A photoaffinity label for the thromboxane A2/prostaglandin H2 receptor in human blood platelets

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...

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Bibliographic Details
Published in:FEBS letters 1987-03, Vol.213 (1), p.179-183
Main Authors: Kattelman, E.J., Arora, S.K., Lim, C.T., Venton, D.L., Le Breton, G.C.
Format: Article
Language:English
Subjects:
Affinity Labels - metabolism
Aspirin - pharmacology
Binding, Competitive
Blood Platelets - metabolism
Humans
Photoaffinity label
Photolysis
Platelet
Platelet Aggregation
Prostaglandin Endoperoxides, Synthetic - metabolism
Prostanoic Acids - metabolism
Receptors, Prostaglandin - metabolism
Receptors, Thromboxane
Receptors, Thromboxane A2, Prostaglandin H2
Thromboxane receptor
U46619
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Summary: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 radio‐iodinated form will prove to be useful tools for the isolation and purification of the TXA2/PGH2‐binding protein in human platelets.
ISSN:0014-5793
1873-3468
DOI:10.1016/0014-5793(87)81487-4