. 2015 Jul;88(1):151–160. doi: 10.1124/mol.115.098756

TABLE 1.

Agonists and antagonists of the P2Y₁₄R

	Molecule	Potency
Natural agonists^a	UDP-glucose	EC₅₀ = 132 nM
	UDP	EC₅₀ = 33 nM
Selective synthetic agonists^b^,^c	2-thio-UDP-glucose (MRS2690)	EC₅₀ = 49 nM
	α,β-methylene-2-thio-UDP (MRS2905)	EC₅₀ = 0.92 nM
Selective competitive antagonist^d	PPTN	K_B = 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 Gα_q/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}

K_B 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).