Nicotinic receptor agonist. Medical search. Frequent questions

Dr. Quik found that the targeted nAChR agonist varenicline resulted in significant declines in levodopa-induced AIMs at a relatively low dose of the agonist, with no worsening of parkinsonism. (michaeljfox.org)
Varenicline, a nicotinic receptor agonist for the treatment of Excessive Daytime Sleepiness in Parkinson s Disease: a placebo-controlled cross-over pilot study. (neurodegenerationresearch.eu)
Therefore the effect of varenicline, an alpha4beta2 nicotinic receptor partial agonist, on excessive daytime sleepiness in Parkinson's disease will be studied in a placebo-controlled cross-over study.The effect of varenicline, an alpha4beta2 nicotinic receptor partial agonist on excessive daytime sleepiness in Parkinson's disease will be studied in a randomized, double blind, placebo-controlled clinical trial with a within-subject crossover design. (neurodegenerationresearch.eu)
This study evaluated association between common and rare sequence variants in 10 nicotinic acetylcholine receptor subunit genes and the severity of nausea 21 days after initiating the standard, Food and Drug Administration-approved varenicline regimen for smoking cessation. (nature.com)
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. (nature.com)
Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. (nature.com)
Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. (nature.com)
Varenicline is a partial agonist of the nicotinic acetylcholine receptor and is used to help in smoking cessation. (nih.gov)
Varenicline (var en' i kleen) is a partial agonist of the α4 β2 nicotinic acetylcholine receptor and appears to act by blocking the binding of nicotine to this receptor while providing partial agonist effect thus relieving nicotine craving. (nih.gov)
Varenicline is a nicotine receptor partial agonist available only by prescription. (cdc.gov)
Varenicline tartrate is a prescription nicotinic receptor/partial agonist used to treat the addiction to smoking. (tcdailyplanet.net)
Due to both language and Iron Curtain barriers, this went unnoticed in the West until Pfizer launched a partial nicotinic receptor agonist varenicline, inspired by and similar to Tabex, as an effective treatment for smoking cessation in 2006. (bmj.com)
Varenicline, an α4β2 Nicotinic Acetylcholine Receptor Partial Agonist, vs Sustained-Release Bupropion and Placebo for Smoking Cessation. (mims.co.uk)

The antinociceptive effect of ABT-594 was prevented, but not reversed, by the noncompetitive neuronal nicotinic acetylcholine receptor antagonist mecamylamine 5 micromol/kg, i.p. (erowid.org)
In contrast, the antinociceptive effect of ABT-594 was not prevented by hexamethonium 10 micromol/kg, i.p., a neuronal nicotinic acetylcholine receptor antagonist that does not readily enter the central nervous system, nor by naltrexone 0.8 micromol/kg, an opioid receptor antagonist. (erowid.org)
5-HT3 receptor antagonist WAY-317,538 - selective potent full agonist with nootropic and neuroprotective properties Anabasine Acetylcholine Nicotine Epiboxidine Choline ICH-3: subtype-selective partial agonist At least two types of positive allosteric modulators (PAMs) can be distinguished. (wikipedia.org)
Coniine has direct effects on nicotinic (cholinergic) receptors, both agonist and antagonist. (medscape.com)
Water hemlock contains cicutoxin, a potent, noncompetitive gamma-aminobutyric acid (GABA) receptor antagonist. (medscape.com)
Bupropion is a dopamine and norepinephrine reuptake inhibitor with nicotine receptor antagonist properties. (cdc.gov)
Tropisetronul este un antagonist al receptorilor serotoninergici de tipul 5-HT 3 , [9] dar prezintă și efect agonist asupra receptorilor nicotinici de tipul α 7 . (wikipedia.org)
As an antagonist, it competes with nicotine at the receptor binding sites resulting in a reduction of the rewarding and reinforcing effects of smoking. (mims.co.uk)
These small currents were linked to ACh release since anticholinesterases (neostigmine) increased their effects, while cholinergic receptor antagonist (tubocurarine, a nicotinic receptor blocker) blocked. (pharmacology2000.com)
It is a serotonin modulator and stimulator that blocks the serotonin transporter, a partial agonist of serotonin receptor 1B and antagonist of serotonin receptors 3A and 7. (psychiatrictimes.com)

It is a selective partial agonist of nicotinic acetylcholine receptors. (scitechdaily.com)

In this study, we systematically compared the effects of non-selective and selective nicotinic agonists and antagonists in two different tests for antidepressant effects in mice: the tail suspension test and the forced swim test. (nih.gov)
Although nicotine is an agonist of ionotropic acetylcholine receptors, we found that nicotine-induced polyspermy was neither mimicked by acetylcholine and carbachol nor inhibited by specific antagonists of nicotinic acetylcholine receptors. (mdpi.com)

Nicotinic acetylcholine receptor partial agonist. (drugs.com)

slowly reversible β-Caryophyllene Bupropion (very weakly) Dehydronorketamine Ethanol Hydroxybupropion (very weakly) Hydroxynorketamine Ketamine Kynurenic acid Memantine Lobeline Methyllycaconitine Norketamine Quinolizidine (-)-1-epi-207I: α7 subtype preferring blocker α3β2-Nicotinic receptor α3β4-Nicotinic receptor α4β2-Nicotinic receptor RIC3, a chaperone protein for α7 receptors Endocannabinoids Pharmacology, (Rang, Dale, Ritter & Moore, ISBN 0-443-07145-4, 5th ed. (wikipedia.org)
Benson, J.A. (1992) Electrophysiological pharmacology of the nicotinic and muscarinic cholinergic responses of isolated neuronal somata from locust thoracic ganglia. (springer.com)

The alpha-3 beta-4 nicotinic receptor , also known as the α3β4 receptor and the ganglion-type nicotinic receptor , [1] is a type of nicotinic acetylcholine receptor , consisting of α3 and β4 subunits . (wikipedia.org)

GAT107 is an allosteric agonist and positive allosteric modulator (ago-PAM) of α7 nAChR that can produce persistent activation of this receptor. (listlabs.com)
The α7-selective positive allosteric modulator PNU-120596 was used to reveal receptor activation, measured as an increase in intracellular calcium using fluorescent indicators. (bath.ac.uk)
Dose-dependent effects of GAT107, a novel allosteric agonist-positive allosteric modulator (ago-PAM) for the α7 nicotinic cholinergic receptor: a BOLD phMRI and connectivity study on awake rats. (bvsalud.org)
GAT107, a type 2 allosteric agonist-positive allosteric modulator (ago-PAM) to the α7 nAChR was designed to activate the α7 nAChR while reducing desensitization. (bvsalud.org)

The alpha-7 nicotinic receptor, also known as the α7 receptor, is a type of nicotinic acetylcholine receptor implicated in long-term memory, consisting entirely of α7 subunits. (wikipedia.org)

Alijevic O, McHugh D, Rufener L, Mazurov A, Hoeng J, Peitsch M ( 2020 ) An electrophysiological characterization of naturally occurring tobacco alkaloids and their action on human alpha4beta2 and alpha7 nicotinic acetylcholine receptors. (multichannelsystems.com)

Ligands which inhibit the α3β4 receptor have been shown to modulate drug-seeking behavior, [6] making α3β4 a promising target for the development of novel antiaddictive agents. (wikipedia.org)
Interestingly, the third binding site has, so far, only been documented using electrophysiological assays, actual binding affinities of nicotinic receptor ligands to this site are not known. (ku.dk)
The present study was therefore aimed at determining binding affinities of nicotinic ligands to the α4-α4 interface. (ku.dk)
A strong correlation between binding affinities at the (α4)3(β2(HQT))2 receptor and functional potencies at the wild-type receptor of a range of nicotinic ligands highlighted the validity of using the mutational approach. (ku.dk)
Cieslikiewicz-Bouet M, Naldi M, Bartolini M, Pérez B, Servent D, Jean L, Aráoz R, Renard P-Y ( 2020 ) Functional characterization of multifunctional ligands targeting acetylcholinesterase and alpha 7 nicotinic acetylcholine receptor. (multichannelsystems.com)
Zaveri N, Jiang F, Olsen C, Polgar W and Toll L: Novel α3β4 nicotinic acetylcholine receptor-selective ligands. (spandidos-publications.com)

The central hypothesis underlying this proposal is that drugs targeting CNS nicotinic acetylcholine receptors (nAChRs) may be of therapeutic value for the treatment of levodopa-induced dyskinesias in Parkinson's disease. (michaeljfox.org)
We therefore propose to test the effect of nAChR agonists that preferentially stimulate brain nAChRs and not those in the peripheral nervous system. (michaeljfox.org)
Current literature suggests involvement of nicotinic acetylcholine receptors (nAChRs) in major depression. (nih.gov)
The aim of this study was to investigate the ability of sazetidine-A, a novel partial agonist at α4β2 nicotinic acetylcholine receptors (nAChRs), to affect the function of native α7 nAChRs in SH-SY5Y cells and primary cortical cultures. (bath.ac.uk)

The results will allow for the development of selective nicotinic drugs against levodopa-induced dyskinesias with optimal therapeutic efficacy and a minimum of adverse effects. (michaeljfox.org)

2019 ) Agonist Selectivity and Ion Permeation in the α3β4 Ganglionic Nicotinic Receptor. (academictree.org)

These data indicate that ABT-594 is a centrally acting neuronal nicotinic acetylcholine receptor agonist with potent antinociceptive and anxiolytic-like effects in mice. (erowid.org)

Nicotinergic acetylcholine receptors are made up of 5 subunits, symmetrically arranged around a central pore (ion channel). (axonmedchem.com)

It is an agonist at both muscarinic and nicotinic acetylcholine receptors. (bvsalud.org)

Broide RS, Winzer-Serhan UH, Chen Y and Leslie FM: Distribution of alpha7 nicotinic acetylcholine receptor subunit mRNA in the developing mouse. (spandidos-publications.com)

It has a high affinity for the α-4 β-2 receptor subtype, which is thought to be the main receptor that mediates the central effects of nicotine. (bmj.com)

Skok VI: Nicotinic acetylcholine receptors in autonomic ganglia. (spandidos-publications.com)

Partial agonists exert both agonist and antagonistic effects. (mims.co.uk)

In severe cases, acetylcholine (nicotinic) receptor antagonism develops. (medscape.com)

It will also help determine whether nicotine and/or nicotinic agonists are of benefit in the treatment of dyskinesias that occur with levodopa treatment for Parkinson's disease. (michaeljfox.org)

Gotti C, Zoli M and Clementi F: Brain nicotinic acetylcholine receptors: Native subtypes and their relevance. (spandidos-publications.com)

2018 ) Resolution of Heterogeneity in Nicotinic Receptor Assembly by Cryo-EM Biophysical Journal . (academictree.org)

The exact subunit stoichiometry is not known and it is possible that more than one functional α3β4 receptor assembles in vivo with varying subunit stoichiometries. (wikipedia.org)
As with other nicotinic acetylcholine receptors, functional α7 receptors are pentameric [i.e., (α7)5 stoichiometry]. (wikipedia.org)
Functional α7 receptors are present in the submucous plexus neurons of the guinea-pig ileum. (wikipedia.org)
Given that epibatidine shows large functional potency differences at α4-β2 vs. α4-α4 interfaces, biphasic binding properties would be expected at (α4)3(β2)2 receptors. (ku.dk)

As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric [(α3) m (β4) n where m + n = 5]. (wikipedia.org)

2018 ) Structure of a human synaptic GABA receptor. (academictree.org)

The researchers found that cytisine, a partial agonist-binding nicotine acetylcholine receptor, is a promising cessation intervention. (scitechdaily.com)
The plant, Cytisus laburnum , contains an alkaloid cytisine which is a nicotine analogue, acting as a partial nicotinic acetylcholine receptor agonist. (bmj.com)

5-HT3 differ from all other 5-HT (serotonin) receptors whose actions are mediated via G proteins . (axonmedchem.com)
Genetic variants within the serotonin transporter-serotonin receptors and genes involved in neurodevelopment-have been found to modulate the risk of TRD. (psychiatrictimes.com)

K.L. Brain, J. Somogyi, D.J. Williams, O.J. Levy, T.C. Cunnane m-Chlorophenylbiguanide inhibits neurotransmitter release and nerve terminal Ca2+ influx independently of 5-HT3 receptors in the mouse vas deferens. (ox.ac.uk)

Association of the neuronal nicotinic receptor beta2 subunit gene (CHRNB2) with subjective responses to alcohol and nicotine. (nature.com)
Preincubtion with sazetidine-A concentration-dependently attenuated subsequent responses to the α7-selective agonist PNU-282987 in SH-SY5Y cells (IC 50 476 nM) and cortical cultures. (bath.ac.uk)

It was previously demonstrated that high concentrations of cholinergic agonists such as acetylcholine (ACh), carbamylcholine (CCh), suberyldicholine (SubCh) and spin-labelled acetylcholine (SL-ACh) displaced quinacrine from its high-affinity binding site located at the lipid-protein interface of the nicotinic acetylcholine receptor (AChR) (Arias, H. R. and Johnson, D. A. (1995) Biochemistry, 34, 1589-1595). (okstate.edu)
With this receptor, low affinity binding of epibatidine with a Kd of ∼5 nM was observed in sharp contrast to a Kd value of ∼10 pM observed for wild-type receptors. (ku.dk)
1991. Effects of polychlorinated biphenyls with Ah receptor affinity on lymphoid development in the thymus and the bursa of Fabricius on chick embryos in ovo and in mouse thymus anlagen in vitro . (cdc.gov)

da Costa Couto A, Price KL, Mesoy S, Capes E, Lummis SCR ( 2020 ) The M4 Helix Is Involved in α7 nACh Receptor Function. (multichannelsystems.com)

2018 ) Structural principles of distinct assemblies of the human α4β2 nicotinic receptor. (academictree.org)
Unwin N: Nicotinic acetylcholine receptor and the structural basis of neuromuscular transmission: Insights from Torpedo postsynaptic membranes. (spandidos-publications.com)

An α7 nicotinic agonist appears to have positive effects on neurocognition in persons with schizophrenia. (wikipedia.org)
α7 receptors are also involved in angiogenic and neurogenic activity, and have anti-apoptotic effects. (wikipedia.org)
It reduces nicotine withdrawal symptoms (including craving) and reduces the rewarding effects of cigarettes by blocking nicotinic receptors. (cdc.gov)
and reducing the rewarding effects of nicotine if someone lapses and smokes, by blocking or desensitizing nicotinic receptors. (msdmanuals.com)
1994. Ah receptor in embryonic mouse palate and effects of TCDD on receptor expression. (cdc.gov)

A-867744 Ivermectin Nefiracetam It is found that anandamide and ethanol cause an additive inhibition on the function of α7-receptor by interacting with distinct regions of the receptor. (wikipedia.org)
Although ethanol inhibition of the α7-receptor is likely to involve the N-terminal region of the receptor, the site of action for anandamide is located in the transmembrane and carboxyl-terminal domains of the receptors. (wikipedia.org)
A direct correlation was observed between K p and the apparent inhibition constant (K i ) for agonists to displace AChR-bound quinacrine. (okstate.edu)
By themselves, these results support the conjecture that agonist self-inhibition seems to be mediated by the quinacrine binding site via a membrane approach mechanism. (okstate.edu)
however, we can not discard that the process of agonist self-inhibition can also be mediated by a steric blockage of the ion channel. (okstate.edu)
Conversely, inhibition of PVA neuronal activity using DREADDs (designer receptors exclusively activated by designer drugs) or inactivation of PVA extracellular signal-regulated kinase at the critical time window blunted mechanical hyperalgesia in chronic pain models. (iasp-pain.org)

Brown, JL & Wonnacott, S 2014, ' Sazetidine-A activates and desensitizes native α7 nicotinic acetylcholine receptors ', Neurochemical Research , vol. 40, no. 10, pp. 2047-2054. (bath.ac.uk)

As an agonist, it binds to the receptors to alleviate symptoms of craving and withdrawal. (mims.co.uk)

The idea that nicotinic drugs may be useful for the treatment of dyskinesias is based on our studies, which show that nicotine reduces levodopa-induced abnormal involuntary movements in a non-human primate parkinsonian model and in hemi-parkinsonian rats. (michaeljfox.org)
Levin ED, Bettegowda C, Blosser J and Gordon J: AR-R17779, and alpha7 nicotinic agonist, improves learning and memory in rats. (spandidos-publications.com)

Breer, H., Sattelle, D.B. (1987) Molecular properties and functions of insect acetylcholine receptors. (springer.com)

Resequencing of nicotinic acetylcholine receptor genes and association of common and rare variants with the Fagerström test for nicotine dependence. (nature.com)

Finally, large differences in activities at α4-β2 vs. α4-α4 interfaces were observed for structurally related agonists underscoring the need for establishing all binding parameters of compounds at α4β2 receptors. (ku.dk)

Therefore, an engineered β2 construct (β2(HQT)), which converts the β(-) face to resemble that of an α4(-) face, was utilized to create (α4)3(β2(HQT))2 receptors harboring three α4-α4 interfaces. (ku.dk)

It inhibits parasite growth by acting as an agonist to nicotinic acetylcholine receptors leading to paralysis. (herts.ac.uk)

To further assess the differences in agonist accessibility to the quinacrine binding site, we calculated the agonist concentration in the lipid membrane (C M ) at an external agonist concentration high enough to inhibit 50% of quinacrine binding (IC 50 ), which in turn was obtained by agonist back titration of AChR-bound quinacrine. (okstate.edu)

Alpha 7 nicotinic acetylcholine receptor (α7nAChR) agonists have been developed to treat schizophrenia but failed in clinical trials due to rapid desensitization. (bvsalud.org)

Thus, initiation of antinociception by ABT-594 involves activation of central nicotinic acetylcholine receptors, but does not require activation of naltrexone-sensitive opioid receptors. (erowid.org)
Activation of α7 nicotinic acetylcholine receptor on mast cells, is a mechanism by which nicotine enhances atherosclerosis. (wikipedia.org)

The nicotinic acetylcholine receptor α4β2 is important for normal mammalian brain function and is known to express in two different stoichiometries, (α4)2(β2)3 and (α4)3(β2)2. (ku.dk)

Anatomy25

Organisms11

Diseases3

Chemicals and Drugs178

Analytical, Diagnostic and Therapeutic Techniques and Equipment12

Psychiatry and Psychology3

Phenomena and Processes22

Disciplines and Occupations1

Information Science2

Health Care1

Varenicline13

Antagonist10

Partial agonist of nicotinic acetylcho1

Antagonists2

Acetylcholine receptor partial1

Pharmacology2

Beta-4 nicotinic receptor1

Positive allosteric4

Alpha-7 nicoti1

Alpha4beta21

Ligands6

NAChRs4

Selective nicotinic1

Selectivity1

Potent1

Subunits1

Muscarinic1

Subunit mRNA1

Subtype1

Autonomic Ganglia1

Antagonistic effects1

Antagonism1

Parkinson's Disease1

Subtypes1

Heterogeneity1

Functional4

Pentameric1

GABA1

Cytisine2

Serotonin2

Neurotransmitter1

Responses2

Affinity3

20201

Structural2

Effects5

Inhibition6

Activates1

Binds1

Rats2

Molecular1

Genes1

Structurally1

Interfaces1

Paralysis1

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Schizophrenia1

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Brain1