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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyRidogrel
Identification
- Name
- Ridogrel
- Accession Number
- DB01207 (APRD00271)
- Type
- Small Molecule
- Groups
- Approved
- Description
Ridogrel is a dual action drug useful for the prevention of systemic thrombo-embolism and as an adjunctive agent to thrombolytic therapy in acute myocardial infarction. However, there currently are no clinical indications for preferential use of ridogrel over aspirin.
- Structure
Structure for DB01207 (Ridogrel)
- Synonyms
- R-68070
- Ridogrel
- Ridogrelum
- External IDs
- R 68070
- Categories
- UNII
- QTS5QOO42O
- CAS number
- 110140-89-1
- Weight
- Average: 366.3344
Monoisotopic: 366.119127035 - Chemical Formula
- C18H17F3N2O3
- InChI Key
- GLLPUTYLZIKEGF-HAVVHWLPSA-N
- InChI
- InChI=1S/C18H17F3N2O3/c19-18(20,21)15-7-3-5-13(11-15)17(14-6-4-9-22-12-14)23-26-10-2-1-8-16(24)25/h3-7,9,11-12H,1-2,8,10H2,(H,24,25)/b23-17+
- IUPAC Name
- 5-{[(E)-{pyridin-3-yl[3-(trifluoromethyl)phenyl]methylidene}amino]oxy}pentanoic acid
- SMILES
- OC(=O)CCCCO\N=C(\C1=CN=CC=C1)C1=CC(=CC=C1)C(F)(F)F
Pharmacology
- Indication
Used as an adjunctive therapy to induce thrombolysis in patients suffering acute myocardial infarction.
- Structured Indications
- Not Available
- Pharmacodynamics
Ridogrel, a combined thromboxane synthase inhibitor and receptor antagonist, is used with streptokinase as an adjunctive therapy to reduce the formation and size of blood clots. Blood clots can cause ischemic cardiac events (heart attacks). Ridogrel has the dual property of inhibiting the synthesis of thromboxane and blocking the receptors of thromboxane/prostaglandin/endoperoxides. It has been shown to accelerate the speed of recanalization and to delay or prevent reocclusion during systemic thrombolysis with tissue plasminogen activator (streptokinase). Ridogrel is a more potent antiplatelet agent than aspirin and might offer an advantage over aspirin as an adjunct to thrombolysis in patients suffering from acute myocardial infarction. While aspirin inhibits cyclooxygenase, the enzyme responsible for producing thromboxane, ridogrel inhibits thromboxane synthesis directly. A recent comparison between aspirin and ridogrel in as adjunct to thrombolysis in patients with acute myocardial infarction demonstrated that ridogrel is not superior to aspirin in enhancing the fibrinolytic efficacy of streptokinase but might be more effective in preventing new ischemic events. Clinical experience with this drug is still relatively limited.
- Mechanism of action
Ridogrel inhibits thromboxane A2 synthase and also blocks the thromboxane A2/prostaglandin endoperoxide receptors. Thromboxane synthetase produces thromboxane in platelets. Thromboxane is a vasoconstrictor and facilitates the clumping of platelets. Therefore by inhibiting the production and promotion of thromboxane, thrombolysis is enhanced.
Target Actions Organism AThromboxane-A synthase inhibitorHuman AThromboxane A2 receptor antagonistHuman - Absorption
Rapidly absorbed after oral administration (30-60 min)
- Volume of distribution
- Not Available
- Protein binding
Approximately 60% bound to plasma proteins
- Metabolism
- Not Available
- Route of elimination
- Not Available
- Half life
- Not Available
- Clearance
- Not Available
- Toxicity
- Not Available
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group Abciximab Ridogrel may increase the anticoagulant activities of Abciximab. Approved Acenocoumarol Ridogrel may increase the anticoagulant activities of Acenocoumarol. Approved, Investigational Acetylsalicylic acid The risk or severity of adverse effects can be increased when Ridogrel is combined with Acetylsalicylic acid. Approved, Vet Approved Aloxiprin The risk or severity of adverse effects can be increased when Ridogrel is combined with Aloxiprin. Experimental Alprostadil Alprostadil may increase the antiplatelet activities of Ridogrel. Approved, Investigational Alteplase Ridogrel may increase the anticoagulant activities of Alteplase. Approved Aminosalicylic Acid The risk or severity of adverse effects can be increased when Ridogrel is combined with Aminosalicylic Acid. Approved Anagrelide Ridogrel may increase the anticoagulant activities of Anagrelide. Approved Ancrod Ridogrel may increase the anticoagulant activities of Ancrod. Approved, Investigational Andrographolide Ridogrel may increase the antiplatelet activities of Andrographolide. Investigational Anistreplase Ridogrel may increase the anticoagulant activities of Anistreplase. Approved Antithrombin III human Ridogrel may increase the anticoagulant activities of Antithrombin III human. Approved Apixaban The risk or severity of adverse effects can be increased when Ridogrel is combined with Apixaban. Approved Ardeparin Ridogrel may increase the anticoagulant activities of Ardeparin. Approved, Investigational, Withdrawn Argatroban Ridogrel may increase the anticoagulant activities of Argatroban. Approved, Investigational Astaxanthin Ridogrel may increase the anticoagulant activities of Astaxanthin. Investigational Azelastine Azelastine may increase the antiplatelet activities of Ridogrel. Approved Balsalazide The risk or severity of adverse effects can be increased when Ridogrel is combined with Balsalazide. Approved, Investigational Batroxobin Ridogrel may increase the anticoagulant activities of Batroxobin. Experimental Becaplermin Ridogrel may increase the anticoagulant activities of Becaplermin. Approved, Investigational Bemiparin Ridogrel may increase the anticoagulant activities of Bemiparin. Approved, Investigational Beraprost Ridogrel may increase the anticoagulant activities of Beraprost. Investigational Bivalirudin Ridogrel may increase the anticoagulant activities of Bivalirudin. Approved, Investigational Brinase Ridogrel may increase the anticoagulant activities of Brinase. Experimental Buflomedil Ridogrel may increase the antiplatelet activities of Buflomedil. Experimental Butylphthalide Ridogrel may increase the antiplatelet activities of Butylphthalide. Investigational Cangrelor Ridogrel may increase the anticoagulant activities of Cangrelor. Approved Caplacizumab Ridogrel may increase the anticoagulant activities of Caplacizumab. Investigational Carbaspirin calcium The risk or severity of adverse effects can be increased when Ridogrel is combined with Carbaspirin calcium. Experimental, Investigational Certoparin Ridogrel may increase the anticoagulant activities of Certoparin. Approved, Investigational Cilostazol Ridogrel may increase the anticoagulant activities of Cilostazol. Approved, Investigational Citric Acid Ridogrel may increase the anticoagulant activities of Citric Acid. Approved, Nutraceutical, Vet Approved Clopidogrel Ridogrel may increase the anticoagulant activities of Clopidogrel. Approved Cloricromen Ridogrel may increase the anticoagulant activities of Cloricromen. Experimental Clorindione Ridogrel may increase the anticoagulant activities of Clorindione. Experimental Collagenase clostridium histolyticum The risk or severity of adverse effects can be increased when Ridogrel is combined with Collagenase clostridium histolyticum. Approved, Investigational Dabigatran etexilate Ridogrel may increase the anticoagulant activities of Dabigatran etexilate. Approved Dalteparin Ridogrel may increase the anticoagulant activities of Dalteparin. Approved Danaparoid Ridogrel may increase the anticoagulant activities of Danaparoid. Approved, Withdrawn Darexaban Ridogrel may increase the anticoagulant activities of Darexaban. Investigational Dasatinib Dasatinib may increase the anticoagulant activities of Ridogrel. Approved, Investigational Defibrotide Ridogrel may increase the anticoagulant activities of Defibrotide. Approved, Investigational Deoxycholic Acid The risk or severity of adverse effects can be increased when Ridogrel is combined with Deoxycholic Acid. Approved Dersalazine The risk or severity of adverse effects can be increased when Ridogrel is combined with Dersalazine. Investigational Desirudin Ridogrel may increase the anticoagulant activities of Desirudin. Approved Desmoteplase Ridogrel may increase the anticoagulant activities of Desmoteplase. Investigational Dextran Ridogrel may increase the anticoagulant activities of Dextran. Approved, Investigational, Vet Approved Dextran 40 Ridogrel may increase the anticoagulant activities of Dextran 40. Approved Dextran 70 Ridogrel may increase the anticoagulant activities of Dextran 70. Approved Dextran 75 Ridogrel may increase the anticoagulant activities of Dextran 75. Approved Dicoumarol Ridogrel may increase the anticoagulant activities of Dicoumarol. Approved Diflunisal The risk or severity of adverse effects can be increased when Ridogrel is combined with Diflunisal. Approved, Investigational Diphenadione Ridogrel may increase the anticoagulant activities of Diphenadione. Experimental Dipyridamole Ridogrel may increase the anticoagulant activities of Dipyridamole. Approved Ditazole Ridogrel may increase the anticoagulant activities of Ditazole. Approved, Withdrawn Drotrecogin alfa Ridogrel may increase the anticoagulant activities of Drotrecogin alfa. Approved, Investigational, Withdrawn Edetic Acid Ridogrel may increase the anticoagulant activities of Edetic Acid. Approved, Vet Approved Edoxaban Ridogrel may increase the anticoagulant activities of Edoxaban. Approved Enoxaparin Ridogrel may increase the anticoagulant activities of Enoxaparin. Approved Epinastine Epinastine may increase the antiplatelet activities of Ridogrel. Approved, Investigational Eplivanserin Ridogrel may increase the anticoagulant activities of Eplivanserin. Investigational eplivanserine Ridogrel may increase the anticoagulant activities of eplivanserine. Investigational Epoprostenol Ridogrel may increase the anticoagulant activities of Epoprostenol. Approved Eptifibatide Ridogrel may increase the anticoagulant activities of Eptifibatide. Approved, Investigational Ethyl biscoumacetate Ridogrel may increase the anticoagulant activities of Ethyl biscoumacetate. Withdrawn Ferulic acid Ridogrel may increase the anticoagulant activities of Ferulic acid. Experimental Fibrinolysin Ridogrel may increase the anticoagulant activities of Fibrinolysin. Investigational Fluindione Ridogrel may increase the anticoagulant activities of Fluindione. Approved, Investigational Fondaparinux Ridogrel may increase the anticoagulant activities of Fondaparinux. Approved, Investigational Fondaparinux sodium Ridogrel may increase the anticoagulant activities of Fondaparinux sodium. Approved, Investigational Gabexate Ridogrel may increase the anticoagulant activities of Gabexate. Investigational Glucosamine Glucosamine may increase the antiplatelet activities of Ridogrel. Approved, Investigational Guacetisal The risk or severity of adverse effects can be increased when Ridogrel is combined with Guacetisal. Experimental Hemoglobin crosfumaril The risk or severity of adverse effects can be increased when Ridogrel is combined with Hemoglobin crosfumaril. Experimental Heparin Ridogrel may increase the anticoagulant activities of Heparin. Approved, Investigational Higenamine Ridogrel may increase the anticoagulant activities of Higenamine. Investigational Hydroxytyrosol Ridogrel may increase the antiplatelet activities of Hydroxytyrosol. Investigational Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ridogrel is combined with Ibritumomab tiuxetan. Approved, Investigational Ibrutinib The risk or severity of adverse effects can be increased when Ibrutinib is combined with Ridogrel. Approved Ibudilast Ridogrel may increase the antiplatelet activities of Ibudilast. Approved, Investigational Icosapent ethyl Ridogrel may increase the antiplatelet activities of Icosapent ethyl. Approved, Investigational, Nutraceutical Idraparinux Ridogrel may increase the anticoagulant activities of Idraparinux. Investigational Ifenprodil Ridogrel may increase the antiplatelet activities of Ifenprodil. Approved, Investigational, Withdrawn Ifetroban Ridogrel may increase the antiplatelet activities of Ifetroban. Investigational Iloprost Ridogrel may increase the anticoagulant activities of Iloprost. Approved, Investigational Indobufen Ridogrel may increase the anticoagulant activities of Indobufen. Investigational Ketanserin Ridogrel may increase the antiplatelet activities of Ketanserin. Investigational Lepirudin Ridogrel may increase the anticoagulant activities of Lepirudin. Approved Letaxaban Ridogrel may increase the anticoagulant activities of Letaxaban. Investigational Limaprost Limaprost may increase the antiplatelet activities of Ridogrel. Approved, Investigational Linsidomine Ridogrel may increase the antiplatelet activities of Linsidomine. Experimental Melagatran Ridogrel may increase the anticoagulant activities of Melagatran. Experimental Mesalazine The risk or severity of adverse effects can be increased when Ridogrel is combined with Mesalazine. Approved Methyl salicylate The risk or severity of adverse effects can be increased when Ridogrel is combined with Methyl salicylate. Approved, Vet Approved Milrinone Milrinone may increase the antiplatelet activities of Ridogrel. Approved Nadroparin Ridogrel may increase the anticoagulant activities of Nadroparin. Approved, Investigational Nafamostat Ridogrel may increase the anticoagulant activities of Nafamostat. Approved, Investigational Naftopidil Ridogrel may increase the antiplatelet activities of Naftopidil. Investigational Nimesulide Ridogrel may increase the antiplatelet activities of Nimesulide. Approved, Investigational, Withdrawn Nitroaspirin The risk or severity of adverse effects can be increased when Ridogrel is combined with Nitroaspirin. Investigational Obinutuzumab The risk or severity of adverse effects can be increased when Ridogrel is combined with Obinutuzumab. Approved, Investigational Olsalazine The risk or severity of adverse effects can be increased when Ridogrel is combined with Olsalazine. Approved Omega-3 fatty acids Omega-3 fatty acids may increase the antiplatelet activities of Ridogrel. Approved, Nutraceutical Otamixaban Ridogrel may increase the anticoagulant activities of Otamixaban. Investigational Ozagrel Ridogrel may increase the anticoagulant activities of Ozagrel. Investigational Parnaparin Ridogrel may increase the anticoagulant activities of Parnaparin. Approved, Investigational Pentaerythritol Tetranitrate Ridogrel may increase the anticoagulant activities of Pentaerythritol Tetranitrate. Approved Pentosan Polysulfate The risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Ridogrel. Approved Pentoxifylline Pentoxifylline may increase the antiplatelet activities of Ridogrel. Approved, Investigational Phenindione Ridogrel may increase the anticoagulant activities of Phenindione. Approved, Investigational Phenprocoumon Ridogrel may increase the anticoagulant activities of Phenprocoumon. Approved, Investigational Phenyl aminosalicylate The risk or severity of adverse effects can be increased when Ridogrel is combined with Phenyl aminosalicylate. Approved Picotamide Ridogrel may increase the anticoagulant activities of Picotamide. Experimental Prasugrel Ridogrel may increase the anticoagulant activities of Prasugrel. Approved Protein C Ridogrel may increase the anticoagulant activities of Protein C. Approved Protein S human Ridogrel may increase the anticoagulant activities of Protein S human. Approved Protocatechualdehyde Ridogrel may increase the anticoagulant activities of Protocatechualdehyde. Approved Ramatroban Ridogrel may increase the antiplatelet activities of Ramatroban. Investigational Relcovaptan Ridogrel may increase the antiplatelet activities of Relcovaptan. Investigational Resveratrol Ridogrel may increase the antiplatelet activities of Resveratrol. Approved, Experimental, Investigational Reteplase Ridogrel may increase the anticoagulant activities of Reteplase. Approved, Investigational Reviparin Ridogrel may increase the anticoagulant activities of Reviparin. Approved, Investigational Rivaroxaban Ridogrel may increase the anticoagulant activities of Rivaroxaban. Approved Rosiglitazone Ridogrel may increase the anticoagulant activities of Rosiglitazone. Approved, Investigational Salicylic acid The risk or severity of adverse effects can be increased when Ridogrel is combined with Salicylic acid. Approved, Investigational, Vet Approved Sarpogrelate Ridogrel may increase the anticoagulant activities of Sarpogrelate. Investigational Saruplase Ridogrel may increase the anticoagulant activities of Saruplase. Experimental Selexipag Ridogrel may increase the anticoagulant activities of Selexipag. Approved Sevoflurane Ridogrel may increase the antiplatelet activities of Sevoflurane. Approved, Vet Approved SRT501 Ridogrel may increase the antiplatelet activities of SRT501. Investigational Streptokinase Ridogrel may increase the anticoagulant activities of Streptokinase. Approved, Investigational Sulodexide Ridogrel may increase the anticoagulant activities of Sulodexide. Approved, Investigational Tenecteplase Ridogrel may increase the anticoagulant activities of Tenecteplase. Approved Tesmilifene Ridogrel may increase the antiplatelet activities of Tesmilifene. Investigational Ticagrelor Ridogrel may increase the anticoagulant activities of Ticagrelor. Approved Ticlopidine Ridogrel may increase the anticoagulant activities of Ticlopidine. Approved Tinzaparin Ridogrel may increase the anticoagulant activities of Tinzaparin. Approved Tioclomarol Ridogrel may increase the anticoagulant activities of Tioclomarol. Experimental Tipranavir Tipranavir may increase the antiplatelet activities of Ridogrel. Approved, Investigational Tirofiban Ridogrel may increase the anticoagulant activities of Tirofiban. Approved Tositumomab The risk or severity of adverse effects can be increased when Ridogrel is combined with Tositumomab. Approved, Investigational Tranilast Ridogrel may increase the antiplatelet activities of Tranilast. Approved, Investigational Trapidil Ridogrel may increase the antiplatelet activities of Trapidil. Approved Treprostinil Ridogrel may increase the anticoagulant activities of Treprostinil. Approved, Investigational Triflusal Ridogrel may increase the anticoagulant activities of Triflusal. Approved, Investigational Trolamine salicylate The risk or severity of adverse effects can be increased when Ridogrel is combined with Trolamine salicylate. Approved Troxerutin Ridogrel may increase the anticoagulant activities of Troxerutin. Investigational Urokinase Ridogrel may increase the anticoagulant activities of Urokinase. Approved, Investigational, Withdrawn Vitamin E Vitamin E may increase the antiplatelet activities of Ridogrel. Approved, Nutraceutical, Vet Approved Vorapaxar Ridogrel may increase the anticoagulant activities of Vorapaxar. Approved Warfarin Ridogrel may increase the anticoagulant activities of Warfarin. Approved Ximelagatran Ridogrel may increase the anticoagulant activities of Ximelagatran. Approved, Investigational, Withdrawn - Food Interactions
- Not Available
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015338
- PubChem Compound
- 5362391
- PubChem Substance
- 46506774
- ChemSpider
- 4515025
- BindingDB
- 50003795
- ChEBI
- 135542
- ChEMBL
- CHEMBL280728
- Therapeutic Targets Database
- DAP000469
- PharmGKB
- PA164746413
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 4.3 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00839 mg/mL ALOGPS logP 3.24 ALOGPS logP 3.13 ChemAxon logS -4.6 ALOGPS pKa (Strongest Acidic) 3.5 ChemAxon pKa (Strongest Basic) 4.26 ChemAxon Physiological Charge -1 ChemAxon Hydrogen Acceptor Count 5 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 71.78 Å2 ChemAxon Rotatable Bond Count 9 ChemAxon Refractivity 88.89 m3·mol-1 ChemAxon Polarizability 34.94 Å3 ChemAxon Number of Rings 2 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9925 Blood Brain Barrier + 0.9613 Caco-2 permeable - 0.5694 P-glycoprotein substrate Non-substrate 0.5312 P-glycoprotein inhibitor I Non-inhibitor 0.6419 P-glycoprotein inhibitor II Non-inhibitor 0.8893 Renal organic cation transporter Non-inhibitor 0.5991 CYP450 2C9 substrate Non-substrate 0.8073 CYP450 2D6 substrate Non-substrate 0.7912 CYP450 3A4 substrate Non-substrate 0.5846 CYP450 1A2 substrate Non-inhibitor 0.5 CYP450 2C9 inhibitor Non-inhibitor 0.6234 CYP450 2D6 inhibitor Non-inhibitor 0.839 CYP450 2C19 inhibitor Non-inhibitor 0.5103 CYP450 3A4 inhibitor Non-inhibitor 0.7368 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7691 Ames test Non AMES toxic 0.6001 Carcinogenicity Non-carcinogens 0.864 Biodegradation Not ready biodegradable 0.9938 Rat acute toxicity 2.5990 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9916 hERG inhibition (predictor II) Non-inhibitor 0.6611
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as trifluoromethylbenzenes. These are organofluorine compounds that contain a benzene ring substituted with one or more trifluoromethyl groups.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Trifluoromethylbenzenes
- Direct Parent
- Trifluoromethylbenzenes
- Alternative Parents
- Pyridines and derivatives / Heteroaromatic compounds / Monocarboxylic acids and derivatives / Carboxylic acids / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organofluorides / Organic oxides / Hydrocarbon derivatives show 2 more
- Substituents
- Trifluoromethylbenzene / Pyridine / Heteroaromatic compound / Carboxylic acid derivative / Carboxylic acid / Monocarboxylic acid or derivatives / Organoheterocyclic compound / Azacycle / Alkyl fluoride / Hydrocarbon derivative show 11 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Thromboxane-a synthase activity
- Specific Function
- Not Available
- Gene Name
- TBXAS1
- Uniprot ID
- P24557
- Uniprot Name
- Thromboxane-A synthase
- Molecular Weight
- 60517.69 Da
References
- Park SJ, Lee JJ, Vanhoutte PM: Endothelin-1 releases endothelium-derived endoperoxides and thromboxane A2 in porcine coronary arteries with regenerated endothelium. Zhongguo Yao Li Xue Bao. 1999 Oct;20(10):872-8. [PubMed:11270983]
- Tytgat GN, Van Nueten L, Van De Velde I, Joslyn A, Hanauer SB: Efficacy and safety of oral ridogrel in the treatment of ulcerative colitis: two multicentre, randomized, double-blind studies. Aliment Pharmacol Ther. 2002 Jan;16(1):87-99. [PubMed:11856082]
- Authors unspecified: Randomized trial of ridogrel, a combined thromboxane A2 synthase inhibitor and thromboxane A2/prostaglandin endoperoxide receptor antagonist, versus aspirin as adjunct to thrombolysis in patients with acute myocardial infarction. The Ridogrel Versus Aspirin Patency Trial (RAPT). Circulation. 1994 Feb;89(2):588-95. [PubMed:8313547]
- De Cree J, Geukens H, Gutwirth P, De Clerck F, Vercammen E, Verhaegen H: The effect of a combined administration of ridogrel and ketanserin in patients with intermittent claudication. Int Angiol. 1993 Mar;12(1):59-68. [PubMed:8376914]
- Carty E, Macey M, McCartney SA, Rampton DS: Ridogrel, a dual thromboxane synthase inhibitor and receptor antagonist: anti-inflammatory profile in inflammatory bowel disease. Aliment Pharmacol Ther. 2000 Jun;14(6):807-17. [PubMed:10848666]
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Thromboxane a2 receptor activity
- Specific Function
- Receptor for thromboxane A2 (TXA2), a potent stimulator of platelet aggregation. The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messen...
- Gene Name
- TBXA2R
- Uniprot ID
- P21731
- Uniprot Name
- Thromboxane A2 receptor
- Molecular Weight
- 37430.69 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Heinisch G, Holzer W, Kunz F, Langer T, Lukavsky P, Pechlaner C, Weissenberger H: On the bioisosteric potential of diazines: diazine analogues of the combined thromboxane A2 receptor antagonist and synthetase inhibitor Ridogrel. J Med Chem. 1996 Sep 27;39(20):4058-64. [PubMed:8831771]
- Soyka R, Heckel A, Nickl J, Eisert W, Muller TH, Weisenberger H: 6,6-Disubstituted Hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors. J Med Chem. 1994 Jan 7;37(1):26-39. [PubMed:8289199]
- Hempelmann RG, Pradel RH, Mehdorn HM, Ziegler A: Threshold concentrations of endothelin-1: the effects on contractions induced by 5-hydroxytryptamine in isolated rat cerebral and mesenteric arteries. Pharmacol Toxicol. 1999 Sep;85(3):115-22. [PubMed:10522750]
- Carvalho MH, Fortes ZB, Nigro D, Oliveira MA, Scivoletto R: The role of thromboxane A2 in the altered microvascular reactivity in two-kidney, one-clip hypertension. Endothelium. 1997;5(3):167-78. [PubMed:9272380]
- Ragni M, Golino P, Cirillo P, Pascucci I, Scognamiglio A, Ravera A, Esposito N, Battaglia C, Guarino A, Chiariello M: [Inactivated factor VII exercises a powerful antithrombotic activity in an experimental model of recurrent arterial thrombosis]. Cardiologia. 1996 Jan;41(1):51-8. [PubMed:8697470]
Drug created on June 13, 2005 07:24 / Updated on March 02, 2018 02:09