Title : Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog.

Pub. Date : 2004 Dec

PMID : 15345752






3 Functional Relationships(s)
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Protein Name
Organism
1 ADP is the cognate agonist of the P2Y1, P2Y12, and P2Y13 receptors. Adenosine Diphosphate purinergic receptor P2Y12 Homo sapiens
2 In the case of the Gi-linked P2Y12 and P2Y13 receptors, a chimeric G protein, Galphaq/i, was coexpressed to confer a capacity of these Gi-linked receptors to activate phospholipase C. 2MeSADP (2-methylthio-ADP) was a potent agonist at all three receptors exhibiting EC50 values in the sub to low nanomolar range. methylthio-ADP purinergic receptor P2Y12 Homo sapiens
3 The P2Y1 receptor selectivity of (N)-methanocarba-2MeSADP was confirmed in human platelets where it induced the shape change promoted by P2Y1 receptor activation without inducing the sustained platelet aggregation that requires simultaneous activation of the P2Y12 receptor. (N)-methanocarba-2MeSADP purinergic receptor P2Y12 Homo sapiens