Agonist potencies** |
cAMP: ATPγS (EC50 3.4 ± 0.3 μM) > BzATP (EC50 7.2 ± 0.5 μM) > dATP (EC50 8.9 ± 0.6 μM) > ATP (EC50 17.4 ± 6.1 μM) > ADPβS (EC50 29.7 ± 2.7 μM) > 2-MeSATP (EC50 50 ± 4 μM) (Communi et al., 1999b); IP3: BzATP (EC50 10.5 ± 0.3 μM) > ATPγS (EC50 13.5 ± 2.7 μM) > dATP (EC50 16.3 ± 0.7 μM) > ATP (EC50 65 ± 12 μM) > ADPβS (EC50 174 ± 28 μM) > 2-MeSATP (EC50 210 ± 6 μM) (Communi et al., 1999b) |
Antagonist potencies |
PI hydrolysis: suramin (IC50 1 μM), reactive blue 2 (IC50 9 μM); cAMP: suramin (IC50 16 μM) (Communi et al., 1999b) |
Radioligand assays |
None |
Radioligands |
None |
Transduction mechanism |
Gq/G11 and Gs (see “Comments”); PI hydrolysis (PLCβ activation) and elevated [Ca2+]i in expression systems; adenylate cyclase stimulation and elevated cAMP levels (Qi et al., 2001a) |
Distribution |
Brain, spleen, lymphocytes, intestine; all other tissues expressed more moderate levels of P2Y11 mRNA, with lowest levels detected in liver, cartilage, and bone (Moore et al., 2001) |
Tissue function |
Role in maturation, migration of dendritic cells (Wilkin et al., 2001; Schnurr et al., 2003), and in granulocytic differentiation (Communi et al., 2000); secretory role in pancreatic duct epithelial cells (Nguyen et al., 2001) |
Phenotypes |
None |
Comments |
In P2Y11 gene, an intron was found (Communi et al., 1997)*; P2Y11 couples to Gq and Gs, and the pharmacological profile of the GPCR is slightly different for each transduction pathway (PLCβ/IP3 and adenylate cyclase/cAMP) (Communi et al., 1999b; Qi et al., 2001a); the receptor does not activate PLA2 or PLD (Communi et al., 1999b); the P2Y12 antagonist ARC67085MX is an agonist here; a chimeric mRNA due to intergenic splicing between the P2Y11 and Ssf1 genes has been found in many mammalian cells— the function of this fusion protein is unknown (Communi et al., 2001); a canine (Qi et al., 2001a; Zambon et al., 2001) but no mouse and rat orthologs have been cloned; agonist potencies are species-dependent (Qi et al., 2001a; Zambon et al., 2001)** |