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

P2X Receptor

P2XRs

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-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-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
  • HY-150270
    NP-1815-PX
    Antagonist
    NP-1815-PX is a potent and selective P2X4R antagonist. NP-1815-PX has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX also inhibits guinea pig tracheal/bronchial smooth muscle (TSM and BSM) contractions.
    NP-1815-PX
  • HY-108960
    PPADS
    Antagonist
    PPADS is a P2 receptor antagonist, with IC50s of 68 nM (P2X1) and 214 nM (P2X3). PPADS acts as an ATP (nucleotide) mimetic and competes with ATP for its binding site on P2 receptors. PPADS is also a reversible competitive antagonist of the NAADP receptor. PPADS reverses nociceptive hypersensitivity and reduces the increased NO/NOS system and IL-1β in both peripheral and central steps of nervous system.
    PPADS
  • HY-175196
    P2X7 receptor antagonist-6
    Antagonist
    P2X7 receptor antagonist-6 (Compound 2g) is a negative allosteric P2X7 receptor antagonist with an IC50 of 1.31  μM for hP2X7. P2X7 receptor antagonist-6 can be used for cancer, neurodegenerative, inflammatory, and infectious diseases research.
    P2X7 receptor antagonist-6
  • HY-134440
    α,β-Methylene-ATP dilithium
    Agonist
    α,β-Methylene-ATP dilithium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP dilithium 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 dilithium 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 dilithium 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 dilithium
  • HY-19427
    AZD9056
    Antagonist
    AZD9056 is a P2X7 purinergic receptor antagonist with anticancer activity. AZD9056 can inhibit the invasion and metastasis of cancer stem cells.
    AZD9056
  • HY-134370
    Ap4G
    Ap4G is a dinucleoside polyphosphate compound with vasoconstrictor activity. Ap4G regulates vasoconstriction through P2 receptors, especially P2X receptors, and is an important tool for studying vascular physiology and pathology.
    Ap4G
  • HY-129731
    Lappaconine
    Inhibitor
    Lappaconine is a diterpenoid alkaloid. Lappaconine can be used for α-hydroxylation of β-oxo esters.
    Lappaconine
  • HY-122272S
    Paroxetine-d4
    Inhibitor
    Paroxetine-d4 (BRL29060-d4) is deuterium labeled Paroxetine. 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>4</sub>
  • HY-15488AR
    A 438079 hydrochloride (Standard)
    Antagonist
    A 438079 (hydrochloride) (Standard) is the analytical standard of A 438079 (hydrochloride). This product is intended for research and analytical applications. A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
    A 438079 hydrochloride (Standard)
  • HY-15488R
    A 438079 (Standard)
    Antagonist
    A 438079 (Standard) is the analytical standard of A 438079. This product is intended for research and analytical applications. A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
    A 438079 (Standard)
  • HY-B1901R
    Eperisone hydrochloride (Standard)
    Antagonist
    Eperisone (hydrochloride) (Standard) is the analytical standard of Eperisone (hydrochloride). This product is intended for research and analytical applications. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex.
    Eperisone hydrochloride (Standard)
  • HY-14483R
    AF-353 (Standard)
    Antagonist
    AF-353 (Standard) is the analytical standard of AF-353. This product is intended for research and analytical applications. AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3.
    AF-353 (Standard)
  • HY-N1478R
    Gardenoside (Standard)
    Gardenoside is an orally active natural compound found in Gardenia fruits. Gardenoside reliefs chronic constriction injury (CCI)-induced neuropathic pain by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside reduces reactive oxygen species (ROS). Gardenoside can be used for anti-inflammatory, antinociceptive and hepatoprotective study.
    Gardenoside (Standard)

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