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
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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. -
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.
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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 -
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.
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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. - 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.
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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. - 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.
