nAChR Agonist

Pyrantel hydrochloride is an orally active antiparasitic agent. Pyrantel hydrochloride induces spastic paralysis in parasites via actions on neural and muscular cholinergic receptors as a nicotinic acetylcholine receptor (nAChR) agonist. Pyrantel hydrochloride eliminates both immature and mature endoparasites in horses. Pyrantel hydrochloride can be used in research related to parasitic infections.

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

Succinylcholine iodide (Suxamethonium iodide) is a depolarizing neuromuscular blocker with rapid onset and short duration of action. Succinylcholine iodide also acts as an agonist of the Acetylcholine receptor. Succinylcholine iodide is used for emergency airway management.

Galanthamine-d₃ (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).

Lobeline (α-Lobeline) sulfate is a brain-penetrant nicotinic receptor agonist. Lobeline sulfate increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline sulfate is effective in smoking cessation.

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

nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (K_d=26 nM).

TC-2559 is an orally active, selective central nervous system Nicotinic acetylcholine receptor agonist with a K_i value of 5 nM. TC-2559 activates central nervous system receptors selectively over peripheral nervous system receptors. TC-2559 improves scopolamine (HY-N0296)-induced cognitive impairment and enhances radial arm maze performance. TC-2559 can be used in the research of neurodegenerative diseases.

A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.

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.

QND8 is a selective and potent α7 nicotinic acetylcholine receptor (nAChR) agonist. QND8 can alleviate thermal hyperalgesia and mechanical hyperalgesia in carrageenan-induced inflammatory pain mouse model. QND8 can reduce the swelling of the mice feet, inhibit the release of pro-inflammatory factors at the inflammatory site, and prevent the infiltration of white blood cells. QND8 can be used for the research of inflammation and neurological disease, such as arthritis.

Doxacurium chloride (BW A938U) is a potent non-depolarizing neuromuscular blocking agent. Doxacurium chloride binds to cholinergic receptors to antagonize acetylcholine, resulting in a block of neuromuscular transmission. Doxacurium chloride can be used for the research of neurological diseases.

TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC₅₀ of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC₅₀s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain.

Varenicline-¹⁵N,¹³C,d₂ is ¹⁵N and deuterated labeled Varenicline (HY-10019). 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.

RJR 2429 hydrochloride is a α4β2 and α7 nAChR agonist.

TC-6683 (AZD1446) is a selective α4β2 nicotinic acetylcholine receptor (nAChR) agonist. TC-6683 does not show significant therapeutic effects in the animal model of DYT1 dystonia.TC-6683 can be used for the research of neurological disease, such as cognitive disorder.

Rivanicline (RJR-2403) hydrochloride is a neuronal nicotinic receptor agonist. Rivanicline hydrochloride is highly selective for the rat brain cortex nAChRs (K_i = 26 nM, EC₅₀ of 732 nM) and α4β2 subtype (K_i = 26 nM, EC₅₀ = 16 μM). Rivanicline hydrochloride can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hydrochloride can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease).

Anabasine (Standard) is the analytical standard of Anabasine. This product is intended for research and analytical applications. Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC₅₀=0.7 μM).

TC299423 is an orally active, brain-penetrant, selective and potent agonist for α6β2^? and α4β2^? nicotinic acetylcholine receptors (nAChRs) with anxiolytic and antinociceptive properties. TC299423 acts primarily through α6β2^? nAChRs that are implicated in the anxiolytic effects of nicotine. TC299423 elicits reward-related behavior mediated through α6β2^? nAChRs in hypersensitive α6L90’S mice. TC299423 elicits dopamine release and dose not suppress nicotine self-administration in rats. TC299423 is proming for rasearch of addiction and Parkinson’s disease.

PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR).PHA 568487 reduces neuroinflammation and oxidative stress. PHA-568487 has rapid brain penetration.