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
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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) | [+] 3 Approved Drugs | + | ||||
1 | Alprostadil | Drug Info | Approved | Erectile dysfunction | [2], [3] | |
2 | Ridogrel | Drug Info | Approved | Acute myocardial infarction | [4] | |
3 | LAROPIPRANT | Drug Info | Phase 4 | Coronary heart disease | [5] | |
Clinical Trial Drug(s) | [+] 10 Clinical Trial Drugs | + | ||||
1 | Ramatroban | Drug Info | Phase 2/3 | Perennial allergic rhinitis | [6], [7] | |
2 | FK-070 | Drug Info | Phase 2 | Angina pectoris | [8] | |
3 | Ifetroban sodium | Drug Info | Phase 2 | Thrombosis | [9] | |
4 | KP-496 | Drug Info | Phase 2 | Asthma | [10] | |
5 | TAK-128 | Drug Info | Phase 2 | Diabetic neuropathy | [11] | |
6 | BIBV 308 | Drug Info | Phase 1 | Peripheral vascular disease | [12] | |
7 | DT-TX-30 | Drug Info | Phase 1 | Angina pectoris | [13] | |
8 | G-619 | Drug Info | Phase 1 | Thrombosis | [14] | |
9 | YM-57158 | Drug Info | Phase 1 | Allergic rhinitis | [15] | |
10 | PGF2alpha | Drug Info | Clinical trial | Solid tumour/cancer | [16] | |
Discontinued Drug(s) | [+] 16 Discontinued Drugs | + | ||||
1 | Domitroban | Drug Info | Discontinued in Preregistration | Thrombosis | [17], [18] | |
2 | Seratrodast | Drug Info | Discontinued in Phase 3 | Allergic asthma | [19] | |
3 | Terutroban sodium | Drug Info | Discontinued in Phase 3 | Thrombosis | [20] | |
4 | ICI-192605 | Drug Info | Discontinued in Phase 2 | Thrombosis | [21], [22] | |
5 | Linotroban | Drug Info | Discontinued in Phase 2 | Thrombosis | [23] | |
6 | SQ-30741 | Drug Info | Discontinued in Phase 2 | Thrombosis | [24] | |
7 | Z-335 | Drug Info | Discontinued in Phase 2 | Thrombosis | [25] | |
8 | CGS-22652 | Drug Info | Discontinued in Phase 1 | Angina pectoris | [26] | |
9 | KT2-962 | Drug Info | Discontinued in Phase 1 | Thrombosis | [27] | |
10 | KW-3635 | Drug Info | Discontinued in Phase 1 | Thrombosis | [28], [29] | |
11 | ON-579 | Drug Info | Terminated | Asthma | [30] | |
12 | SQ-33961 | Drug Info | Terminated | Thrombosis | [31] | |
13 | Sulotroban | Drug Info | Terminated | Asthma | [32] | |
14 | UP-116-77 | Drug Info | Terminated | Thrombosis | [33] | |
15 | Vapiprost | Drug Info | Terminated | Cardiovascular disease | [34], [35] | |
16 | ZT-386 | Drug Info | Terminated | Asthma | [36] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Modulator | [+] 14 Modulator drugs | + | ||||
1 | Alprostadil | Drug Info | [37] | |||
2 | FK-070 | Drug Info | [8] | |||
3 | KP-496 | Drug Info | [10] | |||
4 | TAK-128 | Drug Info | [11] | |||
5 | G-619 | Drug Info | [14] | |||
6 | YM-57158 | Drug Info | [15] | |||
7 | CGS-22652 | Drug Info | [52] | |||
8 | ON-579 | Drug Info | [56] | |||
9 | SQ-33961 | Drug Info | [57] | |||
10 | Sulotroban | Drug Info | [58] | |||
11 | UP-116-77 | Drug Info | [59] | |||
12 | Vapiprost | Drug Info | [60] | |||
13 | ZT-386 | Drug Info | [61] | |||
14 | S 18204 | Drug Info | [71] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | Ridogrel | Drug Info | [1] | |||
Inhibitor | [+] 6 Inhibitor drugs | + | ||||
1 | LAROPIPRANT | Drug Info | [38] | |||
2 | DALTROBAN | Drug Info | [44] | |||
3 | L-657925 | Drug Info | [55] | |||
4 | BM-573 | Drug Info | [64] | |||
5 | SQ-29548 | Drug Info | [41], [55] | |||
6 | U-44069 | Drug Info | [73] | |||
Antagonist | [+] 20 Antagonist drugs | + | ||||
1 | Ramatroban | Drug Info | [39] | |||
2 | Ifetroban sodium | Drug Info | [40] | |||
3 | BIBV 308 | Drug Info | [40] | |||
4 | DT-TX-30 | Drug Info | [13] | |||
5 | Domitroban | Drug Info | [42], [43] | |||
6 | Seratrodast | Drug Info | [45] | |||
7 | Terutroban sodium | Drug Info | [46] | |||
8 | ICI-192605 | Drug Info | [47] | |||
9 | Linotroban | Drug Info | [48] | |||
10 | SQ-30741 | Drug Info | [49], [50] | |||
11 | Z-335 | Drug Info | [50], [51] | |||
12 | KT2-962 | Drug Info | [50], [53] | |||
13 | KW-3635 | Drug Info | [54] | |||
14 | AH23848 | Drug Info | [41] | |||
15 | I-SAP | Drug Info | [68] | |||
16 | ONO-3708 | Drug Info | [69] | |||
17 | ONO-8809 | Drug Info | [50], [70] | |||
18 | [125I]PTA-OH | Drug Info | [75] | |||
19 | [125I]SAP | Drug Info | [68] | |||
20 | [125I]SQ-29548 | Drug Info | [76] | |||
Agonist | [+] 17 Agonist drugs | + | ||||
1 | PGF2alpha | Drug Info | [41] | |||
2 | 10,10-difluoro TXA2 | Drug Info | [62] | |||
3 | AGN 191976 | Drug Info | [63] | |||
4 | AGN192093 | Drug Info | [63] | |||
5 | butaprost (free acid form) | Drug Info | [41] | |||
6 | carbacyclin | Drug Info | [41] | |||
7 | carbocyclic thromboxane A2 | Drug Info | [65] | |||
8 | cloprostenol | Drug Info | [41] | |||
9 | EP 171 | Drug Info | [66] | |||
10 | fluprostenol | Drug Info | [41] | |||
11 | I-BOP | Drug Info | [67] | |||
12 | M&B 28767 | Drug Info | [41] | |||
13 | PGH2 | Drug Info | [65] | |||
14 | SQ 26655 | Drug Info | [72] | |||
15 | STA2 | Drug Info | [67] | |||
16 | U46619 | Drug Info | [41] | |||
17 | [125I]BOP | Drug Info | [74] |
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 | 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 10 | 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 11 | ClinicalTrials.gov (NCT00229437) Efficacy and Safety Study of TAK-128 in Treating Subjects With Diabetic Peripheral Neuropathy. U.S. National Institutes of Health. | |||||
REF 12 | 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 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 | 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 15 | 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 16 | Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81. | |||||
REF 17 | 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 18 | 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 19 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
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 | 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 22 | 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 23 | 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 24 | 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 25 | 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 26 | 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 27 | 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 28 | 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 29 | 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 30 | 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 31 | 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 32 | 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 33 | 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 34 | 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 35 | 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 36 | 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 37 | 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 38 | Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806. | |||||
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 | Terutroban and endothelial TP receptors in atherogenesis. Med Sci (Paris). 2006 Apr;22(4):437-43. | |||||
REF 47 | 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 48 | 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 49 | 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 50 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 51 | 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 52 | Blood pressure effects of thromboxane A2 blockade in spontaneously hypertensive rats. Clin Exp Pharmacol Physiol. 1993 Nov;20(11):679-87. | |||||
REF 53 | 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 54 | Antithrombotic effects of KW-3635, a thromboxane A2-receptor antagonist, in guinea pigs. Jpn J Pharmacol. 1994 Jun;65(2):93-8. | |||||
REF 55 | 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 56 | 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 57 | Conformationally-restricted analogs of TXA2 antagonist SQ 33,961: Receptor binding conformation of the carboxyl sidechain. Bioorganic & Medicinal Chemistry Letters Volume 1, Issue 9, 1991, Pages 465-470. | |||||
REF 58 | The PGI2-analogue iloprost and the TXA2-receptor antagonist sulotroban synergistically inhibit TXA2-dependent platelet activation. Prostaglandins. 1988 Dec;36(6):751-60. | |||||
REF 59 | Synthesis and structure-activity relationships of novel benzimidazole and imidazo[4,5-b]pyridine acid derivatives as thromboxane A2 receptor antagonists. J Med Chem. 1993 Apr 30;36(9):1175-87. | |||||
REF 60 | 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 61 | 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 62 | 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 63 | 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 64 | Synthesis and pharmacological evaluation of novel nitrobenzenic thromboxane modulators as antiplatelet agents acting on both the alpha and beta iso... J Med Chem. 2006 Jun 15;49(12):3701-9. | |||||
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 | 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 67 | 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 68 | 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 69 | 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 70 | Anti-thrombotic effect of ONO-8809, a novel TXA2/PG endoperoxide receptor antagonist. Adv Prostaglandin Thromboxane Leukot Res. 1991;21B:599-602. | |||||
REF 71 | Antithrombotic effects of S 18886, a novel orally active thromboxane A2 receptor antagonist. J Thromb Haemost. 2004 Mar;2(3):492-8. | |||||
REF 72 | 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 73 | 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 74 | Characterization of an 125I-labeled thromboxane A2/prostaglandin H2 receptor agonist. J Pharmacol Exp Ther. 1989 Nov;251(2):557-62. | |||||
REF 75 | Binding of thromboxane A2/prostaglandin H2 agonists to human platelets. Br J Pharmacol. 1987 May;91(1):223-7. | |||||
REF 76 | 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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