Catalog No.
Product Name
Application
Product Information
Citations
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nAChR Agonist
Epibatidine dihydrochloride is a potent agonist of nicotinic acetylcholine receptors (nAChRs), significantly influencing neurotransmission and synaptic activity. Its strong affinity for nAChRs makes it a valuable tool for studying cholinergic signaling pathways and their implications in various neurological disorders. This compound is commonly utilized in research aimed at elucidating the roles of nAChRs in addiction, pain modulation, and cognitive functions. -
nAChR Antagonist
BTMPS is a selective antagonist of the nicotinic acetylcholine receptor (nAChR). It has been shown to mitigate the adverse effects of morphine in animal models, making it a valuable tool for research into addiction and pain management therapies. Its role in modulating neurotransmitter systems presents opportunities for further studies in neuropharmacology and the development of novel therapeutic strategies. -
nAChR Agonist
(E/Z)-Acetamiprid is a neonicotinoid insecticide acting as an agonist of nicotinic acetylcholine receptors (nAChR). Its mechanism of action involves the modulation of neurotransmission, which is critical in neuromuscular junction function. This compound is primarily utilized in research exploring insect physiology, neurobiology, and the potential effects of insecticides on reproduction and neuromuscular disorders. -
Deuterium Labeled Acetamiprid
Acetamiprid-d3 is a deuterium-labeled derivative of Acetamiprid, a neonicotinoid insecticide that acts as an agonist at nicotinic acetylcholine receptors (nAChRs). This labeled compound is useful for tracing and quantifying Acetamiprid in various biological and environmental samples. Research applications include studying the pharmacokinetics and dynamics of Acetamiprid, as well as its impact on insect physiology and behavior. -
nAChR Inhibitor
nAChR-IN-2 is an inhibitor of insect nicotinic acetylcholine receptors (nAChR), targeting the acetylcholine binding site and the NCB/PCP binding site. It demonstrates an IC50 of 360 μM for α-bungarotoxin binding and 84 μM for Phencyclidine binding in honeybee head preparations. This compound is valuable for studying nAChR-mediated signaling pathways and their role in insect neurobiology. Research applications include investigating insecticide mechanisms and assessing the neurophysiological effects of nAChR modulation. -
α3β4 nAChR Ligand
F4-Trp (4,5,6,7-Tetrafluoro-L-tryptophan) is a selective ligand for the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR). This compound exhibits significant activity in modulating neurotransmission and is valuable for studying addiction and related neurological disorders. F4-Trp serves as a critical tool for researchers investigating the intricate mechanisms of receptor function and the pathophysiology of associated diseases. -
nAChRs Inhibitor
bPiDI is a selective antagonist of the α6β2 nicotinic acetylcholine receptors (nAChRs). It effectively inhibits nicotine-evoked dopamine release in the striatum, making it a valuable tool for studying dopaminergic signaling pathways. This compound is particularly useful in research pertaining to nicotine addiction and dopamine-related disorders. -
α7 nAChR Agonist
PHA-543613 hydrochloride is a potent agonist of the α7 nicotinic acetylcholine receptor (nAChR) with demonstrated brain permeability. This compound selectively targets α3β4, α1β1γδ, α4β2, and 5-HT3 receptors. PHA-543613 hydrochloride has shown significant effects on sensory gating and memory in in vivo models of schizophrenia, making it valuable for research in neuropharmacology and psychopharmacology. -
α7 nAChR Agonist
PHA-543613 dihydrochloride is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR), exhibiting a Ki value of 8.8 nM. This compound is orally active and capable of penetrating the blood-brain barrier, making it suitable for in vivo studies. PHA-543613 dihydrochloride demonstrates strong selectivity for the α7 nAChR over α3β4, α1β1γδ, α4β2, and 5-HT3 receptors. It is applied in research pertinent to cognitive deficits associated with Alzheimer's disease and schizophrenia. -
nAChR Potentiator
LY-2087101 is an allosteric potentiator of the α7 nicotinic acetylcholine receptors (nAChRs). This compound enhances agonist-evoked responses by binding to the transmembrane region of the receptor, leading to increased receptor activation. LY-2087101 is useful for research focused on synaptic transmission, neuropharmacology, and the modulation of cognitive functions. -
α7-AChR Agonist/α4β2 nAChR Antagonist
DMAB-anabaseine dihydrochloride acts as a selective partial agonist at the α7 nicotinic acetylcholine receptor (nAChR) and an antagonist at the α4β2 nAChR. This compound has been shown to enhance cognitive function, making it a valuable tool for research in neuropharmacology and cognitive disorders. Its unique receptor profile highlights its potential applications in investigating therapeutic strategies for enhancing cognition and treating related diseases. -
Nicotinic Acetylcholine Receptor Agonist
DBO-83 dihydrochloride is an innovative agonist of the nicotinic acetylcholine receptor (nAChR), exhibiting a high affinity for nAChRs in rat cortical membranes with a Ki value of 4.1 nM. This compound demonstrates significant antinociceptive and anti-amnesic properties, making it a valuable tool for research into pain modulation and cognitive function. Its potential applications in neuroscience and pharmacology make DBO-83 dihydrochloride a critical reagent for studying neuronal signaling pathways and associated disorders. -
AChE Reversible Inhibitor
Asoxime dimesylate is a reversible inhibitor of acetylcholinesterase (AChE) that serves as a thiosemicarbazone-based antidote. Its primary mechanism of action involves reactivating AChE inhibited by nerve agents, thus restoring cholinergic nerve function. Additionally, Asoxime dimesylate has been shown to significantly restore muscle function compromised by poisoning without the reactivation of AChE. It also acts as an antagonist at acetylcholine receptors, including nicotinic receptors and α7 nAChR, and demonstrates potential as an immunomodulator, enhancing immune responses in the nervous system. This compound is valuable for research in neuropharmacology and toxicology. -
Nicotinic Acetylcholine Receptor Agonists
A85380 is a high-affinity agonist for neuronal nicotinic acetylcholine receptors (nAChRs), demonstrating selectivity for the α4β2 nAChR subtype. This compound has been shown to possess a broad-spectrum analgesic profile, making it valuable in pain research. Its distinct mechanism of action offers potential insights into the therapeutic applications of nAChR modulation in various neurological disorders. -
nAChR Inhibitor
Lupanine perchlorate is a natural ketonic derivative of sparteine that functions as an nAChR inhibitor. It exhibits significant ganglioplegic activity and demonstrates a binding affinity for nicotinic receptors with a Ki value of 500 nM. This compound is commonly utilized in research focused on studying neuronal signaling and the effects of cholinergic modulation. -
α4β2 nAChR Agonist
nAChR agonist 2 is a selective agonist for the α4β2 nicotinic acetylcholine receptor (nAChR) with a dissociation constant (Kd) of 26 nM. This compound demonstrates significant biological activity in modulating neurotransmitter release and enhancing synaptic transmission. It is valuable for research applications involving neuropharmacology and the study of neurological disorders associated with cholinergic signaling. -
nAChR Antagonist
Lobelanidine is a selective antagonist of nicotinic acetylcholine receptors (nAChR), effectively inhibiting the α7 nAChR response as well as the α3β2/α3β4 nAChR responses, with IC50 values of 2.8 μM and 8.2 μM, respectively. This compound serves as a valuable tool for investigating the role of nAChRs in neuronal signaling and various neurological disorders. Its pharmacological properties make it suitable for research applications in neurobiology, drug discovery, and toxicology studies. -
α7 nAChR Potentiator
RO5126946 is a selective allosteric potentiator of the α7 nicotinic acetylcholine receptor (nAChR) with an EC50 of 0.06 μM for human α7 nAChR. This compound enhances synaptic transmission and positively modulates GABAergic responses by increasing peak current and elevating the frequency of spontaneous inhibitory postsynaptic currents while preserving receptor recovery from desensitization. RO5126946 is valuable for investigating cognitive deficits associated with neurodegenerative disorders such as Alzheimer's disease and psychiatric conditions including schizophrenia, as it augments the cognitive-enhancing effects of nicotine without detracting from its efficacy. -
nAChR Agonist
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor. This compound enhances the potency and efficacy of various nicotinic acetylcholine receptor agonists, making it a valuable tool in pain management research. In preclinical studies, co-administration of A-424274 with an α4β2 positive allosteric modulator has been shown to significantly improve the analgesic effects of ABT-594, demonstrating its potential for enhancing therapeutic outcomes in pain relief. -
nAChR Antagonist
nAChR antagonist 1 is a selective antagonist of the α7 nicotinic acetylcholine receptor, exhibiting an IC50 value of 3.3 μM. This compound is valuable for studying the role of α7 nAChR in various neurological conditions, including schizophrenia, Alzheimer's disease, and inflammatory disorders. Its modulatory effects on neurotransmission make it a relevant tool for exploring therapeutic strategies in these disease contexts. -
nAChR Inhibitor
Ferulamide is a derivative of ferulic acid that acts as a competitive inhibitor of nicotinic acetylcholine receptors (nAChRs). It exhibits significant anticholinesterase activity, making it a valuable tool for studying cholinergic signaling pathways. This compound is useful in research related to neurodegenerative diseases and the modulation of synaptic transmission. -
α7 nAChR Inhibitor
QND8 is a selective and potent inhibitor of the α7 nicotinic acetylcholine receptor (nAChR). It demonstrates significant biological activity by alleviating thermal and mechanical hyperalgesia in carrageenan-induced inflammatory pain models. QND8 effectively reduces swelling, inhibits the release of pro-inflammatory cytokines, and prevents leukocyte infiltration at the inflammatory site. This compound is valuable for research applications focused on inflammation and neurological disorders, including arthritis. -
α7 nAChR Modulator
RGH-560 is a positive modulator of the α7 nicotinic acetylcholine receptor (nAChR), known for its advanced pharmacological properties and favorable physicochemical characteristics. This compound exhibits significant procognitive effects in vivo, making it a valuable tool for studying cognitive enhancement. RGH-560 is particularly useful in researching scopolamine-induced amnesia in murine models, providing insights into memory and learning processes. -
α7nAChR Antagonist
Methyllycaconitine is a selective competitive antagonist of the α7 nicotinic acetylcholine receptor (α7nAChR). It demonstrates significant neuroprotective effects by alleviating cytotoxicity induced by amyloid-β peptides in SH-SY5Y cells and mitigating methamphetamine-induced effects in the mouse striatum. Methyllycaconitine is a valuable tool for research into neurological disorders, including Alzheimer's disease. -
Stable Isotope
Anabaseine-d4 is a deuterium-labeled form of Anabaseine, functioning as a non-selective nicotinic receptor agonist. This compound effectively stimulates all acetylcholine receptors (AChRs), with a particular preference for skeletal muscle and brain α7 subtypes. Additionally, Anabaseine exhibits weak partial agonistic activity at α4β2 nAChRs, making it valuable for research applications focused on neurotransmission and neuromuscular function. -
nAChR Agonist
RJR-2429 dihydrochloride is an agonist of the α4β2 and α7 nicotinic acetylcholine receptors (nAChRs). This compound exhibits significant biological activity in modulating neurotransmission and is widely used in research to explore the role of nAChRs in neuronal signaling, cognitive processes, and neurodegenerative diseases. Its selective action on these receptor subtypes makes it a valuable tool for investigating cholinergic pathways and their implications in various physiological and pathological conditions. -
α4β2 nAChR Agonist
TC-6683 is a selective agonist of the α4β2 nicotinic acetylcholine receptor (nAChR). This compound has shown potential in modulating cholinergic signaling pathways and is primarily utilized in research related to neurological disorders, particularly cognitive dysfunction. Although TC-6683 demonstrated limited therapeutic efficacy in an animal model of DYT1 dystonia, its role in studying nAChR dynamics makes it a valuable tool for investigating various neurobiological processes. -
nAChRs Agonist
TC299423 is a selective and potent agonist of the α6β2 and α4β2 nicotinic acetylcholine receptors (nAChRs) with significant anxiolytic and antinociceptive properties. This orally active compound effectively penetrates the blood-brain barrier and primarily targets the α6β2 nAChRs, which are associated with the anxiolytic effects of nicotine. Research indicates that TC299423 induces reward-related behaviors in α6L90’S hypersensitive mice and stimulates dopamine release without inhibiting nicotine self-administration in rats. Its pharmacological profile suggests potential applications in the study of addiction and Parkinson's disease. -
nAChR Antagonist
T761-0184 is a potent antagonist of the alpha-7 nicotinic acetylcholine receptor (nAChR). This compound effectively inhibits nAChR activity, making it a valuable tool for studying neurotransmission and synaptic plasticity. It holds potential for research applications in neurological disorders and offers insights into the mechanisms underlying cholinergic signaling. -
α-7 nAchR Agonist
PHA 568487 is a selective agonist of the α-7 nicotinic acetylcholine receptor (α-7 nAchR). This compound demonstrates significant biological activity in reducing neuroinflammation and oxidative stress, making it valuable for research in neurodegenerative diseases and cognitive disorders. Its ability to rapidly penetrate the blood-brain barrier enhances its potential for therapeutic applications in central nervous system studies. -
nAChR Inhibitor
Aristoquinoline is a naturally occurring alkaloid derived from Aristotelia chilensis, functioning primarily as an inhibitor of the α3β4 nicotinic acetylcholine receptor (nAChR). This compound demonstrates significant biological activity by modulating neurotransmitter signaling, making it a valuable tool for research in neuropharmacology, particularly in studies related to addiction, cognitive function, and neurodegenerative diseases. Its specific inhibitory effect on nAChR presents opportunities for investigating the receptor's role in various physiological processes. -
Nicotine Metabolite
R-(+)-Cotinine is a nicotine metabolite that primarily targets nicotinic acetylcholine receptors. It has been shown to enhance acetylcholine-evoked currents in human α7 nAChRs, indicating its potential role in modulating cholinergic neurotransmission. This compound is valuable for research applications focused on nicotine effects, signaling pathways, and receptor pharmacology. -
nAChR
Sazetidine A hydrochloride is a potent ligand that targets the α4β2 nicotinic acetylcholine receptor (nAChR). It exhibits high binding affinity and selectivity for this receptor subtype, making it a valuable tool in pharmacological research. Its properties may contribute to the development of therapies for conditions related to nicotinic receptor dysfunction. Additionally, Sazetidine A hydrochloride serves as an important compound in studies investigating the binding affinities of various nAChR analogs, enhancing the understanding of subtype selectivity among ligands. -
α4β2 nAChR Agonist
A 844606 is a highly selective agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), demonstrating potent activation of this target. Its significant biological activity makes it a valuable tool for investigating neurodegenerative and psychiatric conditions, including schizophrenia, Huntington's disease, Alzheimer's disease, and Parkinson's disease. Researchers can utilize A 844606 to explore the role of α4β2 nAChR in these disorders and to assess potential therapeutic strategies. -
nAChR Agonist
Anabasine hydrochloride is a potent agonist of nicotinic acetylcholine receptors (nAChRs). This alkaloid, derived from tobacco (Nicotiana), functions as a full agonist, inducing depolarization in TE671 cells that endogenously express human fetal muscle-type nAChRs (EC50 = 0.7 µM). Anabasine hydrochloride is relevant for research applications in neurobiology and toxicology, particularly in studies exploring nAChR signaling and muscle contraction mechanisms. -
nAChR Antagonist
Chlorisondamine is a nicotinic acetylcholine receptor antagonist that functions as a ganglionic blocker. It has been employed in studies to assess neurogenic factors influencing blood pressure and sympathetic vasomotor tone in animal models. Chlorisondamine exhibits antihypertensive properties, with significant effects on blood pressure, cardiac output, and heart rate, notably in murine experimental designs. -
nAChR Agonist
nAChR agonist CMPI hydrochloride is a selective positive allosteric modulator of nicotinic acetylcholine receptors (nAChRs) featuring the α4:α4 subunit interface. It significantly enhances the activity of the (α4)3(β2)2 nAChR in response to acetylcholine, with an EC50 value of 0.26 µM. This compound is valuable for research into nicotine dependence and various neuropsychiatric disorders linked to reduced cholinergic activity in the brain. -
α7 nAChR Agonist
SEN 78702 is an orally active, selective full agonist of the α7 nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.13. This compound is known to enhance memory functions, making it a valuable tool for research in cognitive disorders. Additionally, SEN 78702 exhibits an acceptable level of hERG inhibition (IC50: 15.8 μM), indicating its potential for further pharmacological investigations. -
nAChR Agonist
Lobeline is a potent nicotinic acetylcholine receptor (nAChR) agonist that effectively penetrates the blood-brain barrier. By inhibiting dopamine (DA) uptake into synaptic vesicles and altering presynaptic DA storage, Lobeline enhances DA release. It is primarily utilized in research focused on addiction and smoking cessation, making it a valuable reagent in the study of dopaminergic signaling pathways. -
Isotope-Labeled Compounds
Varenicline-15N3 Hydrochloride is the nitrogen-15 labeled isotope of Varenicline hydrochloride, a known partial agonist of the α4β2 nicotinic acetylcholine receptor (α4β2 nAChR) with an IC50 value of 250 nM. It targets nicotine dependence by mitigating the direct agonistic effects of nicotine while providing moderate stimulation of nAChR. Additionally, Varenicline exhibits partial agonist activity at α6β2 nAChR and full agonism at another subset of this receptor. This isotope-labeled compound is valuable for pharmacokinetic studies and research into nicotine addiction and smoking cessation therapies. -
nAChR Antagonist
(S)-UFR2709 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), with a notable preference for the α4β2 subtype over α7. This compound exhibits anxiolytic properties, effectively reducing anxiety and lowering ethanol consumption and preference in alcohol-preferring rat models. (S)-UFR2709 serves as a valuable reagent for research into nicotine addiction and related behavioral studies. -
Stable Isotope
Cytisine-d4 is a deuterium-labeled derivative of Cytisinicline, an alkaloid known for its role as a partial agonist at α4β2 nicotinic acetylcholine receptors (nAChRs) and for displaying full to partial agonism at β4-containing and α7 receptors. This stable isotope is utilized in research applications aimed at studying receptor interactions and pharmacokinetics, as well as in investigations related to smoking cessation therapies. The incorporation of deuterium allows for enhanced tracking of metabolic pathways and biological activity in various experimental settings. -
nAChR Agonist
Epiboxidine is a potent and selective agonist of neural nicotinic acetylcholine receptors (nAChRs), demonstrating Ki values of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. As a methylisoxazole derivative of the alkaloid Epibatidine, Epiboxidine serves as a valuable tool for studying nAChR-related pathways and their physiological functions. This compound is instrumental in exploring the potential therapeutic applications in neuropharmacology and other related fields. -
α7 nAChR Agonist
BMS-902483 is a quinuclidine-derived partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). This compound has been shown to enhance cognitive function in preclinical rodent models, making it a valuable tool for investigating cognitive impairment and associated disorders. Its properties make BMS-902483 suitable for research into neuropharmacology and the development of therapeutic strategies for cognitive enhancement. -
α7 nAChR Antagonist
nAChR antagonist 3 is a selective antagonist of the α7 nicotinic acetylcholine receptor, demonstrating an IC50 of 0.86 μM. It exhibits protective effects against toxicity induced by paraoxon, making it a valuable tool for studying organophosphate poisoning. This compound is suitable for research applications focusing on neuroprotection and receptor modulation associated with cholinergic signaling pathways. -
Stable Isotope
Varenicline-d4 is a deuterium-labeled derivative of Varenicline, a potent partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Additionally, Varenicline acts as a full agonist at the α3β4 and α7 nAChRs, exhibiting EC50 values of 55 μM and 18 μM, respectively. This stable isotope is instrumental for research involving smoking cessation therapies and the pharmacological investigation of nicotinic receptors. -
nAChR Inhibitor
nAChR-IN-1 hydrochloride is a selective nicotinic acetylcholine receptor (nAChR) inhibitor that specifically targets nAChRs lacking the α5, α6, or β3 subunits. This compound is particularly useful in studying the roles of nAChRs in neurological disorders and offers potential insights into therapeutic strategies for conditions involving nicotinic acetylcholine receptor dysfunction. Its effectiveness in modulating nAChR activity makes it a valuable tool for chemical biology and pharmacological research. -
nAChR Agonist
Rivanicline fumarate is a selective agonist of neuronal nicotinic acetylcholine receptors (nAChRs), primarily targeting the α4β2 subtype with a Ki of 26 nM and an EC50 of 16 μM. This compound has demonstrated the ability to significantly restore learning impairments and alleviate cognitive dysfunctions. Rivanicline fumarate is valuable in research focused on neurodegenerative diseases, including schizophrenia and Alzheimer's disease, providing insights into potential therapeutic approaches. -
nAChR Antagonist
(rel)-Asperparaline A is a potent antagonist of nicotinic acetylcholine receptors (nAChR), extracted from okara fermented with Aspergillus japonicas JV-23. This compound displays significant paralytic activity in silkworms, highlighting its potential as an anthelmintic agent. Its selectivity and effectiveness make it valuable for research applications focused on neurotransmission and parasitic control. -
nAChR Inhibitor
Lupanine hydrochloride is a natural ketonic derivative of Sparteine, functioning as a nicotinic acetylcholine receptor (nAChR) inhibitor. It demonstrates binding affinity for the nAChR with a Ki value of 500 nM, indicating its potential role in modulating cholinergic signaling. This compound is suitable for research applications related to neuromuscular transmission and ganglioplegic activity.
