α7 nAchR-JAK2-STAT3 agonist 1 is a potent inhibitor of the α7 nAchR-JAK2-STAT3 pathway that acts on nitric oxide (NO) (IC50: 0.32 μM). α7 nAchR-JAK2-STAT3 agonist 1 has been shown to have a positive effect on iNOS, IL-1β and IL-1β in murine macrophages RAW264.7. α7 nAchR-JAK2-STAT3 agonist 1 was effective in inhibiting the expression of iNOS, IL-1β and IL-6 in mouse macrophages. α7 nAchR-JAK2-STAT3 agonist 1 inhibited LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 agonist 1 was able to be used to study sepsis.

Pozanicline hydrochloride is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [3H]cytisine sites[1]. Pozanicline hydrochloride is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant[2].

Cynandione A, an acetophenone derived from Cynanchum wilfordii, has anti-inflammatory activity and significantly reduces pro-inflammatory cytokine overexpression via macrophage α7 nAChR activation and subsequent IL-10 expression.

PHA 543613 is a specific agonist of α7 nAChR (Ki = 8.8 nM) and can be used in studies about the cognitive deficits of Alzheimer's disease and schizophrenia.

SSR180711 hydrochloride (SSR-180711A HCl) is a selective Alpha7 nicotinic acetylcholine partial agonist for the study of neurodegenerative and cognitive disorders.

SEN12333 is an α7 nicotinic acetylcholine receptor (nAChR) agonist

High affinity α7 nAChR partial agonist (Ki = 1.1 nM in rat; Emax < 10% of the response to ACh in rat and human). Inhibits ACh (IC50 = 2.7 nM) at α7 nAChR. Reduces LPS-induced TNF-α release from microglia enriched cultures. Anti-inflammatory. Briggs et al (2009) Role of channel activation in cognitive enhancement mediated by α7 nicotinic acetylcholine receptors. Br.J.Pharmacol. 158 1486 PMID:19845675 |Thomsen et al (2012) The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS6740 and GTS-21 reduce lipopolysaccharide-induced TNF-α release from microglia. J.Neuroimmunol. 251 65 PMID:22884467 |Papke et al (2015) The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor. Neuropharmacology 91 34 PMID:25497451

A-867744 is an effective and selective type II positive allosteric modulator of the α7 nAChR (EC50: 1.0 μM).

PNU-282987 S enantiomer free base is an agonist of α7 nicotinic acetylcholine receptor (α7 nAChR).

(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium. It is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes

nAChR agonist 1 (DUN71755) is a brain-permeable and orally efficacious positive allosteric α7 nicotinic acetylcholine receptor (α7 nAChR)modulator.

A-582941 dihydrochloride (A 582941) is a Selective agonist of α7 nAChR partial

BNC210 (IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.

Aspergillimide is a fungal metabolite originally isolated from A. japonicus.1 It reduces nicotinic acetylcholine receptor (nAChR) peak and slowly-desensitizing amplitudes induced by acetylcholine in silkworm (B. mori) larval neurons (IC50s = 20.2 and 39.6 nM, respectively) but has no effect on chicken α3β4-, α4β2-, and α7-containing nAChRs.2 Dietary administration of aspergillimide A (10 μg/g of diet) induces paralysis in silkworm fourth instar larvae.1 Aspergillimide A (10 and 20 mg/kg) reduces T. colubriformis fecal egg count in gerbils.3References1. Hayashi, H., Nishimoto, Y., Akiyama, K., et al. New paralytic alkaloids, asperparalines A, B and C, from Aspergillus japonicus JV-23. Biosci. Biotechnol. Biochem. 64(1), 111-115 (2000).2. Hirata, K., Kataoka, S., Furutani, S., et al. A fungal metabolite asperparaline a strongly and selectively blocks insect nicotinic acetylcholine receptors: The first report on the mode of action. PLoS One 6(4), e18354 (2011).3. Banks, R.M., Blanchflower, S.E., Everett, J.R., et al. Novel anthelmintic metabolites from an Aspergillus species; the aspergillimides. J. Antibiot. (Tokyo) 50(10), 840-846 (1997). Aspergillimide is a fungal metabolite originally isolated from A. japonicus.1 It reduces nicotinic acetylcholine receptor (nAChR) peak and slowly-desensitizing amplitudes induced by acetylcholine in silkworm (B. mori) larval neurons (IC50s = 20.2 and 39.6 nM, respectively) but has no effect on chicken α3β4-, α4β2-, and α7-containing nAChRs.2 Dietary administration of aspergillimide A (10 μg/g of diet) induces paralysis in silkworm fourth instar larvae.1 Aspergillimide A (10 and 20 mg/kg) reduces T. colubriformis fecal egg count in gerbils.3 References1. Hayashi, H., Nishimoto, Y., Akiyama, K., et al. New paralytic alkaloids, asperparalines A, B and C, from Aspergillus japonicus JV-23. Biosci. Biotechnol. Biochem. 64(1), 111-115 (2000).2. Hirata, K., Kataoka, S., Furutani, S., et al. A fungal metabolite asperparaline a strongly and selectively blocks insect nicotinic acetylcholine receptors: The first report on the mode of action. PLoS One 6(4), e18354 (2011).3. Banks, R.M., Blanchflower, S.E., Everett, J.R., et al. Novel anthelmintic metabolites from an Aspergillus species; the aspergillimides. J. Antibiot. (Tokyo) 50(10), 840-846 (1997).

4BP-TQS is an allosteric agonist of α7 nAChRs.

Ultrapotent PSEM (uPSEM) agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki = 0.7 nM for PSAM4-GlyR and <10 nM for PSAM4-5HT3). Exhibits >10,000-fold agonist selectivity for PSAM4-GlyR over α7-GlyR, α7-5HT3, and 5HT3-R, and 230-fold selectivity over α4β2 nAChR. Also weak partial agonist (~10 %) at α4β2 nAChR. Retains the potency of varenicline (Cat.No. 3754) for PSAM4-GlyR with enhanced chemogenetic selectivity. Does not act as a substrate for P-glycoprotein pumps. Silences neurons in vivo. Brain-penetrant. Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science doi: 10.1126/science PMID:30872534

α-Conotoxin ImI is a conotoxin that has been found inC. imperialisand has receptor antagonist and anticancer activities.1It is a peptide antagonist of homomeric α7 nicotinic acetylcholine receptors (nAChRs; IC50= 220 nM). α-Conotoxin ImI is selective for α7 nAChRs over α2β2, α3β2, α4β2, α2β4, α3β4, α4β4, and α1β1γδ subunit-containing nAChRs at 5 μM but does inhibit homomeric α9 nAChRs (IC50= 1,800 nM). Administration of paclitaxel in micelles containing α-conotoxin ImI decreases tumor growth in an MCF-7 mouse xenograft model.2Intracerebroventricular, but not intraperitoneal, administration of α-conotoxin ImI (20 nmol/animal) induces seizures in rats.3 1.Johnson, D.S., Martinez, J., Elgoyhen, A.B., et al.α-Conotoxin ImI exhibits subtype-specific nicotinic acetylcholine receptor blockade: Preferential inhibition of homomeric α7 and α9 receptorsMol. Pharmacol.48(2)194-199(1995) 2.Mei, D., Lin, Z., Fu, J., et al.The use of α-conotoxin ImI to actualize the targeted delivery of paclitaxel micelles to α7 nAChR-overexpressing breast cancerBiomaterials4252-65(2015) 3.McIntosh, J.M., Yoshikami, D., Mahe, E., et al.A nicotinic acetylcholine receptor ligand of unique specificity, α-conotoxin ImIJ. Biol. Chem.269(24)16733-16739(1994)

Rivanicline hemioxalate, also known as RJR-2403 hemioxalate or (E)-Metanicotine hemioxalate, is a chemical compound acting as a neuronal nicotinic receptor agonist with pronounced selectivity for the α4β2 receptor subtype, showing over 1,000-fold greater selectivity for this subtype (Ki=26 nM) compared to α7 receptors (Ki=3.6 μM). Its in vitro studies demonstrate no significant activation of nAChRs in PC12 cells, muscle type nAChRs, or muscarinic receptors at concentrations up to 1 mM. Furthermore, Rivanicline displayed less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy, and failed to antagonize nicotine-induced stimulation of muscle or ganglionic nAChR functions, with an IC50 value greater than 1 mM. Chronic exposure to Rivanicline at 10 microM led to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine. In vivo studies revealed that Rivanicline significantly reversed scopolamine-induced amnesia and improved working and reference memory in a rat model, while being 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses. Metanicitone’s potency was approximately five times lower than nicotine in tail-flick tests following subcutaneous administration, yet slightly more potent upon central administration.

D-Amphetamine sulfate, a central nervous system (CNS) stimulant, acts on monoamine transporters to increase noradrenaline, dopamine, and serotonin levels in synapses. Additionally, it serves as an antagonist to the α7 nicotinic acetylcholine receptor (nAChR).

Azemiopsin, a potent inhibitor of the nicotinic acetylcholine receptor (nAChR), demonstrates half maximal inhibitory concentrations (IC50s) of 0.18 μM for T. californica nAChR and 22 μM for human α7 nAChR. Moreover, it effectively blocks acetylcholine-induced currents in Xenopus oocytes that heterologously express human muscle-type nAChR [1].

CCMI (AVL-3288) is a potent and selective modulator of α7 nAChR-positive allosteric.

Asoxime dichloride (Tert-Butyl2-(2-hydroxyethyl)-1-pyrrolidinecarboxylate) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system. Asoxime dichloride involves in modulating immunity response.

neuronal α7 nAChR antagonist

PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).

NS 1738 (NSC-213859) is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nAChRs)

(S)-UFR2709 is a competitive antagonist of the nicotinic acetylcholine receptor (nAChR), exhibiting a greater affinity for α4β2 nAChRs compared to α7 nAChRs. It effectively reduces anxiety and ethanol consumption, as well as ethanol preference, in alcohol-preferring rats. Additionally, (S)-UFR2709 functions as an anxiolytic agent and holds the potential for investigating nicotine addiction.

BMS-933043 is a Selective α7 nAChR partial agonist. BMS-933043 showed potent binding affinity to native rat (Ki = 3.3 nM) and recombinant human alpha7 nicotinic acetylcholine receptors (Ki = 8.1 nM). BMS-933043 shows agonist activity in a calcium fluoresc

High affinity and subtype selective α6β2 and α4β2 partial agonist (Ki values are 12 and 26nM for rat α6β2 and α4β2 receptors respectively). Has low affinity for α3β4 and α7 receptors (Ki values are 4.8 and 13 μM for human α3β4 and rat α7 receptors respectively). Stimulates dopamine release from striatal slices in vitro. Attenuates nicotine-induced self-administration and conditional place preference in rats. Sala et al (2013) CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking c Br.J.Pharmacol. 168 835 PMID:22957729 |Riganti et al (2005) Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells. Br.J.Pharmacol. 146 1096 PMID:16273122 |Carbonnelle et al (2003) Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes. Eur.J.Pharmacol. 471 85 PMID:12818695

nAChR antagonist 1 (compound B15) is a highly effective antagonist of α7 nAChR, demonstrating an IC50 value of 3.3 μM. Its versatility makes it an ideal candidate for investigating the pathogenesis of schizophrenia, Alzheimer's disease, and inflammatory disorders [1].

Benzethonium chloride (Quatrachlor) is a synthetic quaternary ammonium salt with surfactant, antiseptic, and broad spectrum antimicrobial properties.

AQW051 (VQW-765) is an orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) specific activator that interacts with recombinant human α7-nAChR expression (pKD value 7.56). Alpha7-nachr is considered an attractive target for the treatment of cognitive impairments associated with neurological disorders, so VQW-051 is often used in studies of anxiety disorders and acute anxiety.

AR-R17779 hydrochloride is a potent, selective full agonist of the nAChR, demonstrating K i values of 92 nM for the α7 subtype and 16,000 nM for the α4β2 subtype. It is noted for its ability to enhance learning and memory in rats, suggesting potential therapeutic applications. Additionally, this compound exhibits anxiolytic properties and can mitigate inflammation by activating anti-inflammatory cholinergic (vagal) pathways [1] [2] [4].

α-Conotoxin MrIC is a biased agonist selective for the α7 nicotinic acetylcholine receptor (nAChR), with activation contingent upon the presence of type II positive allosteric modulators, such as PNU120596. It is utilized to investigate neurological disorders and delineate the pharmacological characteristics of the α7nAChR [1].

(S)-VQW-765 ((S)-AQW-051) is an orally active, selective, and effective partial agonist of the α7 nicotinic acetylcholine receptor (nAChR), with potential applications in treating cognitive disorders associated with neurological diseases, including Alzheimer's disease and schizophrenia.

α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, holds promise for neurological research, particularly in studying neuropathic pain and Alzheimer's disease [1].

Facinicline hydrochloride (RG3487) is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM). Facinicline hydrochloride improves cognition and sensorimotor gating in rodents.

S 24795 (Catestatin acetate(142211-96-9 free base)) is an α7 nAChR partial agonist. S 24795 improves mnemonic function in aged mice and can be used in studies about aging-related memory disturbances.

Tropisetron (ICS 205-930) is an α7-nicotinic receptor agonist and 5-HT3 receptor antagonist with Kis of 6.9 nM and 5.3 nM, respectively.

(S)-UFR2709 hydrochloride ((S)-UFR2709 HCl) is a selective and potent nAChR antagonist with anxiolytic activity, inhibits α4β2 nAChR and α7 nAChR, and can be used to study nicotine addiction.

(-)-(S)-B-973B is an effective allosteric agonist and a positive allosteric modulator of α7 nAChR.

T761-0184 is a potent antagonist of α7 nicotinic receptor (nAChR) [1].

PNU-282987 free base is a selective and potent α7 nicotinic acetylcholine receptor (nAChR) agonist and 5-HT3 receptor antagonist with anti-inflammatory activity.PNU-282987 free base protects against sepsis-induced acute lung injury in mice, attenuates activation of ILC2s and Streptozotocin-induced airway inflammation.PNU-282987 free base is used in the study of neurological diseases.

TC-2216 is a partial agonist at the neural nicotinic acetylcholine receptor and is used to treat anxiety and depression.

Varenicline (CP 526555), a cytisine-based nicotinic ligand, is a potent partial agonist for the α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM and acts as a full agonist for α7 and α3β4 nAChRs, with respective EC50 values of 18 μM and 55 μM [1]. Notably, its effectiveness and potential in smoking cessation treatments are underscored by its pharmacological profile [2].

DPNB-ABT594, a nitrobenzyl-caged ABT594, selectively activates nAChRs containing α4β2 subunits over the α7 subunit. It is utilized to map the distribution of nAChRs on medial habenula (MHb) neurons, thereby facilitating a deeper understanding of nAChR-mediated Ca2+ signaling in the MHb [1].

α-Conotoxin GID is a paralytic peptide neurotoxin that selectively antagonizes nAChR with IC50 values of 5 nM (α7), 3 nM (α3β2), and 150 nM (α4β2). It is a small, disulfide-rich peptide with the potential for chronic pain inhibition. The presence of a C-terminal carboxylate in α-Conotoxin GID is crucial, as its substitution with a C-terminal carboxamide results in a loss of activity against α4β2 nAChR. This compound is derived from species of the genus Conus [1] [2] [3].

GTS-21 (DMXB-A) is an α7 nAChR agonist. GTS-21 suppresses inflammation associated with rheumatoid arthritis by inhibiting RA Th1 cell differentiation.

IND8 is a selective and potent α7-nAChR agonist.

Bradanicline is a potent and highly selective agonist of the α7 nicotinic acetylcholine receptor (nAChR) with an EC50 of 17 nM and a Ki of 1.4 nM for the human α7 nAChR. It is primarily employed in research pertaining to cognitive disorders [1] [2].

PNU-120596 (NSC-216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.