Catalog No.
Product Name
Application
Product Information
Citations
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P2X(3)/P2X(2/3) Antagonist
Ro-51 is a selective antagonist of the P2X3 and P2X2/3 receptors, demonstrating IC50 values of 2 nM and 5 nM, respectively. This compound effectively inhibits ATP-mediated signaling through these receptors, making it a valuable tool in pain research. Its specificity and potency allow for detailed investigations into the role of purinergic signaling in nociception and associated pain pathways. -
P2X3 Antagonist
P2X3 antagonist 36 is a potent antagonist of the P2X3 receptor, which plays a critical role in the modulation of pain and sensory signaling. This compound effectively inhibits P2X3 activity, making it a valuable tool for exploring the mechanisms underlying pain pathways. It is particularly useful in research focused on pain management and the development of analgesic therapies. -
ATP Analogue
8-Bromo-ATP, an ATP analogue, serves as a potent agonist for purinergic P2X receptors. This compound demonstrates cytotoxic effects on multiple myeloma cells, with an IC50 value of 23.1 μM, highlighting its potential for cancer research. 8-Bromo-ATP is useful in studies investigating purinergic signaling and its implications in tumor biology. -
P2X Receptor Antagonist
P2X7 receptor antagonist-5 is a potent inhibitor of the P2X7 receptor, a crucial target in various inflammatory and neurological disorders. This compound is characterized by its oral bioavailability and prolonged action, making it suitable for in vivo studies. It holds potential for applications in researching pain, neurodegeneration, and immune responses linked to P2X7 receptor signaling. -
P2X7 Receptor Antagonist
P2X7 receptor antagonist-3 is a highly potent antagonist of the P2X7 receptor, demonstrating IC50 values of 4.2 nM in human cells and 6.8 nM in rat models. This compound inhibits the activation of the P2X7 receptor, which is involved in inflammatory responses and various signaling pathways. It is suitable for research applications focused on pain, neuroinflammation, and autoimmune diseases, enabling the exploration of therapeutic strategies targeting P2X7 receptor-mediated mechanisms. -
P2X7 Receptor Inhibitor
GSK1370319A is a selective inhibitor of the human P2X7 receptor, demonstrating an IC50 of 474 nM and a Ki of 176 nM. This compound effectively inhibits the production of interleukin-1 beta (IL-1β), decreases the generation of reactive oxygen species (ROS), and enhances macrophage survival rates. GSK1370319A is applicable in research related to inflammatory bowel disease and the broader study of inflammatory processes. -
P2X Receptor Inhibitor
P2X receptor-1 is a selective inhibitor of P2X receptors, which play a critical role in mediating pain and inflammatory responses. This compound has potential applications in research focused on understanding nociception and addressing inflammatory conditions. Its ability to modulate P2X receptor activity makes it an important tool for exploring therapeutic strategies in pain management and inflammation research. -
Probe of P2X1 Receptor
MRS 2219 is a selective pharmacological probe for the P2X1 receptor, primarily functioning as an antagonist. It enhances ATP-evoked responses at P2X1 receptors with an EC50 of 5.9 μM, making it essential for studies involving purinergic signaling in cardiovascular and neurological research. This compound is particularly valuable for elucidating the role of P2X1 receptors in various physiological processes and pathological conditions. -
P2X1/3 Receptor Agonist
α,β-Methylene-ATP is a selective agonist of the P2X1 and P2X3 receptors, capable of crossing the blood-brain barrier. Its activation of P2X receptors induces a reflex pressor response associated with the peripheral muscles and the central locus coeruleus, while engaging noradrenergic neurons that mediate antinociceptive effects. α,β-Methylene-ATP is a valuable tool for investigating neuropathic pain mechanisms, cardiovascular reflex regulation, and the central nervous system's antinociceptive pathways. -
P2X2/3 Modulator
P2X2/3 modulator-1 is a selective modulator targeting the P2X2 and P2X3 purinergic receptors. This compound exhibits significant biological activity in the modulation of pain pathways and inflammation processes. It is applicable in research focused on pain management, central nervous system disorders, and inflammatory conditions, providing insights into therapeutic strategies for these ailments. -
P2X4R Antagonist
NP-1815-PX is a selective antagonist of the P2X4 receptor, demonstrating potent inhibition of this target. It exhibits significant anti-inflammatory properties and has been shown to alleviate pain in chronic pain models. Additionally, NP-1815-PX effectively inhibits contractions in guinea pig tracheal and bronchial smooth muscle, making it a valuable tool for research in respiratory and pain-related studies. -
P2X3 Receptor Antagonist
HW091077 is a selective antagonist of the P2X3 receptor, exhibiting an IC50 of 17 nM. By inhibiting ATP-induced calcium influx and preventing cell depolarization, HW091077 effectively disrupts cough reflex pathways. This compound holds potential for research applications focused on chronic cough mechanisms. -
P2X7 Receptor Antagonist
P2X7 receptor antagonist-6 is a negative allosteric modulator targeting the P2X7 receptor, exhibiting an IC50 of 1.31 μM for human P2X7. This compound demonstrates potential for research applications in cancer, neurodegenerative disorders, inflammatory responses, and infectious diseases, contributing to a greater understanding of P2X7's role in these conditions. Its specificity and efficacy make it a valuable tool for exploring therapeutic pathways in related research fields. -
P2X1,3-Selective Agonist
α,β-Methylene-ATP dilithium is a selective agonist for P2X1 and P2X3 receptors, capable of crossing the blood-brain barrier. It induces a reflex pressor response by activating these receptors in peripheral muscles and the central locus coeruleus, with effects that can be inhibited by the P2X antagonist PPADS. Additionally, it stimulates noradrenergic neurons in the central locus coeruleus, contributing to antinociceptive effects that can be reduced by DSP-4. This compound is valuable for investigating the mechanisms underlying neuropathic pain, cardiovascular reflex regulation, and central nervous system analgesia. -
P2X7 Purinergic Receptor Antagonist
AZD9056 is a potent antagonist of the P2X7 purinergic receptor, which plays a significant role in cancer progression. This compound exhibits notable anticancer activity by inhibiting the invasion and metastasis of cancer stem cells. As a result, AZD9056 is valuable for research focused on cancer biology and novel therapeutic strategies targeting purinergic signaling pathways. -
Vasoconstrictor
Ap4G is a dinucleoside polyphosphate that functions as a vasoconstrictor by modulating P2 receptors, particularly P2X receptors. This compound is instrumental for research into vascular physiology and pathology, providing insights into mechanisms of vasoconstriction and related cardiovascular conditions. Its distinct biological activity makes it a valuable reagent for studies investigating the role of purinergic signaling in vascular health. -
P2X7 Antagonist
ITH15004 is a potent antagonist of the P2X7 receptor, effectively penetrating the central nervous system. This compound is utilized in research focused on neurodegenerative diseases, providing insights into the role of ATP-gated ion channels in neuroinflammation and neuronal cell death. Its ability to modulate P2X7 receptor activity makes it a valuable tool in understanding therapeutic strategies for neurological disorders. -
P2X1 Receptor Antagonist
NF449 is a potent antagonist of the P2X1 receptor, demonstrating IC50 values of 0.28 nM for rP2X1, 0.69 nM for rP2X1+5, and 120 nM for P2X2+3. It selectively inhibits Gsα coupling, suppressing GTP[γS] binding to Gsα-s and diminishing adenylyl cyclase activity. This compound is crucial for research applications involving the modulation of purinergic signaling and studies related to cardiovascular and inflammatory conditions. -
P2X Receptor Control
P2X4 antagonist-5 is a selective antagonist for the P2X4 receptor, exhibiting an IC50 greater than 100 μM in human P2X4 assays. This compound serves as a control in studies investigating the modulation of P2X4 receptor activity. It is useful for researchers examining the role of purinergic signaling in various physiological and pathological processes. -
P2X3 Inhibitor
TC-P 262 is a highly effective inhibitor of the P2X3 receptor, a key player in pain and inflammatory responses. By binding to the human P2X3 receptor, TC-P 262 demonstrates significant inhibitory effects, making it a valuable tool for studying conditions such as rheumatoid arthritis, chronic cough, and pain management. This reagent facilitates the exploration of P2X3's role in these biological processes, contributing to the understanding of potential therapeutic interventions. -
AChE/BuChE Inhibitor
Ipidacrine is a potent and selective inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), exhibiting IC50 values of 1 μM and 1.9 μM, respectively. This compound also acts as a partial agonist on M2-cholinergic receptors, promoting neuromuscular transmission and providing a moderate anti-pain effect. Ipidacrine is relevant for research into Alzheimer's disease, ischemic stroke, and diabetic complications, enhancing erectile function and exhibiting effects on ionic channels in neuronal membranes. Its applications extend to studying various deficits in central and peripheral cholinergic disorders. -
AChE/BuChE Inhibitor
Ipidacrine hydrochloride is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), with IC50 values of 1 μM and 1.9 μM, respectively. This compound also acts as a partial agonist at M2-cholinergic receptors and exhibits reversible cholinesterase inhibition. Ipidacrine hydrochloride facilitates neuromuscular transmission and demonstrates moderate analgesic properties. It shows promise in preclinical models for various conditions, including Alzheimer’s disease, ischemic stroke, facial nerve neuropathy, and diabetes-associated erectile dysfunction, highlighting its potential in investigating cholinergic system-related disorders. -
Sodium Channel Inhibitor
Dibucaine hydrochloride is a sodium channel inhibitor that effectively blocks the influx of sodium ions, thereby preventing the propagation of action potentials in excitable tissues. This compound exhibits potent activity as an anesthetic and is utilized in various research applications, including studies of nerve conduction and muscle excitability. Additionally, it serves as a significant inhibitor of serum cholinesterase, contributing to its utility in pharmacological investigations and the development of anesthetic protocols. -
NMDA Receptor Modulator
Neboglamine hydrochloride is a positive modulator of the glycine site on the NMDA receptor, facilitating increased receptor activity. This compound has demonstrated potential in addressing aspects of schizophrenia and related neurological disorders. Researchers can utilize Neboglamine hydrochloride to explore its effects on synaptic transmission and neuroplasticity, contributing to a deeper understanding of NMDA receptor dynamics in psychiatric conditions. -
NMDA Receptor Antagonist
Gavestinel sodium salt is a selective, non-competitive antagonist of the NMDA receptor, targeting the glycine site with a pKi of 8.5. This compound exhibits potent activity in modulating NMDA receptor function, making it valuable for research applications related to neuroprotection and acute ischemic stroke. Its oral bioavailability enhances its potential as a tool for studying NMDA receptor-mediated pathways in various neurological conditions. -
NMDA Receptor Antagonist
Gavestinel (GV 150526) is a selective and potent antagonist of the glycine site on the NMDA receptor. It exhibits neuroprotective effects, making it a valuable tool for research into neurodegenerative diseases and neurological disorders. Its ability to modulate excitotoxicity highlights its potential in studying synaptic transmission and neuronal survival. -
NMDA Receptor Antagonist
DL-AP5 sodium is a competitive antagonist of the NMDA (N-methyl-D-aspartate) receptor. It exhibits notable antinociceptive activity, making it valuable for pain research. Additionally, DL-AP5 sodium effectively blocks ion channels in the rabbit retina, providing insights into retinal pharmacology and neurological studies. -
NMDA Receptor Antagonist
Remacemide is a non-competitive antagonist of the NMDA receptor, demonstrating low-affinity binding. It exhibits neuroprotective properties in preclinical models of hypoxia and ischemic stroke, making it a valuable tool in neurological research. Furthermore, Remacemide possesses anticonvulsant activity and is relevant in the study of neurodegenerative disorders such as Parkinson's disease and Huntington's disease. -
NMDA Receptor NR2B Antagonist
EMD-95885 is a selective antagonist of the NR2B subunit of NMDA receptors, exhibiting an IC50 of 3.9 nM. This specificity enables EMD-95885 to effectively block NR2B-containing NMDA receptor activity without engaging other binding sites on the receptor. It is valuable for research focusing on neurobiology, synaptic plasticity, and the mechanisms underlying neurological disorders. -
NMDA Antagonist
(RS)-CPP ((±)-CPP) is a potent and selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. By inhibiting NMDA receptor-mediated central neuron responses, (RS)-CPP demonstrates anticonvulsant properties. This compound is primarily utilized in neurological research to explore mechanisms of neuroprotection, excitotoxicity, and seizure disorders. -
NMDA Receptor Inhibitor
(R)-CPP is a potent antagonist of the NMDA receptor, effectively inhibiting its activity. It is utilized in various research applications related to neuropharmacology and the study of excitatory neurotransmission. This compound is important for exploring the role of NMDA receptors in neurological disorders and for evaluating potential therapeutic interventions. -
NMDAR Modulator
NYX-2925 is an orally active NMDAR modulator that specifically restores activated Src and its phosphorylation sites on GluN2A and GluN2B in the medial prefrontal cortex. This compound does not affect CAMKII and is devoid of addictive, sedative, or ataxic side effects. NYX-2925 is a valuable tool for investigating NMDA receptor-related central nervous system disorders. -
NMDAR Antagonist
Blixeprodil is a selective antagonist of the N-methyl-D-aspartate receptor (NMDAR) with a binding affinity (Ki) of 3.25 µM in rat cortical tissue. It effectively inhibits NR1/2A-NMDAR-mediated currents in HEK293 cells, exhibiting an IC50 value of 1.192 µM. Preclinical studies demonstrate its antidepressant properties in animal models, and Blixeprodil's ability to cross the blood-brain barrier makes it a valuable tool for investigating neuropharmacological mechanisms and potential therapeutic applications in mood disorders. -
NMDAR Antagonist
(Rac)-Lanicemine is a potent NMDA receptor antagonist that functions as a low-trapping blocker of NMDA channels, exhibiting a Ki value between 0.56-2.1 μM. This compound demonstrates antidepressant properties, supported by IC50 values of 4-7 μM in CHO cells and 6.4 μM in Xenopus oocyte cells. Its unique pharmacological profile makes (Rac)-Lanicemine valuable for research investigating the mechanisms of depression and the role of NMDA receptors in neuropsychiatric disorders. -
NMDA receptor antagonist
Aptiganel hydrochloride is a non-competitive antagonist of the NMDA receptor, exhibiting significant neuroprotective properties. Its ability to modulate glutamate signaling positions it as a valuable tool in research focused on neurodegenerative diseases and conditions associated with excitotoxicity. Aptiganel hydrochloride is particularly relevant for exploring therapeutic approaches for stroke, traumatic brain injury, and various neurodegenerative disorders. -
NMDA Receptor Antagonist
L-701252 is a potent antagonist of the glycine site on the NMDA receptor, exhibiting an IC50 of 420 nM. This compound has demonstrated neuroprotective effects in models of global cerebral ischemia, making it a valuable tool for research into neurodegenerative diseases and excitotoxicity. Its efficacy in modulating NMDA receptor activity positions L-701252 as a promising candidate for studies focused on synaptic transmission and neurological disorders. -
NMDA Receptor Agonist
N-Methyl-DL-aspartic acid is a glutamate analogue that functions as an NMDA receptor agonist. This compound is primarily utilized in research pertaining to neurological disorders, aiding in the study of synaptic transmission and excitotoxicity associated with various neurodegenerative conditions. Its ability to activate NMDA receptors makes it a valuable tool for investigating the physiological and pathological roles of glutamatergic signaling in the central nervous system. -
NMDA Antagonist
Nelonemdaz potassium is an NR2B-selective, uncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors. This compound exhibits significant neuroprotective properties by mitigating cell death induced by NMDA and free radicals. It serves as a valuable tool in research focused on neuroprotection, neurodegenerative diseases, and the mechanisms underlying excitotoxicity. Its dual action as a NMDA antagonist and free radical scavenger supports its potential applications in therapeutic development for conditions linked to oxidative stress and neuronal injury. -
NMDA antagonist
PPDA is a subtype-selective antagonist of the NMDA receptor, specifically targeting the NR2C and NR2D subunits. This compound is known to inhibit NMDA receptor-mediated signaling, making it valuable for research on synaptic plasticity, neuroprotection, and neurological disorders. Its selective binding profile allows for more tailored studies on the role of specific NMDA receptor subtypes in various biological processes. -
Anti-NMDAR Antibody
ART5803 is a humanized IgG1 monoclonal antibody that targets the N-terminal domain of the NMDAR GluN1 subunit. This compound effectively inhibits NMDAR internalization induced by pathogenic autoantibodies and restores both cell-surface expression and functional activity of NMDAR. ART5803 has demonstrated efficacy in reversing behavioral abnormalities and restoring NMDAR expression in marmoset models of disease, making it a valuable tool for research on anti-NMDAR encephalitis. -
NMDA Antagonist
Fluoroethylnormemantine hydrochloride is an NMDA receptor antagonist, derived from Memantine. This compound demonstrates significant anti-amnesic, neuroprotective, and antidepressant-like properties, along with the ability to attenuate fear responses. It is suitable for research applications involving neuropharmacology and may serve as a valuable positron emission tomography (PET) tracer in studying NMDA receptor dynamics and related pathways in the central nervous system. -
NMDA Receptor Antagonist
CGP 37849 is a potent competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor. This compound exhibits anticonvulsant properties in rodent models, as well as demonstrating antidepressant and anxiolytic-like effects. It serves as a valuable tool in research focused on neurological disorders and the modulation of synaptic transmission. -
Glycine/NMDA Partial Agonist/Antagonist
(R)-(+)-HA-966 functions as a partial agonist/antagonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. This compound selectively inhibits the activation of the mesolimbic dopamine system induced by amphetamine, making it relevant for studying addiction and dopamine-related disorders. Its ability to traverse the blood-brain barrier suggests potential applications in addressing conditions such as neuropathic and acute pain. -
NMDA Receptor Antagonist
SDZ 220-040 is a competitive antagonist of the NMDA receptor, exhibiting a pKi of 8.5. This compound is primarily employed in research investigating neurological diseases, offering insights into the mechanisms underlying neurodegeneration and synaptic dysfunction. Its specific targeting of NMDA receptors makes it a valuable reagent for pharmacological studies and the development of novel therapeutic strategies. -
NMDA Receptor Antagonist
Arcaine sulfate is a potent NMDA receptor antagonist that selectively inhibits glutamate signaling at this critical synaptic target. Its ability to modulate excitatory neurotransmission makes Arcaine sulfate a valuable tool for studying neurophysiological processes and evaluating the role of NMDA receptors in various neurological disorders. This compound is widely utilized in research exploring synaptic plasticity, neuroprotection, and the mechanisms underlying excitotoxicity. -
NMDA Agonist
(RS)-(Tetrazol-5-yl)glycine is a potent and selective agonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits effective stimulation with EC50 values of 99 nM and 1.7 μM for the GluN1/GluN2D and GluN1/GluN2A subtypes, respectively. This compound is utilized in research involving seizure activity and neuronal activation, as evidenced by its ability to induce Fos expression in mice models. -
NMDARs Negative Allosteric Modulator
UBP608 is a potent negative allosteric modulator of N-Methyl-D-aspartate receptors (NMDARs). This compound has demonstrated significant biological activity in modulating NMDAR function, making it a valuable tool for investigating neurological disorders. Its mechanism of action offers insights into synaptic transmission and neuroplasticity, facilitating research into therapeutic strategies for various cognitive and behavioral conditions. -
NMDA Receptor Modulator
Neboglamine is an N-methyl-D-aspartate (NMDA) receptor modulator that enhances neuronal activity in key brain regions including the prefrontal cortex, nucleus accumbens, and lateral septal nucleus. This compound has been shown to increase the levels of fos-like immunoreactivity (FLI)-positive cells and effectively restores NMDA-mediated neurotransmitter release. Additionally, Neboglamine demonstrates the ability to inhibit hyperlocomotion induced by phencyclidine, highlighting its potential for research in neuropharmacology and neuropsychiatric disorders. -
GluN1/GluN2A NMDAR Antagonist
TCN 213 is a selective, surmountable antagonist of the GluN1/GluN2A subunits of the N-methyl-D-aspartate receptor (NMDAR), exhibiting IC50 values of 0.55, 3.5, and 40 μM in the presence of 75, 750, and 7500 nM glycine, respectively. This compound serves a critical role in studying the pharmacological modulation of NMDAR expression in developing cortical neurons, making it a valuable tool for research in neurodevelopment and synaptic plasticity. -
NMDA Antagonist
L-689560 is a potent antagonist of the N-methyl-D-aspartate (NMDA) receptor, specifically targeting the GluN1 glycine binding site. This compound is utilized extensively in radiolabeled ligand binding studies and is essential for investigating the roles of NMDA receptors in both normal neurological functions and various neurological disorders. L-689560 aids in advancing our understanding of synaptic transmission and neurotoxicity linked to excitatory neurotransmission.
