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Vol. 301, Issue 2, 705-713, May 2002
i-Coupled ADP Receptor from Human and Mouse
Human Genome Research (F.L.Z., L.L., E.G., X.Q., S.Y., T.M.L.,
M.B., F.M.), Immunology Department (K.P., X.F.), Schering-Plough
Research Institute, Kenilworth, New Jersey
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 G
i. 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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