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  • Title: A photoaffinity label for the thromboxane A2/prostaglandin H2 receptor in human blood platelets.
    Author: Kattelman EJ, Arora SK, Lim CT, Venton DL, Le Breton GC.
    Journal: FEBS Lett; 1987 Mar 09; 213(1):179-83. PubMed ID: 2951273.
    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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