P2Y13: identification and characterization of a novel Gαi-coupled ADP receptor from human and mouse
FL Zhang, L Luo, E Gustafson, K Palmer, X Qiao… - … of Pharmacology and …, 2002 - ASPET
FL Zhang, L Luo, E Gustafson, K Palmer, X Qiao, X Fan, S Yang, TM Laz, M Bayne…
Journal of Pharmacology and Experimental Therapeutics, 2002•ASPETWe have identified an orphan G protein-coupled receptor, SP174, that shares a high degree
of homology with the recently described ADP receptor P2Y12. mRNA for SP174 is abundant
in the brain and in cells of the immune system. In the present study, we demonstrate that
SP174 is also a receptor for ADP, which is coupled to Gαi. ADP potently stimulates SP174
with an EC50 of 60 nM, and other related nucleotides are active as well, with a rank order of
potency 2-methylthio-ADP tetrasodium= adenosine 5′-O-2-(thio) diphosphate= 2 …
of homology with the recently described ADP receptor P2Y12. mRNA for SP174 is abundant
in the brain and in cells of the immune system. In the present study, we demonstrate that
SP174 is also a receptor for ADP, which is coupled to Gαi. ADP potently stimulates SP174
with an EC50 of 60 nM, and other related nucleotides are active as well, with a rank order of
potency 2-methylthio-ADP tetrasodium= adenosine 5′-O-2-(thio) diphosphate= 2 …
We have identified an orphan G protein-coupled receptor, SP174, that shares a high degree of homology with the recently described ADP receptor P2Y12. mRNA for SP174 is abundant in the brain and in cells of the immune system. In the present study, we demonstrate that SP174 is also a receptor for ADP, which is coupled to Gαi. ADP potently stimulates SP174 with an EC50 of 60 nM, and other related nucleotides are active as well, with a rank order of potency 2-methylthio-ADP tetrasodium = adenosine 5′-O-2-(thio)diphosphate = 2-methylthio-ATP tetrasodium > ADP > AP3A >ATP > IDP. This pharmacological profile is similar to that for P2Y12. We have also identified the murine homolog of SP174, which exhibits 75% homology to the human receptor. ADP is also a potent agonist at the murine receptor, and its pharmacological profile is similar to its human counterpart, but ADP and related nucleotides are more potent at the murine receptor than the human receptor. In keeping with the general nomenclature for the purinergic receptors, we propose designating this novel receptor P2Y13.
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