Competitive and selective antagonism of P2Y1 receptors by N6‐methyl 2′‐deoxyadenosine 3′,5′‐bisphosphate
- 1 May 1998
- journal article
- Published by Wiley in British Journal of Pharmacology
- Vol. 124 (1) , 1-3
- https://doi.org/10.1038/sj.bjp.0701837
Abstract
The antagonist activity of N6‐methyl 2′‐deoxyadenosine 3′,5′‐bisphosphate (N6MABP) has been examined at the phospholipase C‐coupled P2Y1 receptor of turkey erythrocyte membranes. N6MABP antagonized 2MeSATP‐stimulated inositol phosphate hydrolysis with a potency approximately 20 fold greater than the previously studied parent molecule, adenosine 3′,5′‐bisphosphate. The P2Y1 receptor antagonism observed with N6MABP was competitive as revealed by Schild analysis (pKB=6.99±0.13). Whereas N6MABP was an antagonist at the human P2Y1 receptor, no antagonist effect of N6MABP was observed at the human P2Y2, human P2Y4 or rat P2Y6 receptors.Keywords
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