Catalog No.
Product Name
Application
Product Information
Citations
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NMDA Receptor Blocker
Caged MK801 is a selective, non-competitive, irreversible blocker of the NMDA receptor, targeting the open-channel state. It is designed to release MK801 upon photolysis, providing a tool for precise temporal control in neuronal studies. This compound is compatible with neuropharmacological applications, enabling exploration of synaptic plasticity and neurodegeneration mechanisms. -
NMDAR Modulator
NMDAR Modulator 2 is an NMDA receptor modulator that alters NMDA receptor activity. This compound serves as a valuable tool for investigating psychiatric disorders associated with dysregulated glutamatergic transmission, such as treatment-resistant depression. Its targeted action on NMDA receptors makes it suitable for exploring therapeutic strategies in conditions where glutamate signaling is implicated. -
NMDA Receptor Antagonist
DL-AP5 lithium is a competitive antagonist of the NMDA (N-methyl-D-aspartate) receptor. It demonstrates notable antinociceptive properties, making it a valuable tool in pain research. This compound has been shown to specifically inhibit ion channels in the rabbit retina, providing insights into its potential applications in neuropharmacology and retinal studies. -
NMDA Inhibitor
UBP618 is a non-selective N-methyl-D-aspartate (NMDA) receptor inhibitor. This compound exhibits significant modulation of NMDA receptor activity, making it valuable for studying excitatory neurotransmission and various neurological disorders. UBP618 is utilized in research addressing conditions such as Alzheimer's disease, schizophrenia, and other neurodegenerative disorders, providing insights into synaptic plasticity and neuroprotection mechanisms. -
NMDAR Antagonist
Delucemine hydrochloride is a selective N-methyl-D-aspartate receptor (NMDAR) antagonist, known for its role in modulating glutamatergic signaling. This compound exhibits potential antidepressant properties, making it a valuable tool for researching treatments for mood disorders. Additionally, Delucemine hydrochloride may be utilized to explore the underlying mechanisms of NMDAR-related neuropsychiatric conditions. -
NMDA Receptor Modulator
NMDA Receptor Modulator 8 is an NMDA receptor modulator that exhibits 50%-100% potentiation of the NMDA receptor activity at a concentration of 10 μM. This compound can play a significant role in studies related to synaptic plasticity, neuroprotection, and various neurodegenerative diseases. Its modulation of NMDA receptor function makes it a valuable tool for researchers investigating excitatory neurotransmission and associated pathways. -
NMDAR Antagonist
NMDAR antagonist 4 is a specific antagonist of the NMDA receptor, targeting the glycine site with a binding affinity characterized by a Ki value exceeding 100 μM. This compound has been utilized in biological research to investigate the role of NMDA receptors in various neurological pathways and disorders. Its utility spans studies on excitotoxicity, synaptic plasticity, and potential therapeutic applications in neurodegenerative diseases. -
NMDA Receptor Antagonist
LY 235959 is a competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor. This compound enhances the anticonvulsant effects of various antiepileptic agents, making it valuable in the research of epilepsy and related neurological disorders. Its ability to modulate NMDA receptor activity positions LY 235959 as a critical tool for studying synaptic transmission and excitotoxicity. -
NMDA Antagonist
Etoxadrol is a potent NMDA antagonist, exhibiting high affinity for the N-methyl-D-aspartic acid receptor. It is primarily utilized in anesthetic research to modulate pain mechanisms and examine neuroprotective effects. This compound is of particular interest in studies related to pain management and the exploration of anesthetic protocols. -
P2X Receptor Antagonist
PPADS tetrasodium is a non-selective antagonist of P2X receptors, effectively inhibiting recombinant P2X1, -2, -3, and -5 with IC50 values ranging from 1 to 2.6 μM. Additionally, it shows inhibitory effects on native P2Y2-like receptors (IC50 ~0.9 mM) and recombinant P2Y4 receptors (IC50 ~15 mM). This compound also acts as an inhibitor of the reverse mode of the Na/Ca2+ exchanger in guinea pig airway smooth muscle, making it a valuable tool for research on purinergic signaling and related physiological processes. -
α-isomer of Nicotine
α-Nicotine is the α-isomer of nicotine and functions as an agonist of nicotinic acetylcholine receptors (nAChRs). This compound exhibits notable biological activity that may be beneficial for understanding neuropsychiatric disorders, including schizophrenia and attention deficit hyperactivity disorder (ADHD). Its potential applications in research make it a valuable tool for exploring the pharmacological effects of nAChR activation. -
Endogenous Metabolite
Cotinine, a primary metabolite of nicotine, acts as an endogenous biomarker for tobacco exposure. This alkaloid exhibits vasodepressor activity and has demonstrated antiproliferative effects when combined with nicotine against conditions such as pterygium. Additionally, (S)-(-)-Cotinine activates nicotinic acetylcholine receptors (nAChR) in a calcium-dependent manner, facilitating dopamine release. Due to its diverse biological activities, cotinine is employed in research focused on cardiovascular and inflammatory diseases. -
nAChRs Antagonist
Dihydro-β-erythroidine hydrobromide is a competitive antagonist specifically targeting neuronal nicotinic acetylcholine receptors (nAChRs). It demonstrates notable selectivity for the α4β4 and α4β2 nAChR subtypes, with IC50 values of 0.19 μM and 0.37 μM, respectively. This compound is utilized in research exploring its potential antidepressant-like effects and its role in understanding nAChR-mediated signaling pathways. -
Acetylcholine Agonist
Spinosad is an acetylcholine agonist that acts primarily on the nicotinic acetylcholine receptors (nAChRs) in the insect nervous system. Derived from the fermentation products of the soil actinomycete Saccharopolyspora spinosa, Spinosad exhibits potent biological neurotoxic activity, making it effective as a broad-spectrum insecticide. Its favorable environmental and mammalian safety profile, along with its larvicidal properties, supports its use in various pest control applications. -
Insecticide
Acetamiprid is a neonicotinoid insecticide that acts as a selective agonist of nicotinic acetylcholine receptors (nAChRs). It disrupts normal synaptic transmission, leading to paralysis and death in target pests. Research applications include studies on neuromuscular function, insect behavior, and potential reproductive impacts in non-target organisms. -
α7 nAChR Agonist
PHA-543613 is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting a Ki value of 8.8 nM. This compound demonstrates significant selectivity for the α7 nAChR compared to other nicotinic and serotonergic receptors, including α3β4, α1β1γδ, α4β2, and 5-HT3. PHA-543613 is applicable in research focused on cognitive deficits associated with Alzheimer's disease and schizophrenia, making it a valuable tool for neuropharmacological studies. -
Insecticide
Flupyradifurone is a systemic agonist of nicotinic acetylcholine receptors (nAChRs) that disrupts signal transduction in the central nervous system of sap-sucking insects. It functions as a butenolide insecticide, effectively targeting pest populations while offering low toxicity to non-target organisms. Research applications include studying insect neurobiology and developing pest management strategies. -
nAChR Agonist
Tebanicline dihydrochloride is a selective agonist of nicotinic acetylcholine receptors (nAChRs), particularly targeting the α4β2 subtype. It exhibits strong analgesic properties and demonstrates oral bioavailability. This compound is valuable for research into pain management and the modulation of cholinergic signaling in neurological studies. -
nAChR Antagonist
Coclaurine is a tetrahydroisoquinoline alkaloid and a potent antagonist of nicotinic acetylcholine receptors (nAChRs). It exhibits significant anticancer activity by downregulating EFHD2-related NOX4-ABCC1 signaling, thereby enhancing the sensitivity of cancer cells to Cisplatin. Coclaurine also suppresses the stemness and metastatic potentials of non-small cell lung cancer (NSCLC) cells through the disruption of the FOXG1-EFHD2 promoter interaction, leading to reduced EFHD2 transcription. This compound serves as a valuable tool for research focused on cancer therapy and the modulation of nAChR signaling. -
AChE Reversible Inhibitor
Asoxime dichloride is a reversible inhibitor of acetylcholinesterase (AChE) that functions as a thiosemicarbazone-based antidote. Its primary mechanism involves reactivating AChE that has been inhibited by nerve agents, thus restoring cholinergic nerve function. Additionally, Asoxime dichloride enhances muscle function in the presence of poisoning without reactivating AChE and acts as an antagonist to acetylcholine receptors, including nicotinic and α7 nAChRs. Due to its immunomodulatory properties, Asoxime dichloride can also enhance the immune response of the nervous system, making it valuable in neuropharmacological research. -
nAChR Inhibitor
Lupanine is a natural ketonic derivative of Sparteine that acts as an inhibitor of nicotinic acetylcholine receptors (nAChR). It exhibits binding affinity to these receptors with a Ki value of 500 nM, demonstrating its potential as a ganglioplegic agent. Lupanine is utilized in research applications related to neuromodulation and the study of cholinergic signaling pathways. -
nAChR Activator
Myosmine is a specific alkaloid derived from tobacco that acts as an activator of nicotinic acetylcholine receptors (nAChR). It exhibits a relatively low affinity for the α4β2 nAChR subtype, with a Ki value of 3300 nM. Myosmine is utilized in research to explore the pharmacological effects of nAChR modulation and its implications in neurobiology and addiction studies. -
nAChR Antagonist
AT 1001 is a selective antagonist of the α3β4 nicotinic acetylcholine receptor (nAChR), with a high affinity characterized by a Ki value of 2.64 nM. This compound effectively reverses inward currents triggered by Epibatidine in HEK cells expressing α3β4 nAChR. AT 1001 demonstrates dose-dependent inhibition of nicotine self-administration in rat models, while sparing food-reinforced responding, making it a valuable tool in nicotine addiction and smoking cessation therapy research. -
nAChR Agonist
Pozanicline dihydrochloride is a selective agonist for nicotinic acetylcholine receptors (nAChRs), specifically targeting the α4β2 subtype with a binding affinity (Ki) of 17 nM at rat brain nAChR sites. It exhibits an affinity of 16.7 nM for [3H]cytisine binding sites, demonstrating its potential in modulating cholinergic signaling. This compound is instrumental in research focused on neurological disorders, cognition enhancement, and the exploration of nAChR-related pathways. Its oral bioavailability further supports its utility in in vivo studies. -
nAChR Antagonist
Chlorisondamine diiodide is a potent antagonist of the nicotinic acetylcholine receptor (nAChR), functioning as a ganglion blocker. It effectively inhibits specific central actions of nicotine with notable potency and pharmacological selectivity. This compound is valuable in research applications exploring neural signaling, autonomic regulation, and addiction pathways. -
α7-nAChR Antagonist
(2S,6S)-Hydroxynorketamine hydrochloride is an antagonist of the α7-nicotinic acetylcholine receptor (nAChR). It exhibits potential neurorelaxant, antidepressant, and analgesic effects, facilitating the activation of the mTOR pathway and promoting increased phosphorylation of downstream targets. This compound is of particular interest in neurological research, particularly in the exploration of therapeutic avenues for mood disorders and pain management. -
α-7 nAchR Agonist
PHA 568487 free base is a selective agonist of the α-7 nicotinic acetylcholine receptor (nAchR). This compound has been shown to reduce neuroinflammation, making it a valuable tool for research in neurodegenerative diseases and disorders associated with inflammation. Its ability to modulate α-7 nAchR activity provides insights into cholinergic signaling and potential therapeutic strategies targeting these pathways. -
α3β4 nAChR Agonist
NS3861 is a selective agonist of the heteromeric α3β4 nicotinic acetylcholine receptor (nAChR), exhibiting high-affinity binding with a Ki value of 0.62 nM. This compound also demonstrates varied affinities for other nAChR subtypes, with Ki values of 25 nM for α3β2, 7.8 nM for α4β4, and 55 nM for α4β2. NS3861 is valuable for research focused on synaptic transmission and neuropharmacology, facilitating studies of cholinergic signaling in conditions such as neurodegeneration and addiction. -
α7-nAChR Agonist
VQW-765 is a selective agonist for the alpha-7 nicotinic acetylcholine receptor (α7-nAChR), exhibiting a pKD value of 7.56 in recombinant human α7-nAChR assays. This compound demonstrates anxiolytic-like effects in vivo, making it a valuable tool for the study of anxiety disorders and acute performance anxiety. Researchers can utilize VQW-765 to investigate the role of α7-nAChR modulation in neuropsychiatric conditions. -
nAChR Agonist
ABT-107 is a selective agonist of the α7 neuronal nicotinic receptor (nAChR), known for its neuroprotective properties. This compound has demonstrated effectiveness in protecting against nigrostriatal damage in rodent models, specifically in rats with unilateral 6-hydroxydopamine lesions. ABT-107 is a valuable tool for research applications focusing on neurodegenerative diseases and the role of nicotinic receptors in neurological function. -
Neuromuscular Blocker
Pipecuronium bromide functions as a long-acting nondepolarizing steroidal neuromuscular blocker, acting primarily as a competitive antagonist of the nicotinic acetylcholine receptor (nAChR). With a dissociation constant (Kd) of 3.06 μM, it effectively inhibits neuromuscular transmission, making it valuable for facilitating intubation and maintaining muscle relaxation during surgical procedures. Its applications also extend to research examining neuromuscular function and pharmacological studies involving skeletal muscle. -
AChR Agonist
Anabaseine is a potent agonist of various nicotinic acetylcholine receptors (AChRs), including the neuromuscular α12β1γδ or α12β1γɛ and α7 subtypes. This brain-penetrant alkaloid toxin exhibits key biological activity as a stimulator of these receptors, making it valuable for research into neuromuscular transmission and neurobiology. Additionally, Anabaseine acts as a weak partial agonist at α4β2 nAChRs, further broadening its applications in studying cholinergic signaling pathways. -
KATP Opener
Iptakalim hydrochloride is a selective ATP-sensitive potassium channel (KATP) opener that exhibits significant lipophilicity. In addition to its primary mechanism, it also acts as an antagonist of α4β2-containing nicotinic acetylcholine receptors (nAChRs). This dual activity positions Iptakalim hydrochloride as a valuable tool for research in cardiovascular physiology and neuropharmacology, providing insights into potassium channel regulation and cholinergic signaling. -
α4β2 nAChR Agonist
NS 9283 is a positive allosteric modulator of the α4β2 nicotinic acetylcholine receptors (nAChR). It enhances receptor activity, making it useful for studying neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease, and Alzheimer's disease. This compound serves as a valuable tool for research into synaptic transmission and potential therapeutic interventions targeting nAChR-related pathways. -
α7 nAChR Agonist
Bradanicline is a highly selective agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 of 17 nM and a Ki of 1.4 nM in human α7 nAChR assays. This compound is primarily utilized in research focused on cognitive disorders, providing insights into mechanisms of action and potential therapeutic applications for enhancing cognitive function. -
Stable Isotope
(Rac)-Monepantel sulfone-d5 is a deuterium-labeled variant of Monepantel, an organic anthelmintic agent. It functions as a positive allosteric modulator of nematode-specific nicotinic acetylcholine receptor (nAChR) subunits, enhancing receptor activity. This stable isotope is valuable for research applications in studying nematode physiology and drug interaction mechanisms. -
nAChR Inhibitor
CVN417 is an orally active antagonist of the α6 subunit-containing nicotinic acetylcholine receptors (nAChRs). This inhibitor modulates phasic dopaminergic neurotransmission in an impulse-dependent manner and exhibits inhibitory effects on Ca(2+) efflux through various nAChR subunits, with IC50 values of 0.086 μM for α6, 2.56 μM for α3, and 0.657 μM for α4. CVN417 has demonstrated efficacy in reducing resting tremors in rodent models and may offer therapeutic potential for improving movement dysfunction associated with Parkinson's disease. -
Insecticide
Sulfoxaflor is an orally active agonist that specifically targets insect nicotinic acetylcholine receptors (nAChRs), including the α-bungarotoxin-insensitive subtypes nAChR1 and nAChR2. By binding to these receptors, Sulfoxaflor induces inward currents that result in neurotoxicity in insects. This compound is valuable for research applications in agricultural pest control, pesticide toxicology, and the pharmacology of insect neural receptors. -
nAChRs antagonist
Pentapeptide-3 is a pentapeptide derived from the neurotoxin waglerin-1, sourced from Temple Viper venom. It functions as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), effectively blocking nerve transmission at the post-synaptic membrane. Due to its ability to inhibit nAChRs, Pentapeptide-3 exhibits potential anti-aging effects and is often utilized in conjunction with other cosmetic peptides for research applications related to skin rejuvenation. -
α4β2 Partial Agonist
TC-2559 difumarate is a centrally active partial agonist targeting the α4β2 subtype of nicotinic acetylcholine receptors (nAChRs), with an EC50 of 0.18 μM. This compound demonstrates selectivity for α4β2 receptors over α2β4, α4β4, and α3β4 receptors, exhibiting EC50 values between 10-30 µM. TC-2559 difumarate is primarily used in research focused on antinociceptive effects and the modulation of CNS activity. -
nAChR Agonist
AR-R17779 hydrochloride is a potent and selective full agonist of the nicotinic acetylcholine receptor (nAChR), demonstrating Ki values of 92 nM for the α7 subtype and 16,000 nM for the α4β2 subtype. This compound has been shown to enhance cognitive functions, such as learning and memory, in rodent models. Additionally, AR-R17779 hydrochloride exhibits anxiolytic properties and is capable of reducing inflammation through the activation of anti-inflammatory cholinergic pathways. Its diverse biological activities make it a valuable tool for research in neurobiology and inflammation. -
nAChR Agonist
A 85380 hydrochloride is a high-affinity agonist for neuronal nicotinic acetylcholine receptors (nAChRs), specifically exhibiting selectivity for the α4β2 subtypes. This compound demonstrates a broad-spectrum analgesic profile, making it valuable for research in pain mechanisms and therapeutic applications. Its unique properties facilitate investigations into the roles of nAChRs in various biological processes. -
α7 nAChR partial agonist
S 24795 is a partial agonist of the α7 nicotinic acetylcholine receptor (nAChR), known to enhance cognitive function. This compound is particularly relevant for research into aging-related memory disturbances, as it has demonstrated the ability to improve mnemonic performance in aged mice. Its mechanism of action provides a valuable tool for studying cholinergic signaling and its implications in neurodegenerative conditions. -
nAChR Agonist
AN317 is a selective agonist for the α6β2-containing nicotinic acetylcholine receptor (nAChR), exhibiting Ki values of 6.2 nM for the α6/α3β2β3 receptor and 4.1 nM for the α4β2 receptor. This compound effectively induces dopamine release in rat striatum synaptosomes and enhances dopaminergic neuronal activity in the substantia nigra. Additionally, AN317 demonstrates neuroprotective effects against dopamine neurotoxin MPP+ and possesses favorable pharmacokinetic properties, including the ability to cross the blood-brain barrier. Research applications include studies in neuropharmacology and the exploration of mechanisms underlying dopaminergic signaling. -
nAChR Positive Allosteric Modulator
TQS is a positive allosteric modulator of the α7 nicotinic acetylcholine receptor (nAChR). This compound enhances the receptor's activity, making it a valuable tool for investigating mechanisms of neuroinflammatory pain. Researchers may utilize TQS to explore its potential therapeutic effects in neurodegenerative conditions and related pain pathways. -
nAChR Inhibitor
Triflumezopyrim is a selective inhibitor of the nicotinic acetylcholine receptor (nAChR), exhibiting potent insecticidal activity at low dosages. Its primary application is in the control of hopper species, where it demonstrates rapid efficacy while maintaining low toxicity to non-target arthropods. This compound is particularly valuable in agricultural research and pest management studies focused on sustainable and selective insect control strategies. -
α7 nAChR Agonist
α7 Nicotinic receptor agonist-1 is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR). This compound plays a crucial role in the modulation of neurotransmitter release and is significant in studies investigating various psychiatric and neurocognitive disorders. Its applications include research on conditions such as schizophrenia, anxiety disorders, Alzheimer's disease, cognitive deficits, and attention deficit hyperactivity disorder, providing insights into the therapeutic potential for these ailments. -
Insecticide
Dicloromezotiaz is a potent insecticide that targets nicotinic acetylcholine receptors (nAChRs) in insects. This compound exhibits significant efficacy in controlling a wide variety of lepidopteran pests. Research applications include studies on insect neuromuscular signaling and the development of integrated pest management strategies. -
α7 nAChR NAM
Soclenicant (BNC210) is an orally active negative allosteric modulator (NAM) of the α7 nicotinic acetylcholine receptor (nAChR). It demonstrates acute anxiolytic effects in rodent models, making it relevant for research into anxiety, trauma, and stress-related disorders. Soclenicant effectively inhibits α7 nAChR currents induced by acetylcholine, nicotine, choline, and the α7-specific agonist PNU-282987, with IC50 values ranging from 1.2 to 3 μM. This compound presents a valuable tool for investigating the role of α7 nAChRs in neuropsychiatric conditions. -
nAChR Antagonist
(-)-Coclaurine hydrochloride is a tetrahydroisoquinoline alkaloid that functions as a nicotinic acetylcholine receptor (nAChR) antagonist. This compound exhibits significant biological activity in modulating nAChR-related pathways, making it valuable for research into neuropharmacology and the development of therapeutic strategies for conditions involving cholinergic signaling. Its potential applications include studies on cognitive function, addiction, and various neurological disorders.
