p2x3

Indophagolin is a potent, indoline-containing autophagy inhibitor with an IC50 of 140 nM, and it antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40, and 3.49 μM, respectively.

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].

P2X3 antagonist (36) is a compound that functions as a P2X3 antagonist.

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.

P2X3-IN-1 (example 7) is a P2X3 receptor inhibitor suitable for neurogenic disease research [1].

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].

P2X3 antagonist 39 (compound 26a) is a selective P2X3 receptor antagonist with an IC50 of 54.9 nM. It is utilized in the study of neuropathic pain models.

(E Z)-Sivopixant ((E Z)-S-600918) is a potent P2X3 receptor antagonist with an IC50 of 4 nM, suitable for respiratory diseases research.

Gefapixant citrate (AF-219 citrate) is an orally available, highly potent P2X3 receptor antagonist with antitussive properties that inhibits hP2X2 3. It can be used to study chronic cough.

Sivopixant (S-600918) (S-600918) is a potent and selective antagonist of P2X3 receptor (P2X3 IC 50 =4.2 nM; P2X2 3 IC 50 =1100 nM). Sivopixant shows strong analgesic effect .

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

A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2 3 receptor antagonist that inhibits receptor-mediated calcium flux.

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.

α,β-Methylene ATP trisodium, a phosphonate analog of ATP, is a selective P2X agonist that induces enhanced contraction of UBSM. α,β-Methylene ATP trisodium inhibits P2X1 and P2X3, but is inactive against P2X2, 4 and 7.

Opiranserin is a development as an injectable agent for the treatment of postoperative pain. Opiranserin is a non-opioid and non-NSAID analgesic candidate and is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A) (IC50s: 0.86 and 1.3 μM, respectively). Opiranserin displays antagonistic activity on rP2X3 (IC50=0.87 μM).

dual P2X3 and P2X2/3 antagonist

P2X3 and P2X2/3 receptor antagonist

MRS2220 is a selective enhancer of the ATP effects at fast desensitizing P2X (P2X1 and P2X3) receptors.

Piromelatine is an agonist of melatonin MT1 MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.

VVZ-149 is an antagonist of both serotonin receptor 2A (5HT2A) and glycine transporter type 2 (GlyT2), with potential anti-nociceptive activity.

Purotoxin 1, isolated from wolf spider venom, is a P2X3 receptor inhibitor that exhibits antinociceptive activity in animal models of inflammatory pain.

α,β-Methylene ATP dilithium, a phosphonic analog of ATP, serves as a ligand for P2X3 and P2X7 receptors. It is a potent agonist specifically targeting P2X1 and P2X3 receptors while exerting negligible activity on P2X2, P2X4, P2X5, P2X6, and P2X7 receptors.

Gardenoside has hepatoprotective, pain‑relieving, and anti-mastitis effects. it may be a potential therapeutic herb against NASH by suppressed supernatant inflammatory cytokine production and intracellular NFkB activity. Gardenoside may be considere

Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2 3 heterotrimeric receptors.