Catalog No.
Product Name
Application
Product Information
Citations
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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. -
nAChR Agonist
(±)-Coniine hydrochloride is a potent agonist of the nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 value of 0.3 mM. It serves as an important tool in research focused on neurobiology and the modulation of cholinergic signaling. Due to its acute toxicity, characterized by an LD50 value of 7.7 mg/kg, careful handling is advised in laboratory settings. -
α4β2 nAChR Partial Agonist
CP-601927 is a selective partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), exhibiting a Ki value of 1.2 nM and an EC50 of 2.6 μM. This compound demonstrates effective brain penetration and possesses antidepressant-like properties, making it a valuable tool in neurological research. Its modulation of nAChR activity is relevant for studies exploring neuropsychiatric disorders and the underlying mechanisms of depression. -
nAChR Antagonist
Flupyrimin is a potent antagonist of the insect nicotinic acetylcholine receptor (nAChR), exerting insecticidal activity by disrupting normal neural signaling in insects. This compound is utilized in research focused on understanding insect physiology and the mechanisms of action of insecticides. Flupyrimin's ability to inhibit nAChR function makes it a valuable tool for studying insect neurobiology and developing targeted pest control strategies. -
CP-601927 Racemate
(Rac)-CP-601927 hydrochloride is a racemic mixture of CP-601927, functioning as a nicotinic acetylcholine receptor (nAChR) agonist. It exhibits high affinity with Ki values of 1.2 nM for the α4β2 receptor and 102 nM for the α3β4 receptor. This compound is utilized in research applications focused on neurological studies and the modulation of synaptic transmission involving nAChRs. -
nAChR Inhibitor
nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a selective inhibitor of nicotinic acetylcholine receptors (nAChRs) that specifically targets receptors lacking α5, α6, or β3 subunits. This compound demonstrates significant potential in alleviating nerve disorders and is valuable for research focused on nAChR dysfunction and various neurological conditions. Its mechanism of action makes it an essential tool for studying the role of nAChRs in neurological signaling pathways. -
nAChR Agonist
3-Bromocytisine is a potent agonist of nicotinic acetylcholine receptors (nAChRs), exhibiting IC50 values of 0.28 nM, 0.30 nM, and 31.6 nM for human α4β4, α4β2, and α7 nAChRs, respectively. It demonstrates differential effects on high sensitivity (HS) and low sensitivity (LS) α4β2 nAChRs, with EC50 values of 8 nM and 50 nM, respectively. This compound is valuable for research in neuropharmacology and studies related to nicotine addiction and receptor pharmacodynamics. -
nAChR Antagonist
(S)-UFR2709 hydrochloride is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with a higher affinity for the α4β2 subtype compared to the α7 subtype. This compound has demonstrated anxiolytic properties, effectively reducing anxiety levels and decreasing both ethanol consumption and preference in alcohol-preferring rat models. (S)-UFR2709 hydrochloride serves as a valuable tool for research into nicotine addiction and related neuropharmacological studies. -
nAChR Antagonist
MG624 is a potent and selective antagonist of the neuronal α7 nicotinic acetylcholine receptor (nAChR), exhibiting a Ki value of 106 nM. This compound primarily inhibits α7 nAChR-mediated signaling, making it a valuable tool for research investigating cholinergic neurotransmission and related neurological disorders. MG624 can be utilized in studies exploring the role of α7 nAChR in synaptic plasticity, cognitive function, and neurodegenerative disease mechanisms. -
nAChR Agonist
5-AAM-2-CP is a potent nAChR agonist, primarily functioning as a significant metabolite of the neonicotinoid insecticide Acetamiprid. Its primary biological activity includes the modulation of nicotinic acetylcholine receptors, which plays a critical role in neurotransmission. This compound is essential for research applications focused on neurobiology and insect neurophysiology, offering insights into the mechanisms of insecticides and synaptic transmission. -
Stable Isotope
(Rac)-Monepantel-d5 is a deuterium-labeled derivative of Monepantel, an organic anthelmintic. It functions as a positive allosteric modulator of nematode-specific nicotinic acetylcholine receptor (nAChR) subunits, enhancing receptor activity. This reagent is valuable for research applications in parasitology and neurobiology, facilitating studies on receptor modulation and nematode physiology. -
nAChR Agonist
5-AMAM-2-CP is a potent agonist of nicotinic acetylcholine receptors (nAChRs). As a key metabolite of the neonicotinoid insecticide Acetamiprid, it plays a significant role in understanding the neurotoxic effects of neonicotinoids on non-target species. This compound is valuable for research into nAChR-mediated pathways and their implications in both insect physiology and environmental science. -
Stable Isotope
Myosmine-d4 is a deuterated form of myosmine, a tobacco alkaloid known for its role in various biological systems. It exhibits low affinity for the α4β2 nicotinic acetylcholinergic receptors (nAChR), with a Ki of 3300 nM. This stable isotope is primarily used in pharmacokinetic studies and metabolic labeling experiments, providing valuable insights into the behavior and fate of myosmine in biological matrices. -
α4β2 nAChR Ligand
Sazetidine A dihydrochloride is an α4β2 nicotinic acetylcholine receptor (nAChR) ligand known for its potent binding affinity and selectivity for this receptor subtype. It demonstrates significant pharmacological properties, making it a valuable tool for investigating nicotinic receptor-related conditions. Research applications include studies focused on ligand binding affinity and the exploration of analogs, contributing to the understanding of nAChR subtype selectivity. -
nAChR Agonist
S16961 is a potent agonist of nicotinic acetylcholine receptors (nAChRs). This compound induces receptor activation, making it valuable for studies related to neurotransmission and synaptic plasticity. Research applications include exploring neurological disorders, cognitive function, and the mechanisms of addiction. -
α7 nAChR Positive Allosteric Modulator
nAChR agonist 1 is a selective positive allosteric modulator of the α7 nicotinic acetylcholine receptor (α7 nAChR). It demonstrates potent activity with an EC50 of 0.32 μM in a calcium mobilization assay utilizing human IMR-32 neuroblastoma cells that express α7 nAChR endogenously. This compound shows promise for further development in therapeutic applications for Alzheimer's disease. -
α3β4 nAChR Agonist
NS3861 fumarate is a potent agonist of the heteromeric α3β4 nicotinic acetylcholine receptor (nAChR), exhibiting high affinity with a binding Ki of 0.62 nM. This compound selectively engages with α3β4 nAChRs while also demonstrating varying affinities for other nAChR subtypes, including α3β2 (25 nM), α4β4 (7.8 nM), and α4β2 (55 nM). NS3861 fumarate is primarily used in neurological research to investigate nAChR functions and their roles in neuropharmacology. -
α7 nAChR Agonist
SEN12333 is a potent and selective agonist of the α7 nicotinic acetylcholine receptor (nAChR). It demonstrates high affinity for rat α7 nAChRs, with a Ki value of 260 nM, and functions as a full agonist in calcium flux studies, achieving an EC50 of 1.6 μM. This compound is utilized in research focusing on Alzheimer's disease and schizophrenia, facilitating the exploration of therapeutic interventions targeting cholinergic signaling pathways. -
nAChRs Allosteric Modulator
Br-PBTC is a selective positive allosteric modulator of nicotinic acetylcholine receptors (nAChRs), specifically targeting the α2β2, α2β4, α4β2, α4β4, (α4β2)2α4, and (α4β2)2β2 subtypes with effective concentration (EC50) values ranging from 0.1 to 0.6 μM. By acting on the c-terminal region of the α subunit, Br-PBTC enhances receptor activity, making it a valuable tool for studying nAChR-mediated signaling pathways and their implications in neuropharmacology and related fields. -
α3β4 nAChR Agonist
CP-601932 is a high-affinity partial agonist targeting the α3β4 nicotinic acetylcholine receptor (nAChR), with a Ki of 21 nM and an EC50 of approximately 3 μM. It exhibits comparable binding affinity at the α4β2 nAChR, while displaying significantly lower affinity for the α6 and α7 subtypes. CP-601932 is demonstrated to selectively reduce ethanol consumption and operant self-administration behaviors following prolonged exposure, suggesting its potential utility in addiction research. Furthermore, this compound effectively penetrates the central nervous system, enabling comprehensive studies of its effects on neurobiology. -
nAChR Agonist
(Rac)-ABT-202 dihydrochloride is a racemic mixture that functions as an agonist for nicotinic acetylcholine receptors (nAChRs). This compound exhibits notable analgesic properties, making it useful in pain research. Its action on nAChRs elucidates potential pathways in neurological studies and could contribute to the development of novel pain management therapies. -
nAChR Agonist
Epiboxidine hydrochloride is a potent and selective agonist of the nicotinic acetylcholine receptors (nAChRs), exhibiting Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. This compound, a methylisoxazole analog of the alkaloid Epibatidine, plays a critical role in studying nAChR-mediated signaling pathways. Its high affinity and selectivity make it valuable for research applications in neurobiology and pharmacology, particularly in the exploration of neurological disorders and drug development targeting nAChRs. -
nAChRs Agonist
SIB-1553A is a selective agonist of nicotinic acetylcholine receptors (nAChRs), specifically targeting β4 subunit-containing receptors. This compound exhibits neuroprotective properties and enhances cognitive function, making it a valuable tool in the study of Alzheimer’s disease and other cognitive disorders. Its oral bioavailability further supports its potential for therapeutic applications in cognitive enhancement. -
Stable Isotope
Flupyradifurone-d5 is a deuterated derivative of Flupyradifurone, a systemic nicotinic acetylcholine receptor (nAChR) agonist. This compound disrupts signal transduction in the central nervous system of sucking pests, making it effective as a butenolide insecticide. Flupyradifurone-d5 can be utilized in research focused on pest control mechanisms and the study of insecticide efficacy in agricultural applications. -
nAChR Inhibitor
Azemiopsin is a potent inhibitor of nicotinic acetylcholine receptors (nAChR), exhibiting IC50 values of 0.18 μM against the T. californica nAChR and 22 μM against the human α7 nAChR. This compound effectively blocks acetylcholine-induced currents in Xenopus oocytes that are heterologously expressing human muscle-type nAChR. Azemiopsin serves as a valuable tool for investigating nAChR-mediated signaling pathways and contributes to studies on neuropharmacology and synaptic transmission. -
nAChR Antagonist
bPiDDB is a potent antagonist of nicotinic acetylcholine receptors (nAChRs), specifically targeting α6β2-containing subtypes. It demonstrates significant inhibitory activity on nicotine-induced striatal dopamine release, with an IC50 value of 2 nM. This compound is valuable for research focused on nAChR-mediated signaling pathways and the role of dopamine in neurological studies.
