Catalog No.
Product Name
Application
Product Information
Citations
-
B-type AChR activator
Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator. -
nAChR antagonist
Mecamylamine hydrochloride is a nAChR antagonist previously used to treat hypertension. It displays a wide variety of activities, including reducing depression-like behaviors in subjects with Tourette's syndrome and improving rates of smoking cessation. -
nAchR agonist
Pyrantel tartrate is an antinematodal thiophene nicotinic receptor agonist and can elicit spastic muscle paralysis in parasitic worms due to prolonged activation of the excitatory nicotinic acetylcholine (nACh) receptors on body wall muscle. - Choline chloride is a quaternary ammonium salt used as an additive for animal feed.
-
non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. -
α3β4 nAChR ligand
AT-1001 is a tight junction regulator and reverses leaky junctions to their normally closed state. It is being studied in people with celiac disease -
α4β2 nAChR partial agonist
Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. -
nAChR modulator
Tebanicline hydrochloride (ABT594 hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. -
nAChR agonist
PNU 282987 is a highly selective α7 nAChR agonist (Ki = 26 nM) displaying negligible blockade of α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). Found to be inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors (Ki = 930 nM). -
nAChR agonist
Varenicline is a nicotinic receptor partial agonist. -
dopamine transporter/norepinephrine transporters inhibitor
Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator. -
α7 nAChR agonist
Nelonicline (ABT-126) is a selective neuronal nicotinic receptor agonist. -
nAChR agnoist
Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits. -
nAChR agonist
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2 nAChRs (Ki=16 nM) and shows high selectivity for α6β2 and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [3H] cytisine sites is 16.7 nM.
- PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base. PNU-282987 is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.
-
α4β2 nicotinic acetylcholine receptor partial agonist
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation. -
α7 nAChR modulator
-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity. -
nAChR Inhibitor
EVP-6124 is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs); shows selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs. -
nAChR Inhibitor
EVP-6124 hydrochloride is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs). EVP-6124 showed selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs. -
α7 nAchR/JAK2/STAT3 Agonist
α7 nAchR-JAK2-STAT3 agonist 1 is a selective agonist targeting the α7 nicotinic acetylcholine receptor, modulating the JAK2-STAT3 signaling pathway. It demonstrates significant anti-inflammatory activity by inhibiting the expression of inducible nitric oxide synthase (iNOS), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6) in murine RAW264.7 macrophages, with an IC50 of 0.32 μM for nitric oxide production. Additionally, it effectively suppresses lipopolysaccharide (LPS)-induced nitric oxide release, NF-κB activation, and related cytokine production. This compound is valuable for studying sepsis and inflammatory responses. -
α7 nAChR Agonist
A-582941 is a selective α7 nicotinic acetylcholine receptor (nAChR) agonist that effectively crosses the blood-brain barrier. With Ki values of 10.8 nM in rat brain and 17 nM in human frontal cortex, it demonstrates significant biological activity by promoting ERK1/2 and CREB phosphorylation, inhibiting GSK-3β through Ser-9 phosphorylation, and enhancing acetylcholine release. Additionally, A-582941 induces the expression of activity-regulated cytoskeleton-associated protein (Arc) and c-Fos while activating brain regions linked to working memory and attention. This compound is valuable for investigating mechanisms involved in Alzheimer's disease and schizophrenia. -
Nicotine Metabolite
(±)-Nornicotine is a significant metabolite of nicotine, acting as a partial agonist of nicotinic acetylcholine receptors (nAChRs) that contain α7 and α6 subunits. This compound is known to disrupt β-catenin and ZO-1 interactions while inducing depolymerization of F-actin, contributing to its biological effects. (±)-Nornicotine has been implicated in research on various conditions, including atherosclerosis, Alzheimer's disease, and schizophrenia, making it a valuable tool for studies involving neural and vascular pathophysiology. -
Stable Isotope
(±)-Nornicotine-d4 is a deuterium-labeled analog of (±)-Nornicotine, a significant metabolite of nicotine. It acts as a partial agonist at nicotinic acetylcholine receptors (nAChRs), particularly those containing α7 and α6 subunits, influencing various biological pathways. This compound has been shown to disrupt β-catenin and ZO-1 interactions while inducing F-actin depolymerization. (±)-Nornicotine-d4 is valuable for research focused on atherosclerosis, Alzheimer's disease, and schizophrenia, providing insights into nicotine's metabolic effects and related neurological conditions. -
α7nAChR Activator
Lemairamin, an α7nAChR activator, is a hydroxylamine compound derived from the pericarps of Zanthoxylum species. This compound is known to stimulate the expression of anti-inflammatory cytokine IL-10 and proopiomelanocortin (POMC), while concurrently reducing Akt activity. Lemairamin has demonstrated efficacy in attenuating dextran sulfate sodium (DSS)-induced intestinal inflammation and alleviating pain hypersensitivity, making it a valuable reagent for research in inflammation and pain modulation. -
α4β2 nAChR Agonist
TC-2559 free base is an agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), demonstrating an EC50 value of 0.18 μM. It exhibits reduced potency on β4-containing nAChR subtypes, such as α2β4, α4β4, and α3β4, with EC50 values between 10-30 µM. Research indicates that TC-2559 enhances dopamine neuron activity in the ventral tegmental area, which may influence excitability and aggression. Additionally, it possesses anti-inflammatory effects via STAT3 inhibition, proving beneficial in models of mechanical allodynia and cognitive deficits. This compound is useful for investigations into nerve pain and related neurological conditions. -
Anti-Inflammatory Compound
Cynandione A is an acetophenone compound with anti-inflammatory properties. It has been shown to protect hepatocytes and cortical neurons from toxicity, as well as improve neurological deficits in a rat model of cerebral ischemia. Additionally, Cynandione A exerts significant anti-inflammatory effects through the activation of macrophage α7 nAChR and the expression of IL-10, making it a valuable tool for research in neuroprotection and inflammation. -
nAChR Antagonist
Mecamylamine is a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChR). It functions as a ganglionic blocker and is capable of crossing the blood-brain barrier. Mecamylamine is utilized in research focused on neuropsychiatric disorders, hypertension, and the development of antidepressant therapies. -
nAChR Inhibitor
Meclofenoxate, a nAChR inhibitor, is an ester derived from dimethylaminoethanol (DMAE) and para-chlorophenylalanine (pCPA). It is known for its potential to enhance memory and cognitive function. Meclofenoxate is commonly utilized in neurological research to investigate mechanisms underlying cognitive enhancement and memory improvement. -
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.
