibits stress-induced Hematopoietic stem cells (HSCs) homeostasis ulcer and low toxicity, and can maintain the critical regulator. 16,16-Dimethyl prostaglandin content of phospholipase A2 and prostaglandin E2 E2 can act through EP2/EP4 and has an interaction in ulcerated rats induced by water immersed with the Wnt pathway. restrained stress. Purity: ≥98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 1 mg, 5 mg Aganepag AGN 210676 (AGN 210937) Cat. No.: HY-19864 (Simenepag) Cat. No.: HY-14898 Aganepag is a potent Prostanoid EP2 receptor AGN 210676 is a selective prostaglandin EP2 agonist, with an EC50 of 0.19 nM, and shows no agonist extracted from patent US20070203222A1, activity at EP4 receptor. Aganepag can be used in Compound example 23, has an EC50 of 5 nM. the research of wound healing, scar reduction, scar prevention and wrinkle treatment and prevention. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Agnuside AH 6809 (Agnoside) Cat. No.: HY-N2518 Cat. No.: HY-10418 Agnuside is a compound isolated from Vitex negundo, AH 6809 is an antagonist of EP and DP receptor, down-regulates pro-inflammatory mediators PGE2 with Kis of 1217, 1150, 1597, and 1415 nM for the and LTB4, and reduces the expression of cloned human EP1, EP2, EP3-III, and DP cytokines, with anti-arthritic activity. receptor respectively. AH 6809 has a Ki of 350 nM for mouse EP2 receptor. Purity: 99.90% Purity: 99.47% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg AM211 AMG-009 (AM211 free acid) Cat. No.: HY-13213 Cat. No.: HY-19499 AM211 is a potent, selective and orally AMG-009 is a potent antagonist of prostaglandin bioavailable prostaglandin D2 (PGD2) receptor type D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, receptors, respectively. 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. Purity: 99.94% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Asapiprant AZ-1355 (S-555739) Cat. No.: HY-16763 Cat. No.: HY-101692 Asapiprant is a potent and selective DP1 AZ-1355 is an effctive lipid-lowering compound, receptor antagonist with a Ki of 0.44 nM. which also inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro. Purity: 99.58% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg AZ12672857 AZD1981 Cat. No.: HY-136895 Cat. No.: HY-15950 AZ12672857 is an orally active inhibitor of EphB4 AZD1981 is a potent and selective CRTh2 (IC50=1.3 nM) and Src kinases. AZ12672857 shows antagonist; displaces radio-labelled PGD2 from good inhibition of proliferation of c-Src human recombinant DP2 with high potency (pIC50 = transfected 3T3 cells (IC50=2 nM) as well as 8.4). autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM). Purity: 98.44% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg BAY 73-1449 BAY-1316957 Cat. No.: HY-118941 Cat. No.: HY-111539 BAY 73-1449 is a selective antagonist of BAY-1316957 is a potent, selective and orally prostacyclin receptor (IP), with high potency (IC50 active prostaglandin E2 receptor subtype 4 (EP4-R) of less than 0.1 nM) in cAMP assays in Human HEL antagonist with an IC50 of 15.3 nM for human cells and rat DRG. BAY 73-1449 can be used in the EP4-R. BAY-1316957 has excellent drug metabolism research of lowering blood pressure. and pharmacokinetics properties, and can be used for endometriosis research. Purity: 99.81% Purity: 98.94% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Benorilate Beraprost sodium (Salipran) Cat. No.: HY-107795 Cat. No.: HY-13569A Benorylate (Salipran) is the esterification Beraprost sodium, a prostacyclin analog, is a product of paracetamol and acetylsalicylic acid. stable and orally active prodrug of PGI2. Beraprost Benorylate has anti-inflammatory, analgesic and sodium is a potent vasodilator, has the potential antipyretic properties. Benorylate could also for pulmonary arterial hypertension treatment inhibit prostaglandin (PG) synthesis. through expanding renal vessels, improving microcirculation. Purity: 99.80% Purity: 99.88% Clinical Data: Launched Clinical Data: Phase 4 Size: 10 mM × 1 mL, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg BI-671800 Bimatoprost Cat. No.: HY-114141 (AGN 192024) Cat. No.: HY-B0191 BI-671800 is a highly specific and potent Bimatoprost is a prostaglandin analog used antagonist of chemoattractant receptor-homologous topically (as eye drops) to control the molecule on Th2 cells (DP2/CRTH2), with IC50 progression of glaucoma and in the management of values of 4.5 nM and 3.7 nM for PGD2 binding to ocular hypertension. CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. Purity: 99.06% Purity: 99.59% Clinical Data: Phase 2 Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg www.MedChemExpress.com 3 Bunaprolast Butaprost (U66858) Cat. No.: HY-U00170 Cat. No.: HY-100448A Bunaprolast (U66858) is a potent inhibitor of Butaprost is a selective prostaglandin E receptor LTB4 production in human whole blood. (EP2) agonist with an EC50 of 33 nM and a Ki of Bunaprolast (U66858) also exhibits significant 2.4 μM for murine EP2 receptor. Butaprost is inhibition of lipoxygenase and TXB2 release. less activity against murine EP1, EP3 and EP4 receptors. Butaprost attenuates fibrosis by hampering TGF-β/Smad2 signalling. Purity: >98% Purity: ≥99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg (12.24 mM * 1 mL in Methyl acetate), BW 245C Carbacyclin Cat. No.: HY-101987 (Carbaprostacyclin; Carba-PGI2) Cat. No.: HY-112322 BW 245C is a prostanoid DP-receptor (DP1) agonist, Carbacyclin is a PGI2 analogue, acts as a used to treat stroke. prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation. Purity: 99.14% Purity: ≥99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg Size: 1 mg Carboprost tromethamine CAY10471 Cat. No.: HY-A0195 (TM30089) Cat. No.: HY-13706A Carboprost tromethamine is the synthetic 15-methyl CAY10471 (TM30089) is a potent, selective, and analogue of prostaglandin F2α. Carboprost orally active prostaglandin D2 receptor tromethamine can effectively promote law CRTH2 antagonist. CAY10471 attenuates the contraction of the uterus and significantly reduce progression of tubulointerstitial fibrosis and the amount of bleeding during and after delivery. chronic contact hypersensitivity (CHS) in animal model. Purity: 98.28% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg CAY10471 Racemate CAY10595 (TM30089 Racemate) Cat. No.: HY-13706 Cat. No.: HY-118180 CAY10471 Racemate (TM30089 Racemate) is a potent CAY10595 is a potent CRTH2/DP2 receptor and highly selective prostaglandin D2 receptor antagonist that binds to the human receptor with a CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, Ki of 10 nM. selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM).
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  • New Investigational Drugs for Androgenetic Alopecia. Valente Duarte De Sousa IC 1, Tosti A

    New Investigational Drugs for Androgenetic Alopecia. Valente Duarte De Sousa IC 1, Tosti A

    Expert Opin Investig Drugs. 2013 May;22(5):573-89. doi: 10.1517/13543784.2013.784743. Epub 2013 Apr 4. New investigational drugs for androgenetic alopecia. Valente Duarte de Sousa IC 1, Tosti A . Author information • [email protected] Erratum in • Erratum. [Expert Opin Investig Drugs. 2015] Abstract INTRODUCTION: Androgenetic alopecia (AGA) is the most common form of hair loss, however current treatment options are limited and moderately effective. In the past few years, there has been an increased interest in deciphering the molecular mechanisms responsible for this disorder, which has opened the possibility of novel treatments that promise to not only stimulate hair growth, but also to induce formation of new hair follicles. AREAS COVERED: The future holds more effective topical treatments with less systemic side effects (such as topical 5- alfa-reductase inhibitors), prostaglandin analogs and antagonists, medications which act through the Wnt signaling pathway, stem cells for hair regeneration, platelet-rich plasma (PRP) and more effective ways of transplanting hair. A comprehensive search was made using PubMed, GoogleScholar and Clinicaltrial.gov using different combination of key words, which included AGA treatment, new treatments for AGA, Wnt pathway, prostaglandins, PRP and stem cells for hair regrowth. EXPERT OPINION: In the near future, treatments with topical 5-alfa-reductase inhibitors and prostaglandin agonists or antagonists are expected. More evidence is needed to verify the efficacy of PRP. Although hair follicle bioengineering and multiplication is a fascinating and promising field, it is still a long way from being available to clinicians. J Am Acad Dermatol. 2015 Apr;72(4):712-6.
  • WHO Drug Information Vol

    WHO Drug Information Vol

    WHO Drug Information Vol. 24, No. 4, 2010 World Health Organization WHO Drug Information Contents WHO Prequalification Sitaxentan: worldwide withdrawal 307 Programmes Sibutramine: suspension of sales 307 Sibutramine-containing medicines: WHO Prequalification of Medicines withdrawal 308 Programme: survey of service Testosterone transdermal patch: quality provided to manufacturers 293 withdrawal of extension of WHO initiates pilot prequalification of indication application 308 active pharmaceutical ingredients 297 Aliskiren/valsartan: withdrawal of New on-line database for WHO marketing authorization application 308 prequalified vaccines 298 Mometasone furoate/formoterol fumarate: withdrawal of marketing Safety and Efficacy Issues authorization application 309 EMA and US FDA extend confidentiality H1N1 influenza vaccine: narcolepsy 299 arrangements indefinitely 309 Statins: interstitial lung disease 299 Tocilizumab: risk of fatal anaphylaxis 300 Recent Publications, Pioglitazone: potential bladder cancer 301 Information and Events Angiotensin receptor blockers and US Government to share patents with cancer: safety review 301 Medicines Patent Pool 310 GnRH agonists, diabetes and cardio- Clinical trials and global medicines vascular disease 301 development 310 Gadolinium-based contrast agents: Evaluation of future nanomedicines 311 kidney dysfunction 302 Reporting on opioid inaccessibility 311 Lamotrigine: aseptic meningitis Tinzaparin sodium: renal Impairment in elderly 303 Consultation Documents Tamoxifen: drug interactions involving The
  • Effect of Prostanoids on Human Platelet Function: an Overview

    Effect of Prostanoids on Human Platelet Function: an Overview

    International Journal of Molecular Sciences Review Effect of Prostanoids on Human Platelet Function: An Overview Steffen Braune, Jan-Heiner Küpper and Friedrich Jung * Institute of Biotechnology, Molecular Cell Biology, Brandenburg University of Technology, 01968 Senftenberg, Germany; steff[email protected] (S.B.); [email protected] (J.-H.K.) * Correspondence: [email protected] Received: 23 October 2020; Accepted: 23 November 2020; Published: 27 November 2020 Abstract: Prostanoids are bioactive lipid mediators and take part in many physiological and pathophysiological processes in practically every organ, tissue and cell, including the vascular, renal, gastrointestinal and reproductive systems. In this review, we focus on their influence on platelets, which are key elements in thrombosis and hemostasis. The function of platelets is influenced by mediators in the blood and the vascular wall. Activated platelets aggregate and release bioactive substances, thereby activating further neighbored platelets, which finally can lead to the formation of thrombi. Prostanoids regulate the function of blood platelets by both activating or inhibiting and so are involved in hemostasis. Each prostanoid has a unique activity profile and, thus, a specific profile of action. This article reviews the effects of the following prostanoids: prostaglandin-D2 (PGD2), prostaglandin-E1, -E2 and E3 (PGE1, PGE2, PGE3), prostaglandin F2α (PGF2α), prostacyclin (PGI2) and thromboxane-A2 (TXA2) on platelet activation and aggregation via their respective receptors. Keywords: prostacyclin; thromboxane; prostaglandin; platelets 1. Introduction Hemostasis is a complex process that requires the interplay of multiple physiological pathways. Cellular and molecular mechanisms interact to stop bleedings of injured blood vessels or to seal denuded sub-endothelium with localized clot formation (Figure1).