Competitive and selective antagonism of P2Y 1  receptors by  N  6 ‐methyl 2′‐deoxyadenosine 3′,5′‐bisphosphate | Zendy

Boyer José L | Zendy; Mohanram Arvind | Zendy; Camaioni Emidio | Zendy; Jacobson Kenneth A | Zendy; Harden T Kendall | Zendy

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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.

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