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Nicotinic acetylcholine receptor (nAChR) agonists, antagonists and modulators act on ligand-gated cation channels. Each receptor is a pentamer of subunits arranged around a central pore that opens when acetylcholine binds. A refined structure of the Torpedo receptor at 4 Å resolution, published in 2005, resolved its ligand-binding, membrane and cytoplasmic regions. Muscle-type receptors mediate neuromuscular transmission, while neuronal subtypes such as α7 and α4β2 are studied in attention, memory and nicotine dependence. Agonists include PNU 282987, which is selective for α7, and the partial agonist varenicline. PNU-120596, described in 2005, is a positive allosteric modulator of α7 that enhances acetylcholine-evoked currents. Vecuronium bromide, a neuromuscular blocking agent, acts on the muscle-type receptor.
Synonyms: NSC-213859
NS 1738 is a α7 positive allosteric modulator.
PNU-120596 is a positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors.
Synonyms: Chantix
Varenicline is a nicotinic receptor partial agonist.
A-867744 is a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
Synonyms: CP 526555-18
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.
Synonyms: methyl 1,2,5,6-tetrahydro-1-methyl-3-pyridinecarboxylate hydrobromide
Arecoline hydrobromide is a partial agonist of nicotinic (nAChR) and muscarinic acetylcholine receptors (mAChR). This naturally occurring psychoactive alkaloid possesses brain-penetrant properties and is known for its stimulation, alertness enhancement, anxiolytic effects, and anti-parasitic activity. Additionally, Arecoline hydrobromide can induce oxidative stress, making it valuable for research in neuropharmacology and related fields.
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).
Synonyms: CC4
Thermopsidine is a selective partial agonist of the α4β2 and α6β2 nicotinic acetylcholine receptors (nAChRs), exhibiting an EC50 value of 2.2 μM for the α4β2 subtype. This compound is valuable for studying cholinergic signaling pathways and exploring potential therapeutic avenues in neurodegenerative diseases and addiction research. Its specific targeting of nAChRs makes it a useful tool for evaluating receptor function and pharmacology.
Synonyms: TC-1734; AZD-3480
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.
Synonyms: Encenicline
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.
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.
Synonyms: dFBr hydrochloride
Desformylflustrabromine HCl is a positive allosteric modulator of α4β2 and also a muscle-type nAChR inhibitor.
BNC375 is a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of α7 nAChRs.
Synonyms: B-973B
-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity.
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation.
Synonyms: AAD1566
Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
Synonyms: ABT-089
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.
Synonyms: IACS10759
CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs.
Synonyms: CP 526555 hydrochloride; CP-526555
Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist.
Synonyms: Ebanicline hydrochloride; ABT-594 hydrochloride; ABT 594
Tebanicline hydrochloride (ABT594 hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity.
Synonyms: Varenicline 2HCl; HSDB7591; CP 526555
Varenicline is a nicotinic receptor partial agonist.
BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.
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.
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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.
Synonyms: RG3487 free base
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.
