α4β2 nachr

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

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 (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.

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)

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

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.

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.

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

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.

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

(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

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].

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.

AR-R17779 hydrochloride is a potent, selective full agonist of the nAChR, demonstrating K i values of 92 nM for the α7 subtype and 16,000 nM for the α4β2 subtype. It is noted for its ability to enhance learning and memory in rats, suggesting potential therapeutic applications. Additionally, this compound exhibits anxiolytic properties and can mitigate inflammation by activating anti-inflammatory cholinergic (vagal) pathways [1] [2] [4].

DMAB-anabaseine dihydrochloride (N,N-dimethyl-4-[(E)-(6-pyridin-3-yl-3,4-dihydro-2H-pyridin-5-ylidene)methyl]aniline;dihydrochloride) is an α7-containing neuronal nicotinic receptor partial agonist and an antagonist at α4β2 and other nicotinic receptors.

nAChR agonist that displays selectivity for α4β2

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

Iptakalim, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist. Iptakalim is also a K(ir) 6.1 SUR2B activator that can attenuate hypoxia-induced pulmonary arterial hypertension in rats by endothelial function protection.

NS9283 is a positive allosteric modulator of α4β2 receptor.