Catalog No.
Product Name
Application
Product Information
Citations
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Nicotinic (α7) Receptor Modulator
PNU-120596 is a positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors.- Hugo R Arias, .et al. , Br J Pharmacol, 2022, Sep 9 PMID: 36082615
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nAChR agonist
GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation.- P Yamini, .et al. , Pharmacol Biochem Behav, 2022, Jun;217:173402 PMID: 35533773
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α7 Positive Modulator
NS 1738 is a α7 positive allosteric modulator.- Spencer R. Pierce, .et al. , Biomolecules, 2023, 13(4), 698 PMID: 37189445
- Hugo R Arias, .et al. , Br J Pharmacol, 2022, Sep 9 PMID: 36082615
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α7 nAChR agonist
PNU 282987 (PNU-282,987)is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors.- Thorsang Weerakul, .et al. , ACS Pharmacol Transl Sci, 2026, 9 (1): 45-58 PMID: 41536290
- Pyrantel pamoate is a deworming agent in the treatment of hookworms (all species) and roundworms in domesticated animal; acts as a depolarizing neuromuscular blocking agent.
- Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
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nAChR antagonist
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.
- COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM.
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Nicotinic α7 Positive Allosteric Modulator
RGH-857 acts as a selective and potent positive allosteric modulator of nicotinic α7 receptors. It demonstrates effectiveness in ameliorating amnesia and is valuable in studies related to Alzheimer's disease. This compound can facilitate research into cognitive impairment and potential therapeutic interventions in neurodegenerative disorders. -
FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
Apoptosis Inducer
Crebanine is an isoquinoline-like alkaloid that acts as an apoptosis inducer through antagonism of the α7-nAChR, exhibiting an IC50 value of 19.1 μM. This compound suppresses cancer cell proliferation, migration, and invasion while triggering a reactive oxygen species (ROS) burst that promotes apoptosis. Additionally, Crebanine modulates critical signaling pathways including AKT/FoxO3a, NF-κB, and MAPK, and demonstrates antioxidant properties in microglia by reducing ROS and lipid peroxidation. With applications in studying hepatocellular carcinoma, cerebral ischemia, and Alzheimer's disease, Crebanine may also ameliorate cognitive deficits and ischemia-reperfusion brain damage in rodent models. -
α7 nAChR Agonist/5-HT3 antagonist
(S)-PNU-282987 hydrochloride is a potent agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 of 154 nM. In addition, it acts as a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. This compound is valuable for research applications exploring the central and peripheral nervous systems, facilitating the study of neurotransmission and signaling pathways involving cholinergic and serotonergic systems. -
nAChR Agonist
Facinicline (RG3487) is an orally active partial agonist of the nicotinic α7 receptor, exhibiting a Ki of 6 nM for human nAChR. This compound has been shown to enhance cognitive function and sensorimotor gating in rodent models, providing a valuable tool for research into cognitive disorders. Additionally, Facinicline hydrochloride demonstrates high affinity as an antagonist at 5-HT3 receptors with a Ki value of 1.2 nM, further broadening its potential applications in neuroscience research. -
α7-nAChR Agonist
GTS-21 is a selective agonist of the alpha7 nicotinic acetylcholine receptor (α7-nAChR), known for its anti-inflammatory and cognitive-enhancing properties. Additionally, GTS-21 exhibits antagonistic activity at the α4β2 receptor (Ki=20 nM) and the 5-HT3A receptor (IC50=3.1 μM). This compound is utilized in research related to age-associated memory impairment (AAMI) and Alzheimer's disease, making it a valuable tool for investigating cognitive dysfunction and neuroinflammatory processes. -
Apoptosis Inhibitior
(S)-Oxiracetam is an apoptosis inhibitor that targets the PI3K/Akt/GSK3β signaling pathway via α7 nAChR activation. It has demonstrated efficacy in reducing brain infarct size and alleviating neurological dysfunction in middle cerebral artery occlusion/reperfusion (MCAO/R) models. This compound effectively prevents neuronal apoptosis, making it a valuable research tool for studies focused on ischemic stroke and neuroprotection. -
Histone Methyltransferase
Lobelane hydrochloride selectively inhibits the vesicular monoamine transporter-2 (VMAT2). This compound demonstrates an affinity for VMAT2 with a K(i) value of 630 nM, while exhibiting low interaction with nicotinic acetylcholine receptors (nAChR). The unique mechanism of action of lobelane hydrochloride makes it a valuable tool for studying neurotransmitter dynamics and offers potential in the development of therapeutic agents aimed at addressing methamphetamine abuse. Its structural analogs may further expand its applications in neuropharmacological research. -
nAChR Agonist
Facinicline hydrochloride is a selective partial agonist of the nicotinic α7 acetylcholine receptor (nAChR), exhibiting a Ki of 6 nM. This compound has demonstrated potential in enhancing cognitive function and sensorimotor gating in rodent models, making it a valuable tool for research on cognitive disorders. Additionally, Facinicline hydrochloride shows high affinity as an antagonist at the 5-HT3 receptor, with a Ki of 1.2 nM, widening its applicability in neurological and psychiatric research. -
α7 nAChR Agonist
NS-6740 is a partial agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR), exhibiting an IC50 of 3 nM. This compound functions as a potent modulator of the cholinergic anti-inflammatory pathway, influencing α7 signaling in an ion channel-independent manner, which ultimately reduces synaptic function. NS-6740 promotes the desensitized state of α7 nAChR and elicits substantial nAChR-mediated currents. It is effective in decreasing LPS-induced TNF-α release from microglia, making it a valuable tool for research into neuroinflammation and neuropathic pain mechanisms. -
α7 Nicotinic Acetylcholine Receptor Inhibitor
NS-6740 hydrochloride is a potent partial agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR), exhibiting an IC50 of 3 nM. It functions as a modulator of the cholinergic anti-inflammatory pathway and alters α7 signaling in an ion channel-independent manner, which diminishes synaptic function and promotes receptor desensitization. NS-6740 hydrochloride has been shown to significantly reduce LPS-induced TNF-α release from microglia, making it a valuable tool in the study of neuroinflammation and neuropathic pain mechanisms. -
RVG Peptide
RVG (RVG29) is a peptide derived from Rabies Virus Glycoprotein that specifically binds to the α-7 subunit of nicotinic acetylcholine receptors (nAChRs) on neuronal cells. This interaction facilitates the enhanced delivery of Mycobacterium tuberculosis antigens to antigen-presenting cells, making RVG valuable for immunological research and vaccine development studies targeting tuberculosis. -
nAChR Agonist
Pyrantel is an orally active anthelmintic that functions as an agonist of the nicotinic acetylcholine receptor (nAChR). It induces spasmodic muscle paralysis in parasitic organisms, making it effective in the eradication of a variety of helminthic infections. Pyrantel is commonly utilized in the study and treatment of conditions such as ascariasis, hookworm infections, pinworm infections, and trichinosis, providing critical research insights into parasitic diseases. -
nAChR Aagonist
Simpinicline (OC-02) is a highly selective agonist of the nicotinic acetylcholine receptor (nAChR). This compound exhibits potent antiviral activity against SARS-CoV-2 variants in cell culture, with an IC50 value of 0.04 µM. Its unique selectivity and efficacy make it a valuable tool for research in virology and neuropharmacology. -
Anthelmintic Agent/Immunoregulatory Agent
Levamisole is an anthelmintic agent recognized for its immunoregulatory properties. This compound functions as a positive allosteric modulator of the α3β2 (EC50 = 300 μM) and α3β4 (EC50 = 100 μM) subtypes of nicotinic acetylcholine receptors (nAChRs), enhancing receptor activity. It is orally active and is commonly used in research applications related to parasitic infections and immune response modulation. -
Nicotinic acetylcholine receptors Inhibitor
Dinotefuran is a competitive inhibitor targeting insect nicotinic acetylcholine receptors (nAChRs). This compound effectively disrupts neural signaling in insects, leading to dysfunction. With an IC50 of 890 nM for [3H]epibatidine and 36.1 μM for [3H]α-bungarotoxin in American cockroach neural membranes, Dinotefuran demonstrates significant knockdown (KD50=0.351 nmol/g) and lethal activity (LD50=0.173 nmol/g) against German cockroach. Its primary applications include agricultural pest control, specifically targeting piercing-sucking and chewing insects like aphids and planthoppers, and it also serves as a tool for studying environmental toxicological impacts such as oxidative stress and reproductive neurotoxicity in earthworms. -
nAChR Antagonist
Derquantel is a spirocyclic anthelmintic that functions as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs). It inhibits acetylcholine-induced depolarization with an IC50 of 0.22 μM, leading to flaccid paralysis of nematode somatic muscles. This mechanism effectively dislodges parasites from the host gastrointestinal tract, making Derquantel a valuable tool in research related to Haemonchus contortus and Ascaris suum infections. -
nAChR Modulator
GSK575594A is an allosteric modulator of the nicotinic acetylcholine receptor (nAChR) in Ascaris suum. This compound enhances muscle contractions triggered by acetylcholine (ACh) by binding to the allosteric site within the transmembrane domain of the nAChR, leading to a significant increase in contraction amplitude (Emax from 1.19 g to 1.51 g) at a concentration of 3 μM. GSK575594A is applicable in antiparasitic research, providing insights into neuromuscular mechanisms in parasitic infections. -
Pesticide
(S)-Dinotefuran is a neonicotinoid pesticide that primarily targets the α8 subunit of nicotinic acetylcholine receptors (nAChRs) in honeybees, Apis mellifera. It exhibits higher toxicity compared to its R-enantiomer, R-dinotefuran, affecting the survival and behavior of these important pollinators. This compound is utilized in ecological and toxicological research to study the impact of pesticides on non-target species and to evaluate the risks associated with neonicotinoid exposure in agricultural settings. -
Insecticide
Thiacloprid is an orally active neurotoxic insecticide that functions as an agonist of nicotinic acetylcholine receptors (nAChR). It has been shown to reduce cellular viability, deplete reduced glutathione, and elevate malondialdehyde (MDA) levels, leading to cytotoxicity and oxidative stress. While Thiacloprid exhibits lower acute toxicity to honeybees compared to some other insecticides, it adversely affects their learning, memory, immune function, and overall survival. Additionally, this compound disrupts intestinal microbiota, increasing the risk of premature colony collapse in bumblebees. Thiacloprid is utilized in the broad-spectrum control of agricultural pests across various crops, including potatoes, cabbages, fruits, vegetables, and nuts. -
α7 nAChR Inhibitor
Conofurin-Delta is a potent inhibitor of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an IC50 of 177 nM. Additionally, it demonstrates inhibitory activity against the α9α10 nAChR with an IC50 of 98.1 nM. This compound is relevant for research applications in the study of SARS-CoV-2 infection and its impact on cholinergic signaling pathways. - Methyllycaconitine citrate is a potent antagonist for α7-containing neuronal nicotinic receptors (Ki = 1.4 nM). Interacts with α4β2 and α6β2 receptors at concentrations > 40 nM.
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neuronal nicotinic receptor agonist
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM). -
nAChR agonist
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does. -
AChR inhibitor
Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug -
neuromuscular blocking agent
Cisatracurium besylate (51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission. -
nAChR agonist
(±)-Epibatidine is a nicotinic agonist. (±)-Epibatidine is a neuronal nAChR agonist. -
α7 nAChR agonist
A-582941 dihydrochloride is a selective AChR a7 partial agonist. It exhibits high affinity for both rat and human a7 receptors (Ki values are 10.8 and 16.7 nM, respectively).
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nAChR agonist
5-Iodo-A-85380 2HCl is a highly potent and subtype-selective agonist for the a4b2 and a6b2 nicotinic acetylcholine receptors. -
nAChR inhibitor
Benzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively. -
microtubule dynamics inhibitor
Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. -
nAChR agonist
ABT-418 HCl is a neuronal nicotinic acetylcholine receptor agonist. -
nAChR agonist
Sofinicline is a novel nicotinic acetylcholine receptor agonist in the treatment of attention-deficit/hyperactivity disorder. -
nAChR agonist
Ispronicline is a neuronal nicotinic acetylcholine receptor partial agonist. Ispronicline is subtype-selective, binding primarily to the a4b2 subtype. It has antidepressant, nootropic and neuroprotective effects. -
5-HT3 receptor antagonist
Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ?? 0.9 nM for 5-HT3 receptor. -
nAChR Agonist
Desformylflustrabromine HCl is a positive allosteric modulator of α4β2 and also a muscle-type nAChR inhibitor. -
nAChR agonist
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
