For research use only. Not for therapeutic Use.
Terbogrel, also known as BIBV-308; BIBV-308-SE; BIBV-308SE, is a thromboxane A2 receptor antagonist potentially for the treatment of pulmonary arterial hypertension. Terbogrel concentration-dependently inhibited collagen (0.6 microg/ml)- and U46619 (11alpha,9alpha-epoxymethano-15(S)-hydroxy-prosta-5Z,+ ++13E-dienoic acid) (1 microM)-induced aggregation and thromboxane synthesis of washed human platelets. In this system, terbogrel exhibited an equipotent (IC50 of about 10 nM) activity as thromboxane A2 synthase inhibitor and thromboxane A2 receptor antagonist. Terbogrel appears to be a compound with an equipotent molar potency as thromboxane A2 synthase inhibitor and receptor antagonist.
Catalog Number | M096083 |
CAS Number | 149979-74-8 |
Molecular Formula | C11H16O |
Purity | ≥95% |
Target | Prostaglandin Receptor |
Storage | Store at -20°C |
Reference | </br> 1: Zhang HD, Zhang R, Jiang X, Sun K, Wu DC, Jing ZC. Effects of oral treatments on clinical outcomes in pulmonary arterial hypertension: A systematic review and meta-analysis. Am Heart J. 2015 Jul;170(1):96-103, 103.e1-14. doi: 10.1016/j.ahj.2015.04.003. Review. PubMed PMID: 26093869.</br> 2: More AS, Kim HM, Khang G, Hildebrandt T, Bernlöhr C, Doods H, Vanhoutte PM, Wu D. Des-Arg9-bradykinin causes kinin B1 receptor mediated endothelium-independent contractions in endotoxin-treated porcine coronary arteries. Pharmacol Res. 2014 Dec;90:18-24. doi: 10.1016/j.phrs.2014.09.001. PubMed PMID: 25258294.</br> 3: More AS, Kim HM, Zhao R, Khang G, Hildebrandt T, Bernlöhr C, Doods H, Lee D, Lee SH, Vanhoutte PM, Wu D. COX-2 mediated induction of endothelium-independent contraction to bradykinin in endotoxin-treated porcine coronary artery. J Cardiovasc Pharmacol. 2014 Sep;64(3):209-17. doi: 10.1097/FJC.0000000000000105. PubMed PMID: 25192543.</br> 4: Ivandic BT, Giannitsis E, Schlick P, Staritz P, Katus HA, Hohlfeld T. Determination of aspirin responsiveness by use of whole blood platelet aggregometry. Clin Chem. 2007 Apr;53(4):614-9. PubMed PMID: 17332149.</br> 5: Fike CD, Zhang Y, Kaplowitz MR. Thromboxane inhibition reduces an early stage of chronic hypoxia-induced pulmonary hypertension in piglets. J Appl Physiol (1985). 2005 Aug;99(2):670-6. PubMed PMID: 15802364.</br> 6: Lowson SM. Alternatives to nitric oxide. Br Med Bull. 2004 Nov 5;70:119-31. Review. PubMed PMID: 15531733.</br> 7: Guth BD, Narjes H, Schubert HD, Tanswell P, Riedel A, Nehmiz G. Pharmacokinetics and pharmacodynamics of terbogrel, a combined thromboxane A2 receptor and synthase inhibitor, in healthy subjects. Br J Clin Pharmacol. 2004 Jul;58(1):40-51. PubMed PMID: 15206991; PubMed Central PMCID: PMC1884538.</br> 8: Zimmermann N, Wenk A, Kim U, Kienzle P, Weber AA, Gams E, Schrör K, Hohlfeld T. Functional and biochemical evaluation of platelet aspirin resistance after coronary artery bypass surgery. Circulation. 2003 Aug 5;108(5):542-7. PubMed PMID: 12874188.</br> 9: Galiè N, Manes A, Branzi A. Emerging medical therapies for pulmonary arterial hypertension. Prog Cardiovasc Dis. 2002 Nov-Dec;45(3):213-24. Review. PubMed PMID: 12525997.</br> 10: Galiè N, Manes A, Branzi A. The new clinical trials on pharmacological treatment in pulmonary arterial hypertension. Eur Respir J. 2002 Oct;20(4):1037-49. Review. PubMed PMID: 12412701.</br> 11: Langleben D, Christman BW, Barst RJ, Dias VC, Galiè N, Higenbottam TW, Kneussl M, Korducki L, Naeije R, Riedel A, Simonneau G, Hirsch AM, Rich S, Robbins IM, Oudiz R, McGoon MD, Badesch DB, Levy RD, Mehta S, Seeger W, Solèr M. Effects of the thromboxane synthetase inhibitor and receptor antagonist terbogrel in patients with primary pulmonary hypertension. Am Heart J. 2002 May;143(5):E4. PubMed PMID: 12040360.</br> 12: Michaux C, Rolin S, Dogné JM, Durant F, Masereel B, Delarge J, Wouters J. Structure determination and comparison of BM567, a sulfonylurea, with terbogrel, two compounds with dual action, thromboxane receptor antagonism and thromboxane synthase inhibition. Bioorg Med Chem Lett. 2001 Apr 23;11(8):1019-22. PubMed PMID: 11327579.</br> 13: Michaux C, Norberg B, Dogné JM, Durant F, Masereel B, Delarge J, Wouters J. Terbogrel, a dual-acting agent for thromboxane receptor antagonism and thromboxane synthase inhibition. Acta Crystallogr C. 2000 Oct;56 ( Pt 10):1265-6. PubMed PMID: 11025320.</br> 14: Soyka R, Guth BD, Weisenberger HM, Luger P, Müller TH. Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors. J Med Chem. 1999 Apr 8;42(7):1235-49. PubMed PMID: 10197967.</br> 15: Muck S, Weber AA, Schrör K. Effects of terbogrel on platelet function and prostaglandin endoperoxide transfer. Eur J Pharmacol. 1998 Feb 26;344(1):45-8. PubMed PMID: 9570446.</br></br></br> |