P2X purinergic receptor

Selective, high affinity P2X3 and P2X2/3 receptor antagonist; antinociceptive

Oxatomide is an orally active H1-receptor antagonist (antihistamine).

Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.

JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM).

(E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist with an IC50 of 4 nM.

Eliapixant (BAY 1817080) is a potent and selective antagonist of P2X3 receptor, with an IC50 of 8 nM.

Filapixant is a purinoreceptor antagonist extracted from patent WO2016091776A1, example 348.

GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor.

Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively).

JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.

Camlipixant (BLU-5937) is an effective, selective, non-competitive and orally active P2X3 homotrimer receptor antagonist with an IC50 of 25 nM for hP2X3 homotrimer. Camlipixant exhibits strong antitussive effects without taste alteration. Camlipixant can be used in the research of unexplained and refractory chronic cough.

P2X7-IN-2 TFA (compound 58) is an inhibitor of the P2X7 receptor. It inhibits the release of IL-Iβ with an IC50 value of 0.01 nM. P2X7-IN-2 TFA can be used for research on autoimmune diseases, inflammation, and cardiovascular diseases.

P2X7 receptor antagonist-2 is a potent P2X7 receptor antagonist with a pIC50 value of 6.5-7.5.

NP-1815-PX sodium is a potent and selective P2X4R antagonist.

HEI3090 is a P2X7R activator.

PSB-12054 is a P2X4 receptor antagonist with IC 50 values of 0.19 μM, 2.10 μM and 1.77 μM against human, rat and mouse receptors, respectively, and exhibits selectivity over other human P2X receptor subtypes.

PSFL2915 is a selective, orally active P2X receptor inhibitor with oral effectiveness, with an IC 50 of 0.319 μM for human P2X3, 0.261 μM for rat P2X2/3, and 13.3 μM for human P2X2.

PSB-10211 is a P2X2 receptor antagonist with an IC 50 of 0.086 μM against rat P2X2 receptors.