Title : Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor.

Pub. Date : 2016 Dec 8

PMID : 27694321






6 Functional Relationships(s)
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1 Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor. Ticagrelor solute carrier family 29 member 1 (Augustine blood group) Homo sapiens
2 This additional effect of ticagrelor beyond P2Y12R antagonism was in part as a consequence of ticagrelor inhibiting the equilibrative nucleoside transporter 1 (ENT1) on platelets, leading to accumulation of extracellular adenosine and activation of Gs-coupled adenosine A2A receptors. Ticagrelor solute carrier family 29 member 1 (Augustine blood group) Homo sapiens
3 This additional effect of ticagrelor beyond P2Y12R antagonism was in part as a consequence of ticagrelor inhibiting the equilibrative nucleoside transporter 1 (ENT1) on platelets, leading to accumulation of extracellular adenosine and activation of Gs-coupled adenosine A2A receptors. Ticagrelor solute carrier family 29 member 1 (Augustine blood group) Homo sapiens
4 This additional effect of ticagrelor beyond P2Y12R antagonism was in part as a consequence of ticagrelor inhibiting the equilibrative nucleoside transporter 1 (ENT1) on platelets, leading to accumulation of extracellular adenosine and activation of Gs-coupled adenosine A2A receptors. Ticagrelor solute carrier family 29 member 1 (Augustine blood group) Homo sapiens
5 This additional effect of ticagrelor beyond P2Y12R antagonism was in part as a consequence of ticagrelor inhibiting the equilibrative nucleoside transporter 1 (ENT1) on platelets, leading to accumulation of extracellular adenosine and activation of Gs-coupled adenosine A2A receptors. Ticagrelor solute carrier family 29 member 1 (Augustine blood group) Homo sapiens
6 In summary, our studies describe 2 novel modes of action of ticagrelor, inhibition of platelet ENT1 and inverse agonism at the P2Y12R that contribute to its effective inhibition of platelet activation. Ticagrelor solute carrier family 29 member 1 (Augustine blood group) Homo sapiens