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.
Competitive and selective antagonism of P2Y(1) receptors by N-6-methyl 2 '-deoxyadenosine 3 ',5 '-bisphosphate
CAMAIONI, Emidio;
1998
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
