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 (pK(B) = 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
This publication has 10 references indexed in Scilit:
- Deoxyadenosine Bisphosphate Derivatives as Potent Antagonists at P2Y1 ReceptorsJournal of Medicinal Chemistry, 1998
- Molecular Cloning and Expression of an Avian G Protein-Coupled P2Y ReceptorMolecular Pharmacology, 1997
- Avian and human homologues of the P2Y1 receptor: Pharmacological, signaling, and molecular propertiesDrug Development Research, 1996
- PPADS and suramin as antagonists at cloned P2Y‐ and P2U‐purinoceptorsBritish Journal of Pharmacology, 1996
- Pharmacological profile of the novel P2T-purinoceptor antagonist, FPL 67085 in vitro and in the anaesthetized rat in vivoBritish Journal of Pharmacology, 1995
- P2-Purinergic Receptors: Subtype-Associated Signaling Responses and StructureAnnual Review of Pharmacology and Toxicology, 1995
- Differential effects of P2‐purinoceptor antagonists on phospholipase C‐ and adenylyl cyclase‐coupled P2Y‐purinoceptorsBritish Journal of Pharmacology, 1994
- P2-purinoceptor antagonists discriminate three contraction-mediating receptors for ATP in rat vas deferensNaunyn-Schmiedebergs Archiv für experimentelle Pathologie und Pharmakologie, 1994
- PPADS selectively antagonizes P2X‐purinoceptor‐mediated responses in the rabbit urinary bladderBritish Journal of Pharmacology, 1993
- PPADS, a novel functionally selective antagonist of P2 purinoceptor-mediated responsesEuropean Journal of Pharmacology, 1992