PPTN (free base)

PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity[1].

PPTN is a very potent (IC50 = 1 nM) P2Y14 receptor antagonist th at does not interact with any other P2Y receptor at concentrations up to 10 μM. PPTN blocks UDP-glucose inhibition of forskolin-induced cAMP accumulation, and neutrophil chemotaxis towards UDP-glucose gradients with nM potency.

[1] Barrett MO, et al. A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils. Mol Pharmacol. 2013 Jul;84(1):41-9. DOI:10.1124/mol.113.085654
[2] Lin J, et al. The P2Y14 receptor in the trigeminal ganglion contributes to the maintenance of inflammatory pain. Neurochem Int. 2019 Dec;131:104567. DOI:10.1016/j.neuint.2019.104567