Potential P2Y14R antagonists are dihydropyridopyrimidine base compound with analogs acting as noncompetitive antagonists of the receptor.318 Another set of P2Y14 R antagonists are naphthoic acid and derivatives that inhibited [3H]UDP binding to the P2Y14R, suggesting orthosteric antagonism for P2Y14 receptors.319 A selective and highly potent competitive antagonist PPTN that was converted to a prodrug has shown to increase bioavailability allowing further studies of this receptor.320 PPTN has shown to inhibit chemotaxis of human neutrophils in cell line expressing P2Y14 receptor.320 An analog of Alexa Fluor 488 (AF488), MRS4174 has also exhibited selectivity and a remarkably high binding activity of 80 pM at the P2Y14R.320 There has been no report of any PET radioligand for mapping of the P2Y14Rs.
