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Overview: Alongside the 7-transmembrane receptors listed in the Guide to Receptors and Channels, IUPHAR recognises a number of genes, which sequence analysis suggests code for 7-transmembrane receptors and for which an endogenous ligand has yet to be identified (Foord et al., 2006). Below are listed a number of these genes, for which preliminary evidence for an endogenous ligand has been published. Further Reading Citation InformationWe recommend that any citations to information in the Guide are presented in the following format:Alexander SPH, . Guide to Receptors and Channels (GRAC), 3rd edn. Br J Pharmacol 153 (Suppl. 2): S1-S209. GPR1 ENSG00000183671 GPR3 ENSG00000181773 ACCA GPR4 ENSG00000177464 Proton-sensing, sphingosylphosphorylcholine GPR6 ENSG00000146360 GPR10 ENSG00000119973 GPR12 ENSG00000132975 GPCR21 GPR15 ENSG00000154165 GPR19 ENSG00000183150 GPR20 ENSG00000204882 GPR21 ENSG00000188394 GPR22 ENSG00000172209 GPR25 ENSG00000170128 GPR26 ENSG00000154478 GPR27 ENSG00000170837 SREB1 GPR31 ENSG00000120436 GPR32 ENSG00000142511 GPR33 ENSMUSG00000035148 Pseudogene in man GPR37 ENSG00000170775 PAELR, EDNRLB GPR45 ENSG00000135973 PSP24 GPR48 ENSG00000205213 Leucine-rich repeat-containing G-protein coupled receptor 4 GPR49 ENSG00000139292LGR5, GPR67, FEX, HG38 , MGC117008 GPR50 ENSG00000102195 H9 GPR52 ENSG00000203737 GPR56 ENSG00000205336 TM7LN4, TM7XN1 GPR61 ENSG00000156097 BALGR GPR62 ENSG00000180929 GPR63 ENSG00000112218 PSP24B GPR64 ENSG00000173698 HE6 GPR65 ENSG00000140030 TDAG8 GPR68 ENSG00000119714 OGR1, Proton-sensing GPR70 ENSG00000173662 TAS1R1 GPR71 ENSG00000179002 TAS1R2 GPR72 ENSG00000123901 GPR83 GPR75 ENSG00000119737 WI31133 GPR77 ENSG00000134830 C5L2 GPR78 ENSG00000155269 GPR81 ENSG00000196917 TAGPCR, GPR104 GPR82 ENSG00000171657 GPR84 ENSG00000139572 EX33 GPR85 ENSG00000164604 SREB2 GPR87 ENSG00000138271 GPR95 GPR88 ENSG00000181656 STRG GPR90 ENSMUSG00000059408 Mas-related GPR, member H GPR97 ENSG00000182885 Pb99, PGR26 GPR98 ENSG00000164199 VLGR1 GPR101 ENSG00000165370 GPR107 ENSG00000148358 KIAA1624, RP11-88G17, FLJ20998, LUSTR1 GPR110 ENSG00000153292 hGPCR36, PGR19 GPR111 ENSG00000164393 hGPCR35, PGR20 GPR112 ENSG00000156920 RP1-299I16, PGR17 GPR113 ENSG00000173567 hGPCR37, PGR23 GPR114 ENSG00000159618 PGR27 Symbol Ensembl ID Other names GPR115 ENSG00000153294 FLJ38076, PGR18 GPR116 ENSG00000069122 DKFZp564O1923, KIAA0758 GPR123 ENSG00000197177 KIAA1828 GPR124 ENSG00000020181 Tumour endothelial marker 5 GPR126 ENSG00000112414 FLJ14937 GPR127 ENSG00000186629 PGR16, EMR4 GPR128 ENSG00000144820 FLJ14454 GPR132 ENSG00000183484 G2A GPR133 ENSG00000111452 PGR25 GPR136 ENSG00000124818 OPN5, neuropsin, PGR14 GPR137 ENSG00000173264 GPR137A, TM7SF1L1 GPR139 ENSG00000180269 PGR3 GPR140 ENSG00000172935MRGPRF, GPR168, RTA GPR141 ENSG00000187037 PGR13 GPR142 ENSG00000196169 PGR2, KIF19 GPR143 ENSG00000101850 OA1 GPR144 ENSG00000180264 PGR24 GPR146 ENSG0000016...

SummaryIrreversible platelet inhibitors, such as aspirin and clopidogrel, have limited anti-thrombotic efficacy in the clinic due to their bleeding risk. We have developed an orally active reversible P2Y12 receptor antagonist, BX 667.The aim of this study was to determine if the reversible antagonist BX 667 had a greater therapeutic index than the irreversible P2Y12 receptor antagonist clopidogrel. Since BX 667 is rapidly converted to its active metabolite BX 048 in rats,we first injected BX 048 intravenously (iv) in a rat arterial venous (A-V) shunt model of thrombosis.BX 048 dose- and concentration-dependently attenuated thrombosis. When administered orally, BX 667 and clopidogrel had similar efficacy, but BX 667 caused less bleeding than clopidogrel. In a rat model of a platelet-rich thrombus induced by vessel injury with FeCl2, both BX 667 and clopidogrel exhibited higher levels of thrombus inhibition after oral administration compared to their potency in the A-V shunt model.Again, BX 667 caused less bleeding than clopidogrel. In a dog cyclic flow model, iv injection of either BX 667 or clopidogrel dose-dependently reduced thrombus formation with lower bleeding for BX 667 than clopidogrel. Inhibition of thrombosis was highly correlated with inhibition of ADP-induced platelet aggregation in these animal models. In dogs pre-treated with aspirin, BX 667 maintained its wider therapeutic index, measured by inhibition of platelet aggregation over bleeding, compared to the aspirin-clopidogrel combination.These data demonstrate that the reversible P2Y12 receptor antagonist, BX 667, has a wider therapeutic index than clopidogrel in experimental models of thrombosis.