TABLE 1

Agonists and antagonists of the P2Y14R

MoleculePotency
Natural agonistsaUDP-glucoseEC50 = 132 nM
UDPEC50 = 33 nM
Selective synthetic agonistsb,c2-thio-UDP-glucose (MRS2690)EC50 = 49 nM
α,β-methylene-2-thio-UDP (MRS2905)EC50 = 0.92 nM
Selective competitive antagonistdPPTNKB = 400 pM
  • a EC50 values are from experiments measuring inhibition of cAMP accumulation in P2Y14R-expressing CHO cells (Carter et al., 2009).

  • b Values are from experiments measuring inositol phosphate accumulation in Cos-7 cells expressing the human P2Y14R and Gαq/i (Ko et al., 2007).

  • c Values are from experiments measuring inhibition of cAMP accumulation in P2Y14R-expressing HEK293 cells (Das et al., 2010).

  • d KB for PPTN was obtained in Schild analyses measuring antagonism of UDP-glucose–promoted inhibition of cyclic AMP accumulation in P2Y14R-expressing CHO cells (Barrett et al., 2013).