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British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1998 May;124(1):1–3. doi: 10.1038/sj.bjp.0701837

Competitive and selective antagonism of P2Y1 receptors by N6-methyl 2′-deoxyadenosine 3′,5′-bisphosphate

José L Boyer 1,*, Arvind Mohanram 1, Emidio Camaioni 2, Kenneth A Jacobson 2, T Kendall Harden 1
PMCID: PMC1565379  PMID: 9630335

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: P2Y1 antagonist, P2Y1 receptor, inositol lipid signalling, turkey erythrocytes, phospholipase C

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