nAChR Agonist

Hydroxy varenicline (2-Hydroxyvarenicline) is a metabolite of varenicline (HY-10019), a nicotinic acetylcholine receptor (nAChR) agonist.

3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak α4β2 nAChR partial agonist that has been studied as an antidepressant.

Sofinicline benzenesulfonate (ABT 894 benzenesulfonate) is a novel nicotinic acetylcholine receptor agonist, specifically acting on the α4β2 subtype of nAChR (IC₅₀=0.1 nM). Sofinicline benzenesulfonate has the potential to improve cognitive function, including attention, memory and working memory. Sofinicline benzenesulfonate can be used in studies of attention deficit, hyperactivity disorder (ADHD).

Desformylflustrabromine hydrochloride (Standard) is the analytical standard of Desformylflustrabromine hydrochloride (HY-107675). This product is intended for research and analytical applications. Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC₅₀ of 6.48.

4BP-TQS (Standard) is the analytical standard of 4BP-TQS (HY-110087). This product is intended for research and analytical applications. 4BP-TQS is a potent allosteric agonist of α7 nAChR. 4BP-TQS activates nAChRs via an allosteric transmembrane site.

Varenicline (Standard) is the analytical standard of Varenicline. This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.

Facinicline (RG3487) is an orally active nicotinic α7 receptor partial agonist, with a K_i of 6 nM for α7 human nAChR. Facinicline improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride shows high affinity (antagonist) to 5-HT₃Rs with a K_i value of 1.2 nM.

Varenicline-¹³C¹⁵N (CP 526555-¹³C¹⁵N) is ¹³C and ¹⁵N labeled Varenicline. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.

DBO-83 free base is a brain-penetrant nicotinic acetylcholine receptor (nAChR) agonist. DBO-83 free base activates peripheral nicotinic acetylcholine receptors to evoke non-stimulated ileum contractions. DBO-83 free base shows antinociceptive and anti-amnesic activities.

SEN12333 (Standard) is the analytical standard of SEN12333 (HY-107678). This product is intended for research and analytical applications. SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca2+ flux studies (EC₅₀=1.6 μM). SEN 12333 is used for AD and schizophrenia research.

Pozanicline dihydrochloride (Standard) is the analytical standard of Pozanicline (dihydrochloride) (HY-110160). This product is intended for research and analytical applications. Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a K_i of 16.7 nM for binding to [3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a K_i of 17 nM while binding to α7 nAChR is insignificant.

ABT-418 hydrochloride (Standard) is the analytical standard of ABT-418 hydrochloride (HY-105170B). This product is intended for research and analytical applications. ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease.

Varenicline (dihydrochloride) (Standard) is the analytical standard of Varenicline (dihydrochloride). This product is intended for research and analytical applications. Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.

(S)-PNU-282987 hydrochloride is an isoform of PNU-282987 (HY-12560). PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC₅₀ of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT₃ receptor with an IC₅₀ of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems.

Varenicline (Hydrochloride) (Standard) is the analytical standard of Varenicline (Hydrochloride). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.

TC-1698 dihydrochloride is a selective α7 nicotinic acetylcholine receptors agonist with EC₅₀ value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 dihydrochloride improves memory and has neuroprotective effects. TC-1698 dihydrochloride can be used for Alzheimer's disease research.

Dianicline dihydrochloride (Standard) is the analytical standard of Dianicline (dihydrochloride) (HY-110241). This product is intended for research and analytical applications. Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoK_ing cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner.

NS3861 fumarate (Standard) is the analytical standard of NS3861 (fumarate) (HY-110121). This product is intended for research and analytical applications. NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding K_i values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.

TC-1698 is a selective α7 nicotinic acetylcholine receptors agonist with EC₅₀ value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 improves memory and has neuroprotective effects. TC-1698 can be used for Alzheimer's disease research.

TC-2216 is a compound with antidepressant and anxiolytic activity that has shown activity in multiple animal models and may exert its effects by acting on α4β2 neuronal nicotinic receptors.