2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
  4. P2X Receptor

P2X Receptor

P2XRs

P2X Receptor

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P2X receptors are a family of seven (P2X1R-P2X7R) cation permeable ligand-gated ion channels (LGICs) that open in response to binding by the extracellular ligand, adenosine 5′-triphosphate (ATP). P2X receptors have a high permeability to Ca2+, Na+, and K+ and are expressed widely throughout the nervous, immune, cardiovascular, skeletal, gastrointestinal, respiratory, and endocrine systems.

P2X receptors are widely expressed in excitatory and non-excitatory cells, such as neuron, glia, platelet, epithelia and macrophage, and participate in many important physiological and pathological processes, including synaptic transmission, pain perception, inflammation, cardiovascular modulation, immunomodulation and tumorigenesis.

P2X Receptor Isoform Specific Products:

P2X Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-111124
    Paroxetine-d2
    Paroxetine-d2 (CTP 347) is a deuterium labeled Paroxetine (HY-122272). Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches.
    Paroxetine-d<sub>2</sub>
  • HY-159832
    Relicpixant
    		Antagonist
    Relicpixant is a potent purinoreceptor (P2X) antagonist.
    Relicpixant
  • HY-176195
    P2X4-IN-1
    		Inhibitor
    P2X4-IN-1 (Compound 1) is an orally active P2X4 inhibitor. P2X4-IN-1 can be used in the study of prophylaxis disease.
    P2X4-IN-1
  • HY-143576
    P2X3 antagonist 37
    		Antagonist
    P2X3 antagonist 37 is a potent P2X3 receptor antagonist with an IC50 of 32.45 nM for hP2X3 (WO2021115225A1, example 68).
    P2X3 antagonist 37
  • HY-14485
    Ro-51
    		Antagonist
    Ro-51 is a potent and selective dual P2X3/P2X2/3 antagonist, with IC50 of 2 nM and 5 nM for P2X3 and P2X2/3, respectively. Ro-51 can be used for the research for pain.
    Ro-51
  • HY-143568
    P2X3 antagonist 36
    		Antagonist
    P2X3 antagonist 36 is a P2X3 antagonist extracted from patent WO2019081343A1 compound 156.
    P2X3 antagonist 36
  • HY-134262
    8-Bromo-ATP
    		Agonist
    8-Bromo-ATP (8-Bromoadenosine 5'-triphosphate), an ATP analogue, is a purinergic P2X receptor agonist. 8-Bromo-ATP shows cytotoxic to multiple myeloma cells with an IC50 of 23.1 μM.
    8-Bromo-ATP
  • HY-162951
    P2X7 receptor antagonist-5
    		Antagonist
    P2X7 receptor antagonist-5 (compund 13a) is a potent, orally active and long-lasting P2X7 receptor antagonist.
    P2X7 receptor antagonist-5
  • HY-182715
    PSB-10211
    		Antagonist
    PSB-10211 is a P2X2 receptor antagonist with an IC50 of 0.086 μM against rat P2X2 receptors. PSB-10211 inhibits ATP-mediated currents of rat P2X2 receptors expressed in Xenopus oocytes. PSB-10211 can be used in studies related to pain and urinary incontinence.
    PSB-10211
  • HY-137609A
    TNP-GTP tetrasodium
    		Antagonist
    TNP-GTP tetrasodium is a fluorescently labeled GTP (HY-113225) derivative. TNP-GTP tetrasodium can inhibit glutamate dehydrogenase (Ki = 2.7 μM). TNP-GTP tetrasodium is an antagonist of the purinergic P2X2 and P2X2/3 receptors with IC50 values of 0.4 and 1.2 nM, respectively. TNP-GTP tetrasodium also inhibit rat soluble guanylyl cyclase (Ki = 11 nM).
    TNP-GTP tetrasodium
  • HY-148558
    P2X7 receptor antagonist-3
    		Antagonist
    P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC50 values of 4.2 nM in humans and 6.8 nM in rats.
    P2X7 receptor antagonist-3
  • HY-109067
    Opiranserin
    		Antagonist
    Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
    Opiranserin
  • HY-165557
    GSK1370319A
    		Inhibitor
    GSK1370319A is a human P2X7 receptor inhibitor with an IC50 of 474 nM and a Ki of 176 nM. GSK1370319A inhibits the production of IL-1β, reduces the generation of reactive oxygen species (ROS), and increases the survival rate of macrophages. GSK1370319A can be used for the research of inflammatory bowel disease.
    GSK1370319A
  • HY-122163
    MK-3901
    		Antagonist
    MK-3901 is a selective P2X3 receptor antagonist with an IC50 of 24 nM. MK-3901 inhibits UGT1A1 (with an IC50 of 1 μM) and CYP2C9 (with an IC50 of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain.
    MK-3901
  • HY-128891
    Eperisone
    		Antagonist
    Eperisone ((±)-Eperisone) is an antispasmodic agent and centrally acting muscle relaxant useful in the study of diseases characterized by muscle stiffness and pain. Eperisone acts by relaxing skeletal and vascular smooth muscle, resulting in vasodilation, decreased muscle tone, improved circulation, and inhibition of pain reflexes. Eperisone is also a potent P2X7 receptor antagonist.
    Eperisone
  • HY-139627
    P2X receptor-1
    		Inhibitor
    P2X receptor-1 is a potential inhibitor of P2X receptor for the research of pain and inflammation.
    P2X receptor-1
  • HY-102063
    MRS 2219
    		Agonist
    MRS 2219 (Pyridoxol) is a selective pharmacological probe of P2X1 receptor. MRS 2219 selectively potentiated ATP-evoked responses at P2X1 receptors with an EC50 of 5.9 μM.
    MRS 2219
  • HY-134440A
    α,β-Methylene-ATP
    		Agonist
    α,β-Methylene-ATP is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system.
    α,β-Methylene-ATP
  • HY-P992286
    Anti-P2XR4 Antibody
    Anti-P2XR4 Antibody is a monoclonal antibody targeting P2XR4. It can be used in ELISA, FACS, and functional assays. For isotype controls of Anti-P2XR4 Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-P2XR4 Antibody
  • HY-153548
    P2X2/3 modulator-1
    		Modulator
    P2X2/3 modulator-1 (Compound 46) is a P2X2/3 modulator. P2X2/3 modulator-1 can be used in the study of pain, central nervous system disorders and inflammation.
    P2X2/3 modulator-1
P2X Receptor Isoform Comparison

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