nAChR Agonist

VQW-765 (AQW-051) is a selective and orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) agonist with a pK_D value of 7.56 to recombinantly expressed human α7-nAChR. VQW-765 shows anxiolytic-like effect in vivo. VQW-765 can be used for the research of anxiety disorder and acute performance anxiety.

GAT2711 is a full agonist of α9 nAChR with an EC₅₀ of 230 nM. GAT2711 shows 340-fold selective for α9 over α7 nAChRs. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells. GAT2711 retains full analgesic activity in α7 nAChR knockout mice.

SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (K_i=22 nM; IC₅₀=30 nM) and human α7 n-AChR (K_i=14 nM; IC₅₀=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.

Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc.

(Rac)-Monepantel-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile.

(-)-(S)-B-973B is an allosteric activator of α7 nicotinic acetylcholine receptor (α7 nAChR). (-)-(S)-B-973B alleviates pain behaviors. (-)-(S)-B-973B can be used for the research of inflammatory pain.

AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with K_i of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP⁺. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB).

(±)-Coniine hydrochloride (2-Propylpiperidine hydrochloride) is a potent nAChR agonist with an EC₅₀ value of 0.3 mM. (±)-Coniine hydrochloride shows acute toxicity with an LD₅₀ value of 7.7 mg/kg.

Pyrantel pamoate (Standard) (Pyrantel embonate (Standard)) is the analytical standard of Pyrantel pamoate (HY-12640). This product is intended for research and analytical applications. Pyrantel pamoate is an orally active antiparasitic agent. Pyrantel pamoate induces spastic paralysis in parasites via actions on neural and muscular cholinergic receptors as a nicotinic acetylcholine receptor (nAChR) agonist. Pyrantel pamoate eliminates both immature and mature endoparasites in horses. Pyrantel pamoate can be used in research related to parasitic infections.

Decamethonium Bromide is an acetylcholine receptor inhibitor and muscle relaxant. Decamethonium Bromide first induces depolarization of skeletal muscles, and then binds to postsynaptic acetylcholine receptors to induce persistent paralysis.\n

A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with K_i values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a K_i of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia.

PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.

TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC₅₀=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC₅₀s in the range of 10-30 µM. Antinociceptive effect.

Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner.

Bradanicline (TC-5619) is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough.

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 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the research of aging-related memory disturbances.

SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC₅₀ of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA).

Tribendimidine is an orally active, broad-spectrum anthelmintic agent, with particularly high activity against A. lumbricoides and N. americanus. Tribendimidine is also an L-type nicotinic acetylcholine receptor (nAChR) agonist.