Thromboxane synthetase inhibitor

Drugs that target other sites of platelet action include thromboxane synthetase inhibitors, serotonin or 5-hydroxytryptamine (5-HT2) receptor blockers, and thromboxane A2 receptor blockers, in addition to cyclooxygenase inhibitors and prostaglandin analogues. 

Banerjee AK, Peters TJ Experimental nonsteroidal anti-inflammatory drug-induced enteropathy in the rat Similarities to inflammatory bowel disease and effect of thromboxane synthetase inhibitors. Gut 1990 3 i 1358— 1364. 

Tokiyoshi K, Ohnishi T, Nii Y. 1991. Efficacy and toxicity of thromboxane synthetase inhibitor for cerebral vasospasm after subarachnoid hemorrhage. Surg Neurol 36 112-118. 

Uyama O, Nagatsuka K, Nakabayashi S, Isaka Y, Yoneda S, et al. 1985. The effect of a thromboxane synthetase inhibitor, OKY-046, on urinary excretion of immunoreactive thromboxane B2 and 6-keto-prostaglandin El alpha in patients with ischemic cerebrovascular disease. Stroke 16 241-244. 

Hall and Wolf [217] have proposed a hypothesis, concerning the pathogenesis of post-traumatic central nervous system ischaemia, which integrates an injury-induced rise in intracellular Ca2+, the increased synthesis of vasoactive prostanoids and progressive microvascular lipid peroxidation. The model used anaesthetised cats with a contusion injury to the lumbar spinal cord. Antioxidants, vitamin E and selenium, were compared with various Ca2 + antagonists, cyclo-oxygenase inhibitors, a thromboxane synthetase inhibitor and the stable prostacyclin analogue. The most impressive preservation of post-traumatic spinal cord blood flow was provided by the antioxidants. 

Kyowa Hakko Kogyo Co.) anti-inflammatory thromboxane synthetase inhibitor "discovery ... 

Gladue RP, Newborg MF. The protective effects of the thromboxane synthetase inhibitor Dazmegrel on nephrotoxicity in cyclosporine-treated rats.Transplantation 1991 52 837-841. 

Moore J N, Hardee M M, HanJee G E 1986 Modulation of arachidonic acid metabolism in endotoxic horses comparison of flunixin meglumine, phenylbutazone and a selective thromboxane synthetase inhibitor. American Journal of Veterinary Research 47 110-113... 

NAF nafimidone. nafagrel [inn] (DP 1904) is an imidazolylmethylnaphthalenecarboxylic acid, a THROMBOXANE SYNTHETASE INHIBITOR. It inhibits renal thromboxane B2 production and renal damage in hypertensive diabetic rats, nafamostat [inn] (nafamostat mesylate [usan] nafamostat mesilate [jan] FUT 175) is a naphthyl derivative, an ENZYME INHIBITOR active as a (serine) PROTEASE inhibitor and anticomplement agent. It acts as an ANTIFIBRINOLYTIC and PLATELET AGGREGATION INHIBITOR, and can be used for the treatment of acute pancreatitis and cerebrovascular disorders. 

Other examples are symmetrical bradykinin antagonists and symmetrical lexitropsins (netropsine, distamycine), active against HTV-I viruses. Non-symmetrical polymethylenic thromboxane synthetase inhibitors are described by Press et al The compounds contain a thiophene-2-carboxamide moiety, separated from an imidazole ring by 3-8 methylene units. Surprisingly, whereas most of the compounds show... 

Kato, K., Ohkawa, S., Terao, S., Terashita, Z. I., Nishikava, K. Thromboxane synthetase inhibitors (TXSI). Design, synthesis, and evaluation of a novel series of omega-pyridylalkenoic acids. J. Med. Chem. 1985, 28, 287-294. 

Thromboxane A2 is produced by alveolar macrophages, fibroblasts, epithelial cells, neutrophils, and platelets within the lung. Indirect evidence from animal models suggests that thromboxane A2 may have several effects, including bronchoconstriction, involvement in the late asthmatic response, and involvement in the development of airway inflammation and BHR. Potent and specific thromboxane synthetase inhibitors will be crucial tools for understanding the role of thromboxanes in asthma. 

Yu M, Tomasa G. A double-blind, prospective, randomized trial for ke-toconazole, a thromboxane synthetase inhibitor, in the prophylaxis of the adult respiratory distress syndrome. Crit Care Med 1993 21 1635-1642. 

Some 1,5-disubstituted imidazoles have been found to exhibit potent inhibitory activity against platelet aggregation and as thromboxane synthetase inhibitors. Hence synthesis of imidazole analogues of prostaglandin require 1,5-orientation. Good yields of these desired isomers are obtained when 4-/-butyldimethylsilyloxymethylimidazole is treated in succession with butyllithium and an... 

Smeesters C, Chaland P, Giroux L, Moutquin JM, Etienne P, Douglas F, Corman J, St Louis G, Daloze P. Prevention of acute cyclosporine A nephrotoxicity by a thromboxane synthetase inhibitor. Transplant Proc 1988 20 658-664. 

Phospholipase inhibitors Thromboxane synthetase inhibitors Prostacyclin... 

Press, J.B., Wright, W.B., Jr., Chan, P.S., Haug, M.F., Marsico, J.W., etal. (1987) Thromboxane synthetase inhibitors and antihypertensive agents. 3. A -[(lH-imidazol-l-yl)alkyl]heteroaryl amides as potent enzyme inhibitors. J. Med. Chem. 30 1036-1040. 

Zheng, N. X. et al., Pharmacokinetic-pharmacodynamic modehng of DP-1904, a novel thromboxane synthetase inhibitor in rabbits, based on an indirect response model, Eur. J. Drug Metab. Pharmacokinet., 21(4) 285-293, 1996. 

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