p2x2

Minodronic acid(YM-529) is a P2X2/3 receptor antagonist with anticancer activity, directly or indirectly inhibiting the proliferation of cancer cells and inducing apoptosis. Minodronic acid has been shown to inhibit the metastasis of various types of cancer cells.Minodronic-acid has been used in the study of osteoporosis.

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.

P2X2/3 Modulator-1 (Compound 46) serves as a modulator of P2X2/3 receptors and has applications in researching pain, central nervous system disorders, and inflammation [1].

BzATP triethylammonium salt is a P2X7 receptor agonist.

Adenosine 5'-diphosphate (ADP) is a naturally occurring nucleotide derived from the dephosphorylation of ATP. Adenosine 5'-diphosphate is essential for cellular metabolism and induces platelet aggregation.

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.

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].

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.

NF449 is a potent antagonist of the P2X1 receptor, displaying IC50 values of 0.28 nM, 0.69 nM, and 120 nM for rP2X1, rP2X1+5, and P2X2+3, respectively. It acts selectively against Gsα G proteins (G Protein). NF449 inhibits the binding rate of GTP[γS] to Gsα-s, suppresses the stimulation of adenylate cyclase activity, and blocks the coupling of β-adrenergic receptors with Gs.

2-Methylthio-ATP tetrasodium (2-MeS-ATP tetrasodium) is a non-specific P2 receptor agonist, which can activate P2X2 and P2Y1 receptors and mimic the physiological effects of ATP by binding to P2 receptors, and is widely used in the study of cell signaling and metabolic processes. In addition, 2-Methylthio-ATP tetrasodium induces non-competitive inhibition of ADP-induced platelet aggregation in human.

dual P2X3 and P2X2/3 antagonist

P2X3 and P2X2/3 receptor antagonist

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.

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 .

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.

RO3 is a selective antagonist of homomeric P2X3 and heteromeric P2X2/3 receptor

MRS2179 tetrasodium hydrate, a competitive antagonist of the P2Y1 receptor, acts on the turkey P2Y1 receptor (Kb: 102 nM, pA2: 6.99) and exhibits an inhibitory effect on platelet aggregation. IC50: 1.15 μM), P2X3 (IC50: 12.9 μM), P2X2, P2X4, P2Y2, P2Y4 and P2Y6 receptors.

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.

PSB-10211 is a potent competitive antagonist and positive modulator of the P2X2 receptor.

α,β-Methylene ATP, a phosphonic analog of ATP, functions as a ligand for P2X3 and P2X7 receptors, and acts primarily as a selective agonist for P2X1 and P2X3 receptors, exhibiting minimal to no activity on P2X2, P2X4 through P2X7 receptors.

Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.

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.