Thromboxane A2 analogs

Wilson, N. and Jones, R. (1985). Prostaglandin endoperoxides and thromboxane A2 analogs. In Pike, J. and Morton, D. (eds.) Advances in Prostaglandin, Thromboxane and Leukotriene Research, pp. 393-426. (New York Raven Press)... 

Gorman, R., Maxey, K. and Bundy, G. (1981). Inhibition of human platelet thromboxane synthase by lla-carba-thromboxane A2 analogs. Biochem. Biophys. Res. Commun., 100, 184-190... 

The compound cordycepin has been shown to completely inhibit aggregation of human platelets induced by U46619 (a thromboxane A2 analog) (Cho et al. 2006). Similarly, dose-dependent inhibition of collagen-induced human platelet aggregation by cordycepin in the presence of various concentrations of exogenous CaCl2 has been observed (Cho et al. 2007). 

Thromboxane A2 is a potent platelet aggregating agent and vasodilator which undergoes rapid hydrolysis under physiological conditions (ti/2 32 sec. at pH 7 and 37°C). The synthesis of stable analogs was of interest for biological studies of this potent but evanescent prostanoid. 

Fluoro prostaglandin, (IV), PGF2a analogs effective as thromboxane A2 receptor agonists were prepared by Klimko (3) and used in the treatment of glaucoma and ocular hypertension. 

Prostacyclin and its analogs (prostanoids) (Fig. 29.13) are potent vasodilators and possess antithrombotic and antiproliferative properties. Prostacyclin is derived from the endothelium of VSM, and its synthesis is reduced in patients with PAH. Its physiological antagonist, thromboxane A2, is increased, however, causing vasoconstriction. Prostacyclin produces its ... 

Johnson. R.A. Gorman. R.R. Wnuk, R.J. Crittenden. N.J. Aiken. J.W. Troger s base. An alternate synthesis and a structural analog with thromboxane A2 synthetase inhibitory activity. J. Med. Chem. 1993. 36, 3202-3206. 

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