α4β2 nachr

Desformylflustrabromine hydrochloride (dFBr hydrochloride) is a selective agonist of nicotinic acetylcholine receptor (nAChR) in α4β2 neurons, with pEC50 of 6.48.

Rivanicline 2HCl is a selective neuronal nicotinic receptor inhibitor with a high affinity for the α4β2 subtype.

UB 165 fumarate is an agonist of the nAChR, a partial agonist of the α4β2 subtype, and a full agonist of the α3β2 subtype, with a Ki value of 0.27 nM for binding to [3H]-nicotine measured in rat brain.

Ispronicline (TC-1734) An orally active, selective, and potent α4β2 nAChR partial agonist with antidepressant, neuroprotective, and long-lasting cognitive effects.Ispronicline has a high affinity for the α4β2 nAChR with a Ki= 11 nM.

Biricodar dicitrate (VX-710) is a potent MDR inhibitor with no anticancer activity and can be used to study prostate cancer.

Urethane (Ethyl carbamate; Ethylurethane) is a byproduct formed during the fermentation process of various foods. As an ethyl ester of carbamic acid, it has the ability to inhibit the growth of bacteria, sea urchin eggs, protozoa, and plant tissues, and is commonly used for establishing lung cancer models.

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

Thiacloprid is a neonicotinoid insecticide that acts as a selective agonist at insect nicotinic acetylcholine receptors (nAChRs) with IC50values of 2.7 and 860 nM forDrosophilanAChRs and M10 mouse fibroblast cells expressing α4β2 subunit-containing nAChRs, respectively.1It is active against aphids, whiteflies, various species of beetle, andLepidopteraspecies when used at concentrations ranging from 48 to 180 g AI/hectare.2It has anti-estrogenic activity in a yeast estrogen screen and is toxic to adult female houseflies and mice (LD50s = 0.03 and 28 mg/kg, respectively).1,3Formulations containing thiacloprid have been used in the control of insects in agriculture. 1.Tomizawa, M., and Casida, J.E.Selective toxicity of neonicotinoids attributable to specificity of insect and mammalian nicotinic receptorsAnnu. Rev. Entomol.48339-364(2003) 2.Elbert, A., Erdelen, C., Kuhnhold, J., et al.Thiacloprid, a novel neonicotinoid insecticide for foliar applicationProc. Brighton Crop. Prot. Conf. - Pests and Diseases121-26(2000) 3.Westlund, P., and Yargeau, V.Investigation of the presence and endocrine activities of pesticides found in wastewater effluent using yeast-based bioassaysSci. Total Environ.607-608744-751(2017)

Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable agonist of the nicotinic acetylcholine receptor (nAChR) with a Ki of 16.7 nM.

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].

GTS-21 dihydrochloride (DMBX-anabaseine) is a nAChRs agonist. nAChRs are neuron receptor proteins that activated by the binding of the neurotransmitter ACh.

NS9283 is a positive allosteric modulator of α4β2 receptor.

Varenicline dihydrochloride is a Selective α4β2 nicotinic acetylcholine receptor partial agonist.

NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) that binds with high affinity to heteromeric α3β4 and α4β2 nAChRs, displaying β-subunit preference and no activation at α4-containing receptors. The maximal efficacy of NS3861 depends on the ligand-binding domain, and a serine to threonine substitution in the principal subunit may explain the lack of activation at α4-containing receptors.

suvn-911 is a potent and selective antagonist of neuronal nicotinic acetylcholine α4β2 receptor (Ki = 1.5 nM) with antidepressant activity.

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

Adiphenine hydrochloride (Patrovina), a nicotinic receptor inhibitor, can be used as an antispasmodic drug.

(±)-Anatoxin A fumarate is the salt form of (±)-Anatoxin A.(±)-Anatoxin A is a potent neurotoxic naturally occurring alkaloid known as a rapid death factor (VFDF), a potent, direct, and selective agonist of the nAchR (nicotinic acetylcholine receptor), also known as the nicotinic receptor agonist.

Anatabine dicitrate, a tobacco alkaloid that can cross the blood-brain barrier, is a potent α4β2 nAChR agonist and inhibits NF-κB activation, thereby reducing amyloid-β (Aβ) production by preventing β-cleavage of the amyloid precursor protein.

(R)-(+)-Anatabine, the less active R-enantiomer of Anatabine, is a potent agonist of α4β2 nAChR.

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.

Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction. Pozanicline selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a no

A 85380 is a novel and high-affinity agonist for neuronal nicotinic acetylcholine receptors (nAChR). A 85380 hydrochloride demonstrates selectivity for the α4β2 nAChR subtype and exhibits broad-spectrum analgesic properties.

Dexmecamylamine ((+)-Mecamylamine) acts as an antagonist of nicotinic acetylcholine receptors (nAChR), effectively inhibiting α3β4, α4β2, α7, and α1β1γδ receptors, with an IC50 in the micromolar range. It also exhibits anxiolytic and antidepressant-like effects.