UDP | Agonist | No | Yes | Communi et al. (1996b) |
UDPβS | Agonist | Yes | No | Jacobson et al. (2002) |
5BrUTP | Weak agonist | No | No | Communi et al. (1996b) |
UTP | Weak agonist | No | Yes | Communi et al. (1996b) |
ADP | Weak agonist | No | Yes | Communi et al. (1996b) |
2-MeSATP | Weak agonist | No | No | Communi et al. (1996b) |
PPADS | Antagonist | No | No | Robaye et al. (1997) |
Reactive blue 2 | Antagonist | No | No | Robaye et al. (1997) |
MRS2567 | Antagonist | Yes | No | Mamedova et al. (2004) |
MRS2578 | Antagonist | Yes | No | Mamedova et al. (2004) |
MRS2575 | Antagonist | Yes | No | Mamedova et al. (2004) |
Agonist potencies | IP3 formation: UDP (EC50 = 300 nM) > 5BrUTP (EC50 = 800 nM) > UTP (EC50 = 6 μM) > ADP (EC50 = 30uM) >> 2-MeSATP (EC50 = 100 μM) (Communi et al., 1996b) |
Antagonist potencies | Reactive blue 2 > PPADS > suramin (Robaye et al., 1997) |
Radioligand assays | None |
Radioligands | None |
Transduction mechanism | Gq/G11; PI hydrolysis (PLCβ activation) and elevated [Ca2+]i in expression systems |
Distribution | Northern blot: placenta, spleen, thymus, intestine (Communi et al., 1996b); vascular smooth muscle, lung (Ralevic and Burnstock, 1998); RT-PCR: human bone, two osteoblastic cell lines, brain-derived cell lines (Burnstock and Knight, 2004); quantitative RT-PCR: spleen, placenta, kidney (high levels), lung, intestine, adipose, bone, heart (moderate expression), and some brain regions (Moore et al., 2001) |
Tissue function | Regulation of chemokine production and release in monocytes (Warny et al., 2001); NaCl secretion in colonic epithelial cells (Burnstock and Knight, 2004); role in proliferation of lung epithelial tumor cells (Schafer et al., 2003); role in mediating contractions of human cerebral arteries (Malmsjö et al., 2003b); interaction with the TNF-α-related signals to prevent apoptotic cell death (Kim et al., 2003b) |
Phenotypes | None |
Comments | Four transcript variants that encode the same isoform have been identified for this gene*; a pseudogene was also described (Burnstock and Knight, 2004); rat and mouse homologs have also been cloned (Chang et al., 1995; Lazarowski et al., 2001b); rat, mouse, and human P2Y6 receptors are UDP-selective, and UTP is less potent, whereas ATP is a very weak partial agonist; the P2Y6 receptor has a pharmacological profile very similar to the UDP receptor on rat C6—2B glioma cells (Lazarowski et al., 1994b); rat P2Y6 potently inhibited N-type Ca channels when expressed in sympathetic neurons, and receptor transcripts were reported to be present in brain tissues (Filippov et al., 1999) |