Catalog No.
Product Name
Application
Product Information
Citations
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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. -
nAChR Agonist
Spinosyn L is a selective agonist of nicotinic acetylcholine receptors (nAChR). It induces sustained neural excitation and paralysis in insects, demonstrating effective activity against various agricultural pests, including Lepidoptera and Diptera. This compound is valuable for research applications focused on developing novel pesticides and understanding insect physiology. -
Insecticide Agent
nAChR modulator-2 is an orthosteric modulator of insect nicotinic acetylcholine receptors (nAChRs). This compound functions as an effective insecticide by influencing neurotransmission in target insects, leading to neurotoxic effects. It is particularly useful in research applications aimed at understanding insect physiology and the development of novel pest control strategies. -
nAChR Inhibitor
Xanthoplanine is an nAChR inhibitor derived from the root of Xylopia parviflora. It effectively inhibits the EC50 acetylcholine responses of both alpha7 and alpha4beta2 nicotinic acetylcholine receptors, demonstrating estimated IC50 values of 9 μM for alpha7 and 5 μM for alpha4beta2. Its potent inhibitory activity makes it a valuable tool for studying cholinergic signaling and related neurological pathways in research applications. -
α7 nAChR Agonist
Bradanicline tosylate is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR) with significant oral bioavailability and moderate blood-brain barrier penetration. It demonstrates high affinity and subtype specificity for human α7 nAChR, exerting antitussive effects through prolonged receptor activation. Bradanicline tosylate effectively inhibits cough responses induced by citric acid, bradykinin, and inhaled nicotine in a dose-dependent manner. This compound is well tolerated in preclinical studies, making it a valuable tool in research focused on chronic refractory cough and related therapeutic areas. -
Insecticide Agent
nAChR modulator-1 is an orthosteric modulator of insect nicotinic acetylcholine receptors (nAChR), functioning as a targeted insecticide agent. This compound demonstrates significant biological activity by disrupting neurotransmission in insects, leading to paralysis and death. It is widely utilized in research applications for studying pest control mechanisms and developing novel insecticide strategies. -
NF-κB Inhibitor
(R)-(+)-Anatabine is an NF-κB inhibitor that acts to lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). As the less active R-enantiomer of Anatabine, it retains the ability to modulate α4β2 nAChR activity. This compound exhibits anti-inflammatory properties and is being investigated for its potential applications in the treatment of neurodegenerative disorders. -
nAChR Agonist
SIB-1508Y is an orally active and selective agonist of the nicotinic acetylcholine receptor (nAChR). It holds potential for research applications related to parkinsonism and neurodegenerative disorders. Additionally, SIB-1508Y features an alkyne group, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
α7 nAChR Agonist
Nelonicline citrate is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR) with high affinity, as demonstrated by a Ki value of 12.3 nM in human brain tissue. This compound is primarily utilized in research investigating schizophrenia and Alzheimer's disease, providing insights into the modulation of cognitive processes and synaptic plasticity associated with these neurological disorders. Its oral bioavailability makes it a valuable tool for in vivo studies. -
nAChR Agonists
SIB 1663 is a conformationally restricted analog of nicotine that selectively activates α2β4 and α4β4 human recombinant neuronal nicotinic acetylcholine receptors (nAChRs). This compound has been shown to enhance the release of dopamine (DA) and norepinephrine (NE), making it a valuable tool in the study of neurotransmitter dynamics. SIB 1663 is applicable in neurological disease research, providing insights into the mechanisms underlying various neuropharmacological conditions. -
α7nACh Agonist
Epibatidine is an α7 nicotinic acetylcholine receptor (nAChR) agonist with a Kd of 100 nM. This compound is a valuable tool for investigating neurodegenerative diseases such as Alzheimer's and Parkinson's, as well as psychiatric conditions like schizophrenia. By activating the α7nACh receptors, Epibatidine can provide insights into cholinergic signaling and its implications in these disorders. -
α7 nAChR Agonist
WYE-103914 is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting EC50 values of 0.49 µM for rat and 0.57 µM for human receptors. This compound is known to enhance cognitive functions and memory in various experimental models. It is also utilized in research focusing on schizophrenia and can be administered alongside antipsychotic therapies to investigate potential synergistic effects. -
α7 nAChR Activator
IND8 is an activator of the α7 nicotinic acetylcholine receptor (nAChR), known for its cognitive enhancement properties. This compound has demonstrated efficacy in improving spatial working memory, episodic short-term memory, and spatial long-term memory in amnesic mice induced by Scopolamine. IND8 is particularly relevant for research on Alzheimer's disease and can be utilized in studies investigating interventions for cognitive decline. -
Antidepressant Agent
Cypenamine hydrochloride is an antidepressant agent that selectively interacts with human nicotinic acetylcholine receptors (nAchR) subtypes, specifically α2β4, α3β4, and α4β4, exhibiting Ki values of 4.65 μM, 2.69 μM, and 4.11 μM, respectively. This compound is commonly used in research to investigate its potential therapeutic effects in mood disorders and the underlying mechanisms of action related to neurotransmitter regulation. -
α7 nAChR PAMs
GAT107 is a potent positive allosteric modulator (PAM) of the α7 nicotinic acetylcholine receptor (nAChR). It enhances receptor activity, making it useful for research into neuropharmacology and potential treatments for cognitive disorders. Its mechanism allows for modulation of cholinergic signaling, which is crucial in areas such as memory and learning. GAT107 can aid in elucidating the functional properties of α7 nAChR in various biological contexts. -
α7 nAChR Agonist
Bradanicline hydrochloride is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 of 17 nM and a Ki of 1.4 nM for the human α7 nAChR. This compound demonstrates significant biological activity that supports research into cognitive disorders and schizophrenia. Its targeted mechanism makes it a valuable tool for studying therapeutic approaches in neuropsychiatric conditions. -
nAChR Antagonist
SR 16584 is a selective antagonist of the α3β4 nicotinic acetylcholine receptor (nAChR), exhibiting an IC50 value of 10.2 μM. This compound is utilized in research investigating the role of nAChRs in neurological disorders and potential therapeutic applications. Its specific inhibition of α3β4 nAChR makes it valuable for studying the receptor's involvement in neurotransmission and related signaling pathways. -
nAChRs Agonist
SIB-1553A free base is an orally bioavailable agonist of nicotinic acetylcholine receptors (nAChRs), exhibiting selective activity towards receptors containing the β4 subunit. This compound serves as a selective ligand for neuronal nAChRs and demonstrates significant cognitive-enhancing properties. SIB-1553A free base shows therapeutic potential for addressing symptoms associated with Alzheimer's disease and other cognitive disorders in research applications. -
α7 nAChR Partial Agonist
AZD0328 is a selective partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). It is known to enhance midbrain dopaminergic neuronal activity and increase cortical dopamine levels, contributing to improved cognitive performance. This compound is primarily used in research related to cognitive disorders and neurological modeling. -
α7 nACh Receptor Partial Agonist
BMS-933043 is a selective partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). This compound has been shown to mitigate cognitive impairment in murine models, making it a valuable tool for research focused on cognitive dysfunction, particularly in the context of schizophrenia. Its unique mechanism facilitates the exploration of neuropsychological pathways and potential therapeutic interventions. -
α7 nAChR Agonist
CP-810123 is a brain-permeable agonist of the α7 nicotinic acetylcholine receptor (nAChR). It demonstrates significant potential in enhancing cognitive function and is valuable for investigating cognitive impairments associated with psychiatric and neurological disorders, including schizophrenia and Alzheimer's disease. This compound serves as an important tool for researchers exploring therapeutic strategies aimed at modulating cholinergic systems in the context of cognitive deficits. -
α4β2 Agonist
RJR-2429 is a potent agonist of the α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 59 nM and a binding affinity (Ki) of 1 nM. This compound is known to induce contraction in the ileum, making it relevant for studies examining gastrointestinal motility and nAChR-mediated signaling pathways. RJR-2429 serves as a valuable tool in pharmacological research focused on neuropharmacology and cholinergic function. -
nAChR Agonist
1,1-Dimethyl-4-acetylpiperazinium iodide is a potent agonist of nicotinic acetylcholine receptors (nAChRs), facilitating the opening of ion channels and leading to cell membrane depolarization. This compound is instrumental in studying synaptic transmission and has applications in neuropharmacology and neuromuscular research, providing insights into cholinergic signaling pathways and potential therapeutic interventions for related disorders. -
nAChR Ligand
Hepzidine is a novel ligand for nicotinic acetylcholine receptors (nAChRs). It demonstrates binding affinity for acetylcholine binding protein (AChBP), making it a valuable tool in the study of cholinergic signaling. This compound is particularly relevant for neurobiological research, providing insights into the roles of nAChRs in various neurological conditions and processes. -
Stable Isotope
Mecamylamine-d3 hydrochloride is a deuterium-labeled derivative of Mecamylamine hydrochloride, functioning as a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChR). This stable isotope is employed in research applications focused on neuropsychiatric disorders and the pharmacological assessment of nAChR activity. Its ability to cross the blood-brain barrier facilitates investigations into central nervous system functions and disorders, as well as potential therapeutic interventions. -
nAChR Modulator
Bensultap is a nicotinic acetylcholine receptor (nAChR) modulator known for its insecticidal properties against the Colorado beetle and other insect pests. This compound exhibits mild and temporary neuromodulatory effects on the rat nervous system, making it relevant for research into nAChR function and insect neurobiology. Its applications extend to studies in pest management and the exploration of neural signaling pathways impacted by nAChR modulation. -
Alkaloid
(±)-Coniine is a piperidine alkaloid known for its function as an nAChR agonist, demonstrating an EC50 of 0.3 mM. This compound exhibits acute toxicity in murine models, with an LD50 value of 7.7 mg/kg. Its unique properties make it valuable for research applications focused on neuromuscular transmission and toxicity studies. -
nAChR Agonist
Hydroxy Varenicline is a metabolite of varenicline, functioning as a nicotinic acetylcholine receptor (nAChR) agonist. This compound exhibits key biological activity by modulating nAChR signaling, making it relevant for research on nicotine addiction and its neuropharmacological effects. Hydroxy Varenicline serves as a valuable tool in studies aimed at understanding receptor dynamics and developing therapeutic strategies for smoking cessation and related disorders. -
α4β2 nAChR Partial Agonist
3-Pyr-Cytisine is a cytisine derivative that functions as a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR). This compound exhibits weak agonistic properties, making it of interest in antidepressant research. Its modulation of α4β2 nAChR may provide insights into therapeutic strategies for mood disorders and further understanding of cholinergic signaling pathways. -
nAChR Agonist
Sofinicline benzenesulfonate is a potent agonist of the nicotinic acetylcholine receptor, specifically targeting the α4β2 subtype with an IC50 of 0.1 nM. This compound has demonstrated potential to enhance cognitive functions, including attention and memory, making it a valuable tool in the investigation of cognitive impairments. Its applications extend to research on attention deficit hyperactivity disorder (ADHD) and other cognitive disorders. -
nAChR Antagonist
Microgrewiapine A is a selective antagonist of nicotinic acetylcholine receptors (nAChR), specifically inhibiting human α4β2 and α3β4 subtypes with 60% and 70% efficacy, respectively. This compound demonstrates cytotoxic effects in HT-29 human colon cancer cells, exhibiting an IC50 value of 6.8 μM. Microgrewiapine A holds potential for research applications in cancer biology and neuropharmacology. -
AChE/nAChR Inhibitor
AChE/nAChR-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and nicotinic acetylcholine receptors (nAChR). This compound exhibits potent toxicity and larvicidal activity against Culex pipiens larvae, with an LC50 of 4 ng/mL. AChE/nAChR-IN-1 is utilized in research focused on controlling mosquito populations and studying mosquito-borne diseases. -
Stable Isotope
Varenicline-13C,15N is a stable isotope-labeled variant of Varenicline, a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), with an IC50 of 250 nM. This compound also interacts with α6β2 nAChR as a partial agonist and activates α7β2 nAChR as a full agonist. Varenicline-13C,15N is utilized in research to study nicotine dependence and the pharmacodynamics of smoking cessation therapies, providing valuable insights into receptor interactions and metabolic pathways. -
nAChR Antagonist
Dexmecamylamine is a selective antagonist of the nicotinic acetylcholine receptors (nAChR), specifically targeting the α3β4, α4β2, α7, and α1β1γδ subtypes with IC50 values in the micromolar range. This compound demonstrates notable anxiolytic and antidepressant-like effects, making it a valuable tool in neurological research and the study of mood disorders. Its ability to modulate nAChR activity positions it as a potential lead for therapeutic development in psychiatric conditions. -
nAChR Agonist
TC-2216 is an agonist of the α4β2 neuronal nicotinic acetylcholine receptors (nAChRs). This compound demonstrates significant antidepressant and anxiolytic properties, validated by multiple animal models. TC-2216's modulation of nAChR activity represents its potential utility in neuropharmacological research and the development of therapeutic strategies for mood disorders. -
AChE Inhibitor
Sinapine is an acetylcholinesterase (AChE) inhibitor derived from cruciferous seeds. This compound demonstrates a range of biological activities, including anti-inflammatory, antioxidant, anti-tumor, anti-angiogenic, and radio-protective effects. Sinapine is instrumental in research targeting neurodegenerative disorders such as Alzheimer's disease, myasthenia gravis, ataxia, and Parkinson’s disease, making it a valuable tool for advancing scientific understanding in these areas.
