A photoaffinity label for the thromboxane A2/prostaglandin H2 receptor in human blood platelets |
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| Authors: | E J Kattelman S K Arora C T Lim D L Venton G C Le Breton |
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| Affiliation: | 1. Department of Pharmacology, University of Illinois at Chicago, Chicago, IL 60612, USA;2. Department of Medicinal Chemistry, University of Illinois at Chicago, Chicago, IL 60612, USA;3. College of Medicine, University of Illinois at Chicago, Chicago, IL 60612, USA;4. College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA |
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| Abstract: | ![]()
A photoactive iodoarylazide derivative (I-APA-PhN3) of the competitive thromboxane A2/prostaglandin H2 (TXA2/PGH2) antagonist 13-azaprostanoic acid is evaluated. Upon photoactivation, the compound was found to inhibit specifically and irreversibly human platelet aggregation induced by the TXA2/PGH2 mimetic U46619. In receptor-binding studies using [3H]U46619, I-APA-PhN3 exhibited an IC50 of 300 nM for inhibition of U46619 binding. Photoactivation of I-APA-PhN3 resulted in an irreversible 58% reduction in specific binding of U46619. This compound and its corresponding ratio-iodinated form will prove to be useful tools for the isolation and purification of the TXA2/PGH2-binding protein in human platelets. |
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