Thromboxane mimetic

Halmi M, Haye B, Oavaret JM, Vargaftig BB, Jacquemin C. Alkaline phosphatase prevents platelet stimulation by thromboxane-mimetics. Br J Pharmacol 1991 104 554-8... 

Margolin N, True TA, Saussy Ir DL, Mais DE. Effect of alkaline phosphatase on thromboxane mimetic induced platelet activation. Prosts andins 1994 48 235-46... 

Alternatively, the increased pulmonary vascular resistance may be due to an increase in a circulating vasoconstrictor such as endothelin or thromboxane, both of which have been reported to be elevated in children with congenital heart disease following cardiopulmonary bypass. It is noteworthy that the excretion of thromboxane has been found to be elevated during a pulmonary hypertensive crisis ° and that in animal studies inhaled nitric oxide is effective in reversing the pulmonary vasoconstriction induced by thromboxane mimetics. ... 

Whittle, B.J.R., Oren-Wolman, N. and Guth, P.H. (1985). Gastric vasoconstrictor actions of leukotriene C4, PGp2a, and thromboxane mimetic U-46619 on rat submucosal microcirculation in vivo. Am. ]. Physiol, 248, G580-G586... 

Figure 3(a-c) demonstrates a comparison between the abnormal contraction in the SHR that develops spontaneously after the inhibition of endothelial cell NO and the contractions elicited by the thromboxane mimetic U46619 and E2 and F2 isoprostanes (8-iso-prostaglandin E2 and 8-iso-prostaglandin F2 ). It can be seen that the abnormality... 

The reaction of furans with ethyl 2,2-difluoro-l-diethylamino-carboxyacrylate generates fluorinated 7-oxanorbomenes [163]. These cycloadducts undergo alkene catalytic hydrogenation (or other reactions) into the corresponding 7-oxabicyclo[2.2.1]heptanes. Examples have been presented with the synthesis of norcantharidin, 5, with the synthesis of the 2-epimer of rac-3, 6 -epoxyauraptene, 32 (Scheme 3), and with the synthesis of thromboxane mimetics (Scheme 8). In 1929, Diels and Alder first reported the reaction of furan with maleic anhydride that produces at room temperature the exo-adduct 132 [164]. In 1962, Anet found that at low temperature, the reaction produces first the ew fo-adduct 133 in agreement with the endo Alder rule [165]. At 25 °C and in MeCN, the exo-adduct 132 is more stable by 1.9 kcal/mol compared with 133 [166] (Scheme 20). 

The ring expansion reaction has been used in multistep organic syntheses of natural products and analogs, most notably in the preparation of prostaglandins and prostanoids, thromboxane mimetics, and muscarine (Scheme 4). 

Zhao Y, Foegh ML. Angiopeptin, a somatostatin analogue, inhibits rat coronary artery and aorta smooth musde cell proliferation induced by the thromboxane Aj mimetic U46619. Prostaglandins 1997 54 781-93... 

Lid N, Mats DE, Haluslika PV. Desensitization of platdet thromboxane Aj/prostaglandin Hj recqttors by the mimetic TJ46619. J Pharmacol Exp Ther 1988 247 1133-8... 

Morinelli TA, Finley EL, Jaffa AA, Kurtz DT, Ullian ME. Tyrosine phosphcaylatkm of phosphatidylinositiol 3-kinaW and of the thromboxane Aj (TXAi) receptor by TXAj mimetic 1-BOP in A7r5 cells Biodiem Pharmacol 1997 53 1823-32. 

Maeda H, Taniguchi T, Inazu T, Yang C, Nakagawara G, Yamamura H. Proteiii-tyrosine kinase p72 is activated by thromboxane Aj mimetic U44069 in platelets Biochem Biophys Res Commun 1993 197 62-7... 

For prediction of likely in vivo activity, inhibition of ADP or U-46619 (a stable thromboxane A2 mimetic) induced platelet aggregation has been measured in citrated whole blood. The extent of aggregation is determined using a single platelet counter [33, 35, 38], Compounds may be less potent in the whole blood assay than in the partially purified platelet assays described above if the drug is significantly bound to plasma proteins. 

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