Thromboxane receptor structure

SeptisoL hexachlorophane. seractide [ban. inn] (seractide acetate [usan]) is a synthetic peptide, a structural corticotrophin analogue, which has been used clinically. See also corticotrophin. seractide acetate seractide. seratrodast [inn] is a benzoquinone derivative, a THROMBOXANE RECEPTOR ANTAGONIST. It is a BRONCHODILATOR and ANTI ASTHMATIC. 

M. Takasuka, M. Kishi, M. Yamakawa, FTIR spectral study of intramolecular hydrogen bonding in thromboxane A2 receptor agonist (U-46619), prostaglandin (PG)E2, PGD2, PGF2.alpha., prostacyclin receptor agonist (carbacyclin) and their related compounds in dilute carbon tetrachloride solution Structure-activity relationships, J. Med. Chem. 37 (1994) 47. 

Albuquerque, M.G., Hopfinger, A.J., Barreiro, E.J. and de Alencastro, R.B. (1998). Four-Dimensional Quantitative Structure-Activity Relationship Analysis of a Series of Interphenylene 7-Qxabicycloheptane Qxazole Thromboxane A2 Receptor Antagonists. J.Chem.InfComput.ScL, 38,925-938. 

Nicolai, E., Goyard, J., Benchetrit, T., Teulon, J. M., Caussade, F., Virone, A., Delchambre, C., Cloarec, A. Synthesis and structure-activity relationships of novel benzimidazole and imidazo[4,5-h]pyridine acid derivatives as thromboxane A2 receptor antagonists. J. Med. Chem. 1992, 36, 1175-1187. 

Two other publications on the bioisosteric replacement of pyridine show similar results. The first paper reports the study of bioisosteric potential of diazines in the field of combined antithrombic thromboxane A2 synthetase inhibitors and receptor antagonists. On the basis of the structure-activity relationships (SAR) observed in this study, it turned out that only the 2-pyrazinyl, 4-pyridazinyl... 

Thromboxane A2 antagonists whose antiaggregant properties of platelets depends on blocking TXA2 receptors are also being discovered, so far without any structural relationships. Two of many such compounds are cited as examples. The sulfonamide phenoxy-acetic acid BM-13177 has antiplatelet effects not mediated by AA release, cyclooxygenase... 

Figure 6.3 Effect of two structurally distinct thromboxane A2/prostaglandin endoperoxide receptor antagonists, L636,499 and SQ29,548, on the time to coronary occlusion in the canine model of coronary thrombosis following electrically-induced endothelial injury...

Kontogiorgis C, Hadjipavlou-Litina D (2010) Thromboxane synthase inhibitors and thromboxane A2 receptor antagonists a quantitative structure activity relationships (QSARs) analysis. Curr Med Chem 17 3162 3214... 

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