p2x2/3

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].

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.

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).

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

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 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].

dual P2X3 and P2X2/3 antagonist

P2X3 and P2X2/3 receptor antagonist

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.

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.

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.

Minodronic acid-d4 is a deuterated compound of Minodronic acid. Minodronic acid has a CAS number of 180064-38-4. 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.

BzATP triethylammonium salt is a P2X7 receptor agonist.

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.

A-317491 is an effective selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which reverses inflammatory mechanical hyperalgesia and relieves chronic inflammation and neuropathic pain in rats by acting on peripheral receptors.