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Competitive and selective antagonism of P2Y 1 receptors by N 6 ‐methyl 2′‐deoxyadenosine 3′,5′‐bisphosphate
Author(s) -
Boyer José L,
Mohanram Arvind,
Camaioni Emidio,
Jacobson Kenneth A,
Harden T Kendall
Publication year - 1998
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0701837
Subject(s) - antagonism , receptor , chemistry , deoxyadenosine , p2y receptor , stereochemistry , neuroscience , biochemistry , biology , dna , agonist
The antagonist activity of N 6 ‐methyl 2′‐deoxyadenosine 3′,5′‐bisphosphate (N6MABP) has been examined at the phospholipase C‐coupled P2Y 1 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 P2Y 1 receptor antagonism observed with N6MABP was competitive as revealed by Schild analysis (pK B =6.99±0.13). Whereas N6MABP was an antagonist at the human P2Y 1 receptor, no antagonist effect of N6MABP was observed at the human P2Y 2 , human P2Y 4 or rat P2Y 6 receptors.