P2Y13 receptor (previously known as GPR86, GPR94, and SP174) 2.1:NUCT:7:P2Y13
| TM | aa | AC | Chr. Map | References | |
|---|---|---|---|---|---|
| Human | 7 | 333 | NM_176894 | 3q24 | Communi et al. (2001a) |
| Rat | 7 | 336 | AY639875 | 2 | Fumagalli et al. (2004) |
| Mouse | 7 | 337 | NM_028808 | 2 | Zhang et al. (2002a) |
| Functional Assays | Inositol phosphate measurement in 1321N1 astrocytoma cells that express recombinant receptor (Communi et al., 2001a); cAMP assays on stably transfected CHO-K1 cells (Communi et al., 2001a); binding of [33P]2-MeSADP in 1321N1 astrocytoma cells that express recombinant receptor (Marteau et al., 2003); assays of GTPγ[35S] binding to membranes of 1321N1 that express recombinant receptor (Marteau et al., 2003; Fumagalli et al., 2004) | ||||
| Ligand | Action | Selectivity | Endogenous | References |
|---|---|---|---|---|
| 2-MeSADP | Agonist | No | No | Zhang et al. (2002a); Marteau et al. (2003) |
| ADPβS | Agonist | No | No | Zhang et al. (2002a); Marteau et al. (2003) |
| 2-MeSATP | Agonist | No | No | Zhang et al. (2002a); Marteau et al. (2003) |
| ADP | Agonist | No | Yes | Zhang et al. (2002a); Marteau et al. (2003) |
| Ap3A | Agonist | No | No | Zhang et al. (2002a); Marteau et al. (2003) |
| ATP | Agonist | No | Yes | Zhang et al. (2002a); Marteau et al. (2003) |
| IDP | Agonist | No | No | Zhang et al. (2002a); Marteau et al. (2003) |
| PPADS | Antagonist | No | No | Marteau et al. (2003) |
| Suramin | Antagonist | No | No | Marteau et al. (2003) |
| AR-C67085MX | Antagonist | No | No | Marteau et al. (2003) |
| AR-C69931MX | Antagonist | No | No | Marteau et al. (2003) |
| Agonist potencies | Fluorimetric imaging assay: 2-MeSADP (EC50 19 ± 5 nM) = ADPβS (EC50 31 ± 15 nM) = 2-MeSATP (EC50 32 ± 8 nM) > ADP (EC50 60 ± 26 nM) > Ap3A (EC50 72 ± 9 nM) > ATP (EC50 261 ± 48 nM) > IDP (EC50 552 ± 64 nM) (Zhang et al., 2002a) | |||
| Antagonist potencies | AR-C69931MX > PPADS > suramin; MRS2179 inactive (Marteau et al., 2003) | |||
| Radioligand assays | Binding of [33P]2-MeSADP (Marteau et al., 2003) | |||
| Radioligands | [33P]2-MeSADP (Marteau et al., 2003) | |||
| Transduction mechanism | Gi and G16 (Communi et al., 2001) | |||
| Distribution | Spleen, brain regions, liver, pancreas, bone marrow, heart, peripheral leukocyte (Communi et al., 2001a; Zhang et al., 2002a) | |||
| Tissue function | No precise evidence but presence in both immune system and brain implies roles | |||
| Phenotypes | None | |||
| Comments | This receptor clusters in the same region of the human chromosome 3q24–3q25, where some of the cloned P2Y receptors (P2Y1, P2Y12, and P2Y14) and several orphan GPCRs are also present (GPR87, GPR91, and H963) (Abbracchio et al., 2003); activated by diphosphate adenine nucleotides and not by uridine nucleotides; cloning and pharmacological characterization of the P2Y13 receptor from rat tissues has been recently described: by using the [35S]GTPγS binding assay in 1321N1 cells that express the rat receptor, ADP was found to be more potent than 2-MeSADP (Fumagalli et al., 2004) | |||
aa, amino acids; AC, accession; chr., chromosome.