Target Information
Target General Information | Top | |||||
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Target ID |
T76198
(Former ID: TTDS00395)
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Target Name |
Thromboxane A2 receptor (TBXA2R)
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Synonyms |
TXA2-R; TXA2 receptor; Prostanoid TP receptor
Click to Show/Hide
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Gene Name |
TBXA2R
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 4 Target-related Diseases | + | ||||
1 | Diabetic foot ulcer [ICD-11: BD54] | |||||
2 | Myocardial infarction [ICD-11: BA41-BA43] | |||||
3 | Sexual dysfunction [ICD-11: HA00-HA01] | |||||
4 | Coronary atherosclerosis [ICD-11: BA80] | |||||
Function |
The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messenger system. In the kidney, the binding of TXA2 to glomerular TP receptors causes intense vasoconstriction. Activates phospholipase C. Isoform 1 activates adenylyl cyclase. Isoform 2 inhibits adenylyl cyclase. Receptor for thromboxane A2 (TXA2), a potent stimulator of platelet aggregation.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MWPNGSSLGPCFRPTNITLEERRLIASPWFAASFCVVGLASNLLALSVLAGARQGGSHTR
SSFLTFLCGLVLTDFLGLLVTGTIVVSQHAALFEWHAVDPGCRLCRFMGVVMIFFGLSPL LLGAAMASERYLGITRPFSRPAVASQRRAWATVGLVWAAALALGLLPLLGVGRYTVQYPG SWCFLTLGAESGDVAFGLLFSMLGGLSVGLSFLLNTVSVATLCHVYHGQEAAQQRPRDSE VEMMAQLLGIMVVASVCWLPLLVFIAQTVLRNPPAMSPAGQLSRTTEKELLIYLRVATWN QILDPWVYILFRRAVLRRLQPRLSTRPRSLSLQPQLTQRSGLQ Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A04694 |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
1 | Alprostadil | Drug Info | Approved | Erectile dysfunction | [2], [3] | |
2 | Ridogrel | Drug Info | Approved | Acute myocardial infarction | [4] | |
Clinical Trial Drug(s) | [+] 8 Clinical Trial Drugs | + | ||||
1 | Ramatroban | Drug Info | Phase 2/3 | Perennial allergic rhinitis | [6], [7] | |
2 | Ifetroban sodium | Drug Info | Phase 2 | Thrombosis | [10] | |
3 | KP-496 | Drug Info | Phase 2 | Asthma | [11] | |
4 | TAK-128 | Drug Info | Phase 2 | Diabetic neuropathy | [12] | |
5 | BIBV 308 | Drug Info | Phase 1 | Peripheral vascular disease | [14] | |
6 | G-619 | Drug Info | Phase 1 | Thrombosis | [15] | |
7 | YM-57158 | Drug Info | Phase 1 | Allergic rhinitis | [16] | |
8 | PGF2alpha | Drug Info | Clinical trial | Solid tumour/cancer | [17] | |
Discontinued Drug(s) | [+] 13 Discontinued Drugs | + | ||||
1 | Domitroban | Drug Info | Discontinued in Preregistration | Thrombosis | [18], [19] | |
2 | Seratrodast | Drug Info | Discontinued in Phase 3 | Allergic asthma | [21] | |
3 | ICI-192605 | Drug Info | Discontinued in Phase 2 | Thrombosis | [22], [23] | |
4 | Linotroban | Drug Info | Discontinued in Phase 2 | Thrombosis | [24] | |
5 | SQ-30741 | Drug Info | Discontinued in Phase 2 | Thrombosis | [25] | |
6 | Z-335 | Drug Info | Discontinued in Phase 2 | Thrombosis | [26] | |
7 | CGS-22652 | Drug Info | Discontinued in Phase 1 | Angina pectoris | [27] | |
8 | KT2-962 | Drug Info | Discontinued in Phase 1 | Thrombosis | [28] | |
9 | KW-3635 | Drug Info | Discontinued in Phase 1 | Thrombosis | [29], [30] | |
10 | ON-579 | Drug Info | Terminated | Asthma | [33] | |
11 | Sulotroban | Drug Info | Terminated | Asthma | [34] | |
12 | Vapiprost | Drug Info | Terminated | Cardiovascular disease | [35], [36] | |
13 | ZT-386 | Drug Info | Terminated | Asthma | [37] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Modulator | [+] 11 Modulator drugs | + | ||||
1 | Alprostadil | Drug Info | [38] | |||
2 | KP-496 | Drug Info | [11] | |||
3 | TAK-128 | Drug Info | [12] | |||
4 | G-619 | Drug Info | [15] | |||
5 | YM-57158 | Drug Info | [16] | |||
6 | CGS-22652 | Drug Info | [51] | |||
7 | ON-579 | Drug Info | [55] | |||
8 | Sulotroban | Drug Info | [56] | |||
9 | Vapiprost | Drug Info | [57] | |||
10 | ZT-386 | Drug Info | [58] | |||
11 | S 18204 | Drug Info | [66] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | Ridogrel | Drug Info | [1] | |||
Antagonist | [+] 18 Antagonist drugs | + | ||||
1 | Ramatroban | Drug Info | [39] | |||
2 | Ifetroban sodium | Drug Info | [40] | |||
3 | BIBV 308 | Drug Info | [40] | |||
4 | Domitroban | Drug Info | [42], [43] | |||
5 | Seratrodast | Drug Info | [45] | |||
6 | ICI-192605 | Drug Info | [46] | |||
7 | Linotroban | Drug Info | [47] | |||
8 | SQ-30741 | Drug Info | [48], [49] | |||
9 | Z-335 | Drug Info | [49], [50] | |||
10 | KT2-962 | Drug Info | [49], [52] | |||
11 | KW-3635 | Drug Info | [53] | |||
12 | AH23848 | Drug Info | [41] | |||
13 | I-SAP | Drug Info | [62] | |||
14 | ONO-3708 | Drug Info | [63] | |||
15 | ONO-8809 | Drug Info | [49], [64] | |||
16 | [125I]PTA-OH | Drug Info | [71] | |||
17 | [125I]SAP | Drug Info | [62] | |||
18 | [125I]SQ-29548 | Drug Info | [72] | |||
Agonist | [+] 14 Agonist drugs | + | ||||
1 | PGF2alpha | Drug Info | [41] | |||
2 | 10,10-difluoro TXA2 | Drug Info | [59] | |||
3 | AGN 191976 | Drug Info | [60] | |||
4 | AGN192093 | Drug Info | [60] | |||
5 | butaprost (free acid form) | Drug Info | [41] | |||
6 | cloprostenol | Drug Info | [41] | |||
7 | EP 171 | Drug Info | [61] | |||
8 | fluprostenol | Drug Info | [41] | |||
9 | M&B 28767 | Drug Info | [41] | |||
10 | PGH2 | Drug Info | [65] | |||
11 | SQ 26655 | Drug Info | [67] | |||
12 | STA2 | Drug Info | [68] | |||
13 | U46619 | Drug Info | [41] | |||
14 | [125I]BOP | Drug Info | [70] | |||
Inhibitor | [+] 4 Inhibitor drugs | + | ||||
1 | DALTROBAN | Drug Info | [44] | |||
2 | L-657925 | Drug Info | [54] | |||
3 | SQ-29548 | Drug Info | [41], [54] | |||
4 | U-44069 | Drug Info | [69] |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
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KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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Calcium signaling pathway | hsa04020 | Affiliated Target |
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Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
Platelet activation | hsa04611 | Affiliated Target |
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Class: Organismal Systems => Immune system | Pathway Hierarchy |
Degree | 6 | Degree centrality | 6.45E-04 | Betweenness centrality | 1.23E-04 |
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Closeness centrality | 2.11E-01 | Radiality | 1.37E+01 | Clustering coefficient | 2.00E-01 |
Neighborhood connectivity | 2.73E+01 | Topological coefficient | 2.00E-01 | Eccentricity | 12 |
Download | Click to Download the Full PPI Network of This Target | ||||
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-regulating microRNAs | ||||||
Target-regulating Transcription Factors | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
1 | Calcium signaling pathway | |||||
2 | Neuroactive ligand-receptor interaction | |||||
3 | Platelet activation | |||||
Reactome | [+] 4 Reactome Pathways | + | ||||
1 | Prostanoid ligand receptors | |||||
2 | G alpha (q) signalling events | |||||
3 | G alpha (12/13) signalling events | |||||
4 | Thromboxane signalling through TP receptor | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | GPCRs, Class A Rhodopsin-like | |||||
2 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
3 | Small Ligand GPCRs | |||||
4 | Signal amplification | |||||
5 | GPCR ligand binding | |||||
6 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Chronic ouabain treatment exacerbates blood pressure elevation in spontaneously hypertensive rats: the role of vascular mechanisms. J Hypertens. 2009 Jun;27(6):1233-42. | |||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1882). | |||||
REF 3 | Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77. | |||||
REF 4 | Inhibition of cytochromes p450: existing and new promising therapeutic targets. Drug Metab Rev. 2007;39(2-3):481-99. | |||||
REF 5 | ClinicalTrials.gov (NCT01126073) A Double Blind, Randomized Study to Compare Influence of Niacin/Laropiprant on Functional and Morphological Characteristics of Arterial Wall and Parameters of Inflammation in Subjects With Coronary Heart Disease Already Treated With a Statin in Miran Sebestjen, University Medical Centre Ljubljana. | |||||
REF 6 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1911). | |||||
REF 7 | ClinicalTrials.gov (NCT00311051) Ramatroban/Montelukast Versus Montelukast/Placebo on the Early Allergic Reaction in Asthma Sensitive to House Dust Mite. U.S. National Institutes of Health. | |||||
REF 8 | Pharmacokinetic and pharmacodynamic properties of FK070 (KDI-792), a novel thromboxane receptor antagonist/thromboxane synthetase inhibitor, after single and multiple oral administrations to healthy volunteers. J Pharm Pharmacol. 1996 Apr;48(4):380-5. | |||||
REF 9 | ClinicalTrials.gov (NCT03326063) Therapeutic Control of Aspirin-Exacerbated Respiratory Disease. U.S.National Institutes of Health. | |||||
REF 10 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1987). | |||||
REF 11 | Effects of KP-496, a novel dual antagonist for leukotriene D4 and thromboxane A2 receptors, on contractions induced by various agonists in the guinea pig trachea. Allergol Int. 2006 Dec;55(4):403-10. | |||||
REF 12 | ClinicalTrials.gov (NCT00229437) Efficacy and Safety Study of TAK-128 in Treating Subjects With Diabetic Peripheral Neuropathy. U.S. National Institutes of Health. | |||||
REF 13 | DTTX30, a combined thromboxane receptor antagonist and thromboxane synthetase inhibitor, prevents coronary thrombosis in anesthetized dogs. Basic Res Cardiol. 1997 Jun;92(3):181-90. | |||||
REF 14 | ClinicalTrials.gov (NCT02223013) Relative Bioavailability and Tolerability of Two New Different Extended Release Capsules of BIBV 308 SE, Versus a Solution of BIBV 308 SE in Healthy Subjects. U.S. National Institutes of Health. | |||||
REF 15 | G 619, a dual thromboxane synthase inhibitor and thromboxane A2 receptor antagonist, inhibits tumor necrosis factor-alpha biosynthesis. Eur J Pharmacol. 1995 Nov 3;286(1):31-9. | |||||
REF 16 | In vitro pharmacologic profile of YM158, a new dual antagonist for LTD4 and TXA2 receptors. J Pharmacol Exp Ther. 1998 Nov;287(2):633-9. | |||||
REF 17 | Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81. | |||||
REF 18 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1979). | |||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001843) | |||||
REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011626) | |||||
REF 21 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 22 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6072). | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000402) | |||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003261) | |||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000361) | |||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006051) | |||||
REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001983) | |||||
REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002792) | |||||
REF 29 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1977). | |||||
REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000338) | |||||
REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005083) | |||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001755) | |||||
REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003601) | |||||
REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000039) | |||||
REF 35 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1976). | |||||
REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000070) | |||||
REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004057) | |||||
REF 38 | Flow after prostaglandin E1 is mediated by receptor-coupled adenylyl cyclase in human anterior segments. Invest Ophthalmol Vis Sci. 1999 Oct;40(11):2622-6. | |||||
REF 39 | Participation in cysteinyl leukotrienes and thromboxane A2 in nasal congestion model in Brown Norway rats. Int Immunopharmacol. 2007 Nov;7(11):1483-7. | |||||
REF 40 | AT-1 receptor antagonism modifies the mediation of endothelin-1, thromboxane A2, and catecholamines in the renal constrictor response to angiotensin II. Kidney Int Suppl. 2005 Jan;(93):S3-9. | |||||
REF 41 | The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93. | |||||
REF 42 | The effect of a novel thromboxane A2 (TXA2) receptor antagonist (S-1452) on the antigen-induced bronchoconstriction and airway hyperresponsiveness in guinea pigs. Prostaglandins Leukot Essent Fatty Acids. 1993 May;48(5):343-9. | |||||
REF 43 | Mouse thromboxane A2 receptor: cDNA cloning, expression and northern blot analysis. Biochem Biophys Res Commun. 1992 May 15;184(3):1197-203. | |||||
REF 44 | Synthesis and thromboxane A2/prostaglandin H2 receptor antagonistic activity of phenol derivatives. J Med Chem. 1992 Jun 12;35(12):2202-9. | |||||
REF 45 | Thromboxane A2 inhibition: therapeutic potential in bronchial asthma. Am J Respir Med. 2002;1(1):11-7. | |||||
REF 46 | The effects of thromboxane receptor blockade on platelet aggregation and digital skin blood flow in patients with secondary Raynaud's syndrome. Rheumatol Int. 1991;11(4-5):163-8. | |||||
REF 47 | Effects of the novel thromboxane (TXA2) receptor antagonist linotroban on inulin and para-aminohippuric acid clearances in the conscious male and female rat. Arzneimittelforschung. 1997 Sep;47(9):1026-30. | |||||
REF 48 | Influence of SQ 30741 on thromboxane receptor-mediated responses in the feline pulmonary vascular bed. J Appl Physiol (1985). 1991 Nov;71(5):2012-8. | |||||
REF 49 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 50 | Pharmacokinetic and pharmacodynamic properties of a new thromboxane receptor antagonist (Z-335) after single and multiple oral administrations to healthy volunteers. J Clin Pharmacol. 2002 Jul;42(7):782-90. | |||||
REF 51 | Blood pressure effects of thromboxane A2 blockade in spontaneously hypertensive rats. Clin Exp Pharmacol Physiol. 1993 Nov;20(11):679-87. | |||||
REF 52 | Azulene derivatives as TXA2/PGH2 receptor antagonists--II. Synthesis and biological activity of 6-mono- and 6-dihydroxylated-isopropylazulenes. Bioorg Med Chem. 1996 Apr;4(4):575-91. | |||||
REF 53 | Antithrombotic effects of KW-3635, a thromboxane A2-receptor antagonist, in guinea pigs. Jpn J Pharmacol. 1994 Jun;65(2):93-8. | |||||
REF 54 | Novel synthesis and biochemical properties of an [125I]-labeled photoaffinity probe for thromboxane A2/prostaglandin H2 receptors. J Med Chem. 1991 Apr;34(4):1511-4. | |||||
REF 55 | The effect of a TXA2 receptor antagonist ON-579 on experimental allergic reactions. Prostaglandins Leukot Essent Fatty Acids. 1995 Aug;53(2):123-33. | |||||
REF 56 | The PGI2-analogue iloprost and the TXA2-receptor antagonist sulotroban synergistically inhibit TXA2-dependent platelet activation. Prostaglandins. 1988 Dec;36(6):751-60. | |||||
REF 57 | Effects of vapiprost, a novel thromboxane receptor antagonist, on thrombus formation and vascular patency after thrombolysis by tissue-type plasminogen activator.. Br J Pharmacol. 1992 July; 106(3): 533-538. | |||||
REF 58 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004057) | |||||
REF 59 | Difluorothromboxane A2 and stereoisomers: stable derivatives of thromboxane A2 with differential effects on platelets and blood vessels. Proc Natl Acad Sci U S A. 1989 Jul;86(14):5600-4. | |||||
REF 60 | Evidence for human thromboxane receptor heterogeneity using a novel series of 9,11-cyclic carbonate derivatives of prostaglandin F2 alpha. Br J Pharmacol. 1996 Mar;117(6):1171-80. | |||||
REF 61 | EP 171: a high affinity thromboxane A2-mimetic, the actions of which are slowly reversed by receptor blockade. Br J Pharmacol. 1989 Apr;96(4):875-87. | |||||
REF 62 | 7-[(1R,2S,3S,5R)-6,6-dimethyl-3-(4- iodobenzenesulfonylamino)bicyclo[3.1.1]hept-2-yl]-5(Z)-heptenoic acid: a novel high-affinity radiolabeled antagonist for platelet thromboxane A2/prostaglandin H2 receptors. J Pharmacol Exp Ther. 1992 Aug;262(2):632-7. | |||||
REF 63 | Characterization of U46619 binding in unactivated, intact human platelets and determination of binding site affinities of four TXA2/PGH2 receptor antagonists (13-APA, BM 13.177, ONO 3708 and SQ 29,548). Thromb Res. 1986 Feb 15;41(4):471-81. | |||||
REF 64 | Anti-thrombotic effect of ONO-8809, a novel TXA2/PG endoperoxide receptor antagonist. Adv Prostaglandin Thromboxane Leukot Res. 1991;21B:599-602. | |||||
REF 65 | Effects of KW-3635, a novel dibenzoxepin derivative of a selective thromboxane A2 antagonist, on human, guinea pig and rat platelets. Jpn J Pharmacol. 1992 Jul;59(3):357-64. | |||||
REF 66 | Antithrombotic effects of S 18886, a novel orally active thromboxane A2 receptor antagonist. J Thromb Haemost. 2004 Mar;2(3):492-8. | |||||
REF 67 | Synthesis and in vitro pharmacology of 7-oxabicyclo[2.2.1]heptane analogues of thromboxane A2/PGH2. J Med Chem. 1985 Nov;28(11):1580-90. | |||||
REF 68 | Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. | |||||
REF 69 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8. | |||||
REF 70 | Characterization of an 125I-labeled thromboxane A2/prostaglandin H2 receptor agonist. J Pharmacol Exp Ther. 1989 Nov;251(2):557-62. | |||||
REF 71 | Binding of thromboxane A2/prostaglandin H2 agonists to human platelets. Br J Pharmacol. 1987 May;91(1):223-7. | |||||
REF 72 | Characterization of [5,6-3H]SQ 29,548 as a high affinity radioligand, binding to thromboxane A2/prostaglandin H2-receptors in human platelets. J Pharmacol Exp Ther. 1988 Jun;245(3):786-92. |
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