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
Thumb
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.

TargetActionsOrganism
AThromboxane-A synthase
inhibitor
Human
AThromboxane A2 receptor
antagonist
Human
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
DrugInteractionDrug group
AbciximabRidogrel may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolRidogrel may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Ridogrel is combined with Acetylsalicylic acid.Approved, Vet Approved
AloxiprinThe risk or severity of adverse effects can be increased when Ridogrel is combined with Aloxiprin.Experimental
AlprostadilAlprostadil may increase the antiplatelet activities of Ridogrel.Approved, Investigational
AlteplaseRidogrel may increase the anticoagulant activities of Alteplase.Approved
ALX-0081Ridogrel may increase the anticoagulant activities of ALX-0081.Investigational
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Ridogrel is combined with Aminosalicylic Acid.Approved
AnagrelideRidogrel may increase the anticoagulant activities of Anagrelide.Approved
AncrodRidogrel may increase the anticoagulant activities of Ancrod.Investigational
AndrographolideRidogrel may increase the antiplatelet activities of Andrographolide.Investigational
AnistreplaseRidogrel may increase the anticoagulant activities of Anistreplase.Approved
Antithrombin III humanRidogrel may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanThe risk or severity of adverse effects can be increased when Ridogrel is combined with Apixaban.Approved
ArdeparinRidogrel may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanRidogrel may increase the anticoagulant activities of Argatroban.Approved, Investigational
AstaxanthinRidogrel may increase the anticoagulant activities of Astaxanthin.Investigational
AzelastineAzelastine may increase the antiplatelet activities of Ridogrel.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Ridogrel is combined with Balsalazide.Approved, Investigational
BatroxobinRidogrel may increase the anticoagulant activities of Batroxobin.Experimental
BecaplerminRidogrel may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BemiparinRidogrel may increase the anticoagulant activities of Bemiparin.Approved
BeraprostRidogrel may increase the anticoagulant activities of Beraprost.Investigational
BivalirudinRidogrel may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BrinaseRidogrel may increase the anticoagulant activities of Brinase.Experimental
BuflomedilRidogrel may increase the antiplatelet activities of Buflomedil.Experimental
ButylphthalideRidogrel may increase the antiplatelet activities of Butylphthalide.Investigational
CangrelorRidogrel may increase the anticoagulant activities of Cangrelor.Approved
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Ridogrel is combined with Carbaspirin calcium.Experimental
CertoparinRidogrel may increase the anticoagulant activities of Certoparin.Approved
CilostazolRidogrel may increase the anticoagulant activities of Cilostazol.Approved
Citric AcidRidogrel may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClopidogrelRidogrel may increase the anticoagulant activities of Clopidogrel.Approved, Nutraceutical
CloricromenRidogrel may increase the anticoagulant activities of Cloricromen.Experimental
ClorindioneRidogrel may increase the anticoagulant activities of Clorindione.Experimental
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Ridogrel is combined with Collagenase clostridium histolyticum.Approved, Investigational
Dabigatran etexilateRidogrel may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinRidogrel may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidRidogrel may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanRidogrel may increase the anticoagulant activities of Darexaban.Investigational
DasatinibDasatinib may increase the anticoagulant activities of Ridogrel.Approved, Investigational
DefibrotideRidogrel may increase the anticoagulant activities of Defibrotide.Approved, Investigational
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Ridogrel is combined with Deoxycholic Acid.Approved
dersalazineThe risk or severity of adverse effects can be increased when Ridogrel is combined with dersalazine.Investigational
DesirudinRidogrel may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseRidogrel may increase the anticoagulant activities of Desmoteplase.Investigational
DextranRidogrel may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Ridogrel may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Ridogrel may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Ridogrel may increase the anticoagulant activities of Dextran 75.Approved
DicoumarolRidogrel may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Ridogrel is combined with Diflunisal.Approved
DiphenadioneRidogrel may increase the anticoagulant activities of Diphenadione.Experimental
DipyridamoleRidogrel may increase the anticoagulant activities of Dipyridamole.Approved
DitazoleRidogrel may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
Drotrecogin alfaRidogrel may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
Edetic AcidRidogrel may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanRidogrel may increase the anticoagulant activities of Edoxaban.Approved
EnoxaparinRidogrel may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the antiplatelet activities of Ridogrel.Approved, Investigational
EplivanserinRidogrel may increase the anticoagulant activities of Eplivanserin.Investigational
eplivanserineRidogrel may increase the anticoagulant activities of eplivanserine.Investigational
EpoprostenolEpoprostenol may increase the antiplatelet activities of Ridogrel.Approved
EptifibatideRidogrel may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
Ethyl biscoumacetateRidogrel may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ferulic acidRidogrel may increase the anticoagulant activities of Ferulic acid.Experimental
FibrinolysinRidogrel may increase the anticoagulant activities of Fibrinolysin.Investigational
FluindioneRidogrel may increase the anticoagulant activities of Fluindione.Investigational
FondaparinuxRidogrel may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumRidogrel may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateRidogrel may increase the anticoagulant activities of Gabexate.Investigational
GlucosamineGlucosamine may increase the antiplatelet activities of Ridogrel.Approved
GuacetisalThe risk or severity of adverse effects can be increased when Ridogrel is combined with Guacetisal.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Ridogrel is combined with Hemoglobin crosfumaril.Experimental
HeparinRidogrel may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineRidogrel may increase the anticoagulant activities of Higenamine.Investigational
HydroxytyrosolRidogrel may increase the antiplatelet activities of Hydroxytyrosol.Investigational
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Ridogrel is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Ridogrel.Approved
IbudilastRidogrel may increase the antiplatelet activities of Ibudilast.Approved, Investigational
Icosapent ethylRidogrel may increase the antiplatelet activities of Icosapent ethyl.Approved, Nutraceutical
IdraparinuxRidogrel may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilRidogrel may increase the antiplatelet activities of Ifenprodil.Approved, Withdrawn
IfetrobanRidogrel may increase the antiplatelet activities of Ifetroban.Investigational
IloprostIloprost may increase the antiplatelet activities of Ridogrel.Approved, Investigational
IndobufenRidogrel may increase the anticoagulant activities of Indobufen.Investigational
KetanserinRidogrel may increase the antiplatelet activities of Ketanserin.Investigational
LepirudinRidogrel may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanRidogrel may increase the anticoagulant activities of Letaxaban.Investigational
LimaprostLimaprost may increase the antiplatelet activities of Ridogrel.Approved
LinsidomineRidogrel may increase the antiplatelet activities of Linsidomine.Experimental
MelagatranRidogrel may increase the anticoagulant activities of Melagatran.Experimental
MesalazineThe risk or severity of adverse effects can be increased when Ridogrel is combined with Mesalazine.Approved
MilrinoneMilrinone may increase the antiplatelet activities of Ridogrel.Approved
NadroparinRidogrel may increase the anticoagulant activities of Nadroparin.Approved
NafamostatRidogrel may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilRidogrel may increase the antiplatelet activities of Naftopidil.Investigational
NimesulideRidogrel may increase the antiplatelet activities of Nimesulide.Approved, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Ridogrel is combined with Nitroaspirin.Investigational
ObinutuzumabThe risk or severity of adverse effects can be increased when Ridogrel is combined with Obinutuzumab.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Ridogrel is combined with Olsalazine.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Ridogrel.Approved, Nutraceutical
OtamixabanRidogrel may increase the anticoagulant activities of Otamixaban.Investigational
OzagrelRidogrel may increase the anticoagulant activities of Ozagrel.Investigational
ParnaparinRidogrel may increase the anticoagulant activities of Parnaparin.Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Ridogrel.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Ridogrel.Approved, Investigational
PhenindioneRidogrel may increase the anticoagulant activities of Phenindione.Approved
PhenprocoumonRidogrel may increase the anticoagulant activities of Phenprocoumon.Approved
PicotamideRidogrel may increase the anticoagulant activities of Picotamide.Experimental
PrasugrelRidogrel may increase the anticoagulant activities of Prasugrel.Approved
Protein CRidogrel may increase the anticoagulant activities of Protein C.Approved
Protein S humanRidogrel may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeRidogrel may increase the anticoagulant activities of Protocatechualdehyde.Approved
RamatrobanRidogrel may increase the antiplatelet activities of Ramatroban.Investigational
ResveratrolRidogrel may increase the antiplatelet activities of Resveratrol.Experimental, Investigational
ReteplaseRidogrel may increase the anticoagulant activities of Reteplase.Approved
ReviparinRidogrel may increase the anticoagulant activities of Reviparin.Approved
RivaroxabanRidogrel may increase the anticoagulant activities of Rivaroxaban.Approved
RosiglitazoneRidogrel may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
Salicylic acidThe risk or severity of adverse effects can be increased when Ridogrel is combined with Salicylic acid.Approved, Vet Approved
SarpogrelateRidogrel may increase the anticoagulant activities of Sarpogrelate.Investigational
SaruplaseRidogrel may increase the anticoagulant activities of Saruplase.Experimental
SelexipagRidogrel may increase the anticoagulant activities of Selexipag.Approved
SevofluraneRidogrel may increase the antiplatelet activities of Sevoflurane.Approved, Vet Approved
SRT501Ridogrel may increase the antiplatelet activities of SRT501.Investigational
StreptokinaseRidogrel may increase the anticoagulant activities of Streptokinase.Approved
SulodexideRidogrel may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TenecteplaseRidogrel may increase the anticoagulant activities of Tenecteplase.Approved
TesmilifeneRidogrel may increase the antiplatelet activities of Tesmilifene.Investigational
TicagrelorRidogrel may increase the anticoagulant activities of Ticagrelor.Approved
TiclopidineRidogrel may increase the anticoagulant activities of Ticlopidine.Approved
TinzaparinRidogrel may increase the anticoagulant activities of Tinzaparin.Approved
TioclomarolRidogrel may increase the anticoagulant activities of Tioclomarol.Experimental
TipranavirTipranavir may increase the antiplatelet activities of Ridogrel.Approved, Investigational
TirofibanRidogrel may increase the anticoagulant activities of Tirofiban.Approved
TositumomabThe risk or severity of adverse effects can be increased when Ridogrel is combined with Tositumomab.Approved
TranilastRidogrel may increase the antiplatelet activities of Tranilast.Approved, Investigational
TrapidilRidogrel may increase the antiplatelet activities of Trapidil.Approved
TreprostinilTreprostinil may increase the antiplatelet activities of Ridogrel.Approved, Investigational
TriflusalRidogrel may increase the anticoagulant activities of Triflusal.Approved
TroxerutinRidogrel may increase the anticoagulant activities of Troxerutin.Investigational
UrokinaseRidogrel may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
Vitamin EVitamin E may increase the antiplatelet activities of Ridogrel.Approved, Nutraceutical, Vet Approved
VorapaxarRidogrel may increase the anticoagulant activities of Vorapaxar.Approved
WarfarinRidogrel may increase the anticoagulant activities of Warfarin.Approved
XimelagatranRidogrel may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Food Interactions
Not Available

References

Synthesis Reference
Not Available
General References
Not Available
External Links
Human Metabolome Database
HMDB15338
PubChem Compound
5362391
PubChem Substance
46506774
ChemSpider
4515025
BindingDB
50003795
ChEBI
135542
ChEMBL
CHEMBL280728
Therapeutic Targets Database
DAP000469
PharmGKB
PA164746413
ATC Codes
Not Available
AHFS Codes
Not Available
PDB Entries
Not Available
FDA label
Not Available
MSDS
Not Available

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP4.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00839 mg/mLALOGPS
logP3.24ALOGPS
logP3.13ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)3.5ChemAxon
pKa (Strongest Basic)4.26ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area71.78 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity88.89 m3·mol-1ChemAxon
Polarizability34.94 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9925
Blood Brain Barrier+0.9613
Caco-2 permeable-0.5694
P-glycoprotein substrateNon-substrate0.5312
P-glycoprotein inhibitor INon-inhibitor0.6419
P-glycoprotein inhibitor IINon-inhibitor0.8893
Renal organic cation transporterNon-inhibitor0.5991
CYP450 2C9 substrateNon-substrate0.8073
CYP450 2D6 substrateNon-substrate0.7912
CYP450 3A4 substrateNon-substrate0.5846
CYP450 1A2 substrateNon-inhibitor0.5
CYP450 2C9 inhibitorNon-inhibitor0.6234
CYP450 2D6 inhibitorNon-inhibitor0.839
CYP450 2C19 inhibitorNon-inhibitor0.5103
CYP450 3A4 inhibitorNon-inhibitor0.7368
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7691
Ames testNon AMES toxic0.6001
CarcinogenicityNon-carcinogens0.864
BiodegradationNot ready biodegradable0.9938
Rat acute toxicity2.5990 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9916
hERG inhibition (predictor II)Non-inhibitor0.6611
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot 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

Details
1. Thromboxane-A synthase
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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
Details
2. Thromboxane A2 receptor
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
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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 October 02, 2017 04:55