GPIIb/IIIa receptor antagonists,

Mousa SA (1999) Antiplatelet therapies from Aspirin to GPIIb/IIIa receptor antagonists and beyond. Drag Discov Today 4(12) 552-561... 

Mousa SA, Bozarth JM, Edwards S et al (1998) Novel technetium 99m-labeled GPIIb/IIIa receptor antagonists as potential imaging agents for venous and arterial thrombosis. Coron Artery Dis 9 131-141... 

Aminomethyl)pyrrole-2-carboxylic acid (85, Scheme 24) was used with good results as a spacer in the synthesis of cyclic peptide GPIIb/IIIa receptor antagonists.[74 The 1,2-sub-stituted pyrrole 8 represents a cis peptide bond surrogate in which the R1 side chain can easily be varied. However, no application in biologically relevant peptides have been reported to date. 

Lincoff, A. M., and Korngold, S. (1999). An overview of platelet GPIIb/IIIa receptor antagonists trials. Eur. Heart. J. Supplements 1 (Suppl E), E18-E26. 

Burcham DL, Aungst BJ, Hussain M, Gorko MA, Quon CY, Huang S-M (1995) The effect of absorption enhancers on the oral absorption of the GPIIb/IIIa receptor antagonist, DMP 728, in rats and dogs. Pharm Res 12 2065-2070... 

Rote WE, Davis JH, Mousa SA et al. (1994) Antithrombotic effects of DMP 728, a platelet GPIIb/IIIa receptor antagonist, in a canine model of arterial thrombosis. J Cardiovasc Pharmacol 23 681-689... 

F ure 3.28. Peptidomimetics that have been designed based on iterative introduction of constraints into parent peptide and hypotheses concerning receptor-bound conformation. Enkephalin mimetic (388), RGD platelet GPIIb/IIIa receptor antagonists (384,385), thyrohberin [TRH (387)], and somatostatin (383,389).For an overview of recent approaches to peptidomimetic design, see the review by Bursavich and Rich (382). 

Clinically important, potentially hazardous interactions with amiodarone, clarithromycin, clopidogrel, desirudin, dextran, fondaparinux, gpiib/iiia receptor antagonists, heparin, quinidine, rifampin, St John s wort, sulfinpyrazone, thrombolytic agents, tidopidine, verapamil, vitamin k antagonists... 

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