Thromboxane receptor antagonists

A ferret model of acute arterial thrombosis was developed by Schumacher et al. (1996a,b). A 10-min anodal electrical stimulation of 1 mA was delivered to the external surface of the carotid artery while measuring carotid blood flow. This produced an occlusive thrombus in all vehicle treated ferrets within 41 3 min with an average weight of 8 1 mg. Thrombus weight was reduced by aspirin or a thromboxan receptor antagonist. 

A direct effect of AmB on cell function was suggested by in vitro experiments, which demonstrated a vasoconstrictor action of AmB in perfused afferent arterioles and isometrically contracting rings of rabbit aorta or renal artery, effects which were prevented in Ca -free medium and by Ca" " channel blockers or theophylline [103]. Thus, AmB-induced reductions in RBF or GFR are not secondary to activation of TGF, but due to its direct vasoconstrictor effect. A role for thromboxane A2 has also been suggested based upon partial inhibition of the AmB-induced vasoconstriction and reduction in GFR by pretreatment with ibuprofen or a thromboxane receptor antagonist [104]. 

Beasley, C.RW., Featherstone, RL., Church, M.K., Ra rty, P., Varley, J.G., Harris, A. and Holgate, S.T. (1989b). Effea of a thromboxane receptor antagonist on PGD2- and allergen-induced bronchoconstriction. J. Appl. Physiol. 66, 1685-1693. 

Gresek. P. era/. (1991) Thromboxane synthase inhibitors, thromboxane receptor antagonists and dual blockers in thrombotic disorders. Trends Pharmacol Sci., 12.158-163. 

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. 

A tetrahydropyran that inhibits leukotriene biosynthesis Asymmetric synthesis of2-methyl-tetrahydropyran-4-one by kinetic resolution Part VI - Asymmetric Desymmetrisation of a Diels-Alder Adduct Ifetroban sodium a thromboxane receptor antagonist A laboratory synthesis starting with a Diels-Alder reaction Desymmetrisation of a symmetrical anhydride with a chiral Grignard reagent Laboratory and process routes compared Part VII - Asymmetric Synthesis of A Bicyclic 3-Lactone Lactacystin a naturalproteasome inhibitor... 

The chiral auxiliary substituents shield one face of the dienophile so the diene approaches the other. This methodology has been applied by Martinelli [418] to the synthesis of thromboxane receptor antagonists and by Hauser and Tomasi to the synthesis of daunomycinone antibiotics [417]. 

R. Aslam, and A. Sun (2002). A new family of thromboxane receptor antagonists with secondary thromboxane synthase inhibition. J. Pharmacol. Exp. Then 301, 618-624. 

I The thromboxane receptor antagonist SI 8886 but not aspirin inhibits atherogenesis in apo E-deficient mice evidence that... 

A number of stable thromboxane receptor antagonists have been reported. These include 13-aza-prostanoic acid, pinane thromboxane A " and the 7-oxabicycloheptane compounds, SQ 26,536 and SQ 29,548. ... 

Ashton, J.H., Ogletree, M.L., Taylor, A.L., Fitzgerald, C., Rakejo, S., Campbell, W.B., Buja, L.M. and Willerson, J.T. (1985). A thromboxane receptor antagonist, SQ 29,548, abolishes or attenuates cyclic flow variations in severely narrowed canine coronary arteries. Circulation, 72, (Suppl 111), 111—69... 

Brezinski, M.E., Yanagisawa, A. and Lefer, A.M. (1987). Cardioprotective effects of specific thromboxane receptor antagonist in acute myocardial ischemia. ]. Cardiovasc. Pharmacol, 9, 65-71... 

Mais, D., Knapp, D., Ballard, K., Hamanaka, N. and Halushka, P. (1984). Synthesis of thromboxane receptor antagonists with the potential to radiolabel with Tetrahedron Lett., 25, 4207-4208... 

Figure 3.20 Multi-kilogram scale synthesis of a thromboxane receptor antagonist utilizing -selective arylation of N-vinylphthalimide under phosphine-free Mizoroki-Heck conditions.

Davi G, Santilli F, VazzanaN (2012) Thromboxane receptors antagonists and/or synthase inhibitors. Handb Exp Pharmacol 210 261-286... 

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