human p2x3

AF-353 (Ro-4), an effective and orally bioavailable antagonist of the P2X3 P2X2 3 receptor, inhibits human and rat P2X3 (pIC50= 8.0).

BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.

P2X3 antagonist 34, a potent, selective, and orally active antagonist, targets the P2X3 homotrimeric receptor, exhibiting IC50s of 25 nM, 92 nM, and 126 nM for human, rat, and guinea pig P2X3 receptors respectively. It shows reduced activity against P2X2 3 heterotrimeric receptors across human, rat, and guinea pig models. Notably, this compound demonstrates a significant anti-tussive effect without altering taste[1].

Camlipixant (BLU-5937) is an orally active purine P2X3 receptor antagonist that is potent, selective and competitive. camlipixant has an IC50 of 25 nM for the hP2X3 homotrimer. camlipixant can be used for the treatment of respiratory disorders and Camlipixant has a strong cough suppressant effect.

Compound 38, also known as Compound 4, is a potent, orally active P2X3 antagonist that demonstrates inhibitory activity with IC50 values of 0.132 µM, 0.165 µM, and 0.421 µM against human (hP2X3), rat (rP2X3), and guinea pig (gpP2X3) P2X3 receptors, respectively [1].

This novel compound is an orally bioavailable antagonist of P2X3 P2X2 3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2 3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2 3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1 2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

This novel compound is an orally bioavailable antagonist of P2X3/P2X2/3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2/3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2/3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1/2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

NF023 hexasodium is a selective and competitive P2X1 receptor antagonist with IC50 values of 0.21 μM, 28.9 μM, > 50 μM, and > 100 μM for human [P2X1], [P2X3], [P2X2], and [P2X4]-mediated responses, respectively.

A-317491 (ABT 202) is a non-nucleotide P2X3 ( Ki: 22 nM) and P2X2 3 receptor (Ki: 9 nM) antagonist, which inhibits calcium flux mediated by the receptors.