Nicotinic agonists. Medical search. Frequent questions

A nicotinic agonist is a drug that mimics the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs). (wikipedia.org)
When ACh or other agonists bind to the receptors it stabilizes the open state of the ion channel allowing influx of cations such as potassium, calcium and sodium ions. (wikipedia.org)
α4β2 nAChRs account for approximately 90% of the nAChRs in the human brain and when chronically exposed to nicotine or other nicotine agonists leads to increase in density of α4β2 receptors which is the opposite of what usually happens when other receptors are chronically exposed to their agonists. (wikipedia.org)
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)
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)
Current literature suggests involvement of nicotinic acetylcholine receptors (nAChRs) in major depression. (nih.gov)
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). (cdrewu.edu)
Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. (cdrewu.edu)
Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission. (cdrewu.edu)
Central cholinergic regulation of respiration: nicotinic receptors. (cdrewu.edu)
Nicotine, the primary alkaloid in tobacco products binds stereo-selectively to nicotinic-cholinergic receptors on autonomic ganglia, the adrenal medulla, neuromuscular junctions and in the brain. (pharmacycode.com)
3-(2,4-Dimethoxybenzylidene)-anabaseine (DMXB-A) is a partial agonist at alpha7-nicotinic acetylcholine receptors and is now in early clinical development for treatment of deficits in neurocognition and sensory gating in schizophrenia. (druglib.com)
The findings are consistent with the previously established function of alpha7-nicotinic receptors on inhibitory interneurons in the hippocampus and with genetic evidence for deficits in these receptors in schizophrenia. (druglib.com)
Numerous high-resolution crystallographic structures of the acetylcholine binding protein (AChBP), a molluscan cholinergic protein, homologous to the extracellular domain of nicotinic acetylcholine receptors, are available. (pasteur.fr)
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)
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)
Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. (nature.com)
Role of presynaptic nicotinic acetylcholine receptors in the regulation of gastrointestinal motility. (nature.com)
Coniine has direct effects on nicotinic (cholinergic) receptors, both agonist and antagonist. (medscape.com)
As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric [(α3) m (β4) n where m + n = 5]. (wikipedia.org)
It is a selective partial agonist of nicotinic acetylcholine receptors. (scitechdaily.com)
As an agonist, it binds to the receptors to alleviate symptoms of craving and withdrawal. (mims.co.uk)
Both alpha7 and alpha4beta2 nicotinic receptors in the hippocampus are involved. (duke.edu)
Finally, nicotine administration has been demonstrated to rescue long‑term potentiation in individuals with sleep deprivation, AD, chronic stress and hypothyroidism, primarily by desensitizing α7 nicotinic acetylcholine receptors. (spandidos-publications.com)
Skok VI: Nicotinic acetylcholine receptors in autonomic ganglia. (spandidos-publications.com)
Gotti C, Zoli M and Clementi F: Brain nicotinic acetylcholine receptors: Native subtypes and their relevance. (spandidos-publications.com)
Hone AJ and McIntosh JM: Nicotinic acetylcholine receptors in neuropathic and inflammatory pain. (spandidos-publications.com)
The effects on AC were equally noted in brain regions enriched (striatum) or sparse (cerebellum) in cholinergic projections, implying that the effects are secondary to activation/repression of neural circuits, rather than representing direct effects on AC mediated by nicotinic cholinergic receptors. (duke.edu)
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)
It is an agonist at both muscarinic and nicotinic acetylcholine receptors. (bvsalud.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)

Both binding sites work together and thus, both sites need to be occupied with a nAChR agonist so that channel activation can take place. (wikipedia.org)
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)
ABT 594 hydrochloride is a selective α4β2 nAChR agonist (EC 50 = 140 nM for human α4β2 nAChRs, in vitro ). (tocris.com)

ABT-594 [5-2R-azetidinylmethoxy-2-chloropyridine], a novel neuronal nicotinic acetylcholine receptor agonist, produced significant antinociceptive effects in mice against both acute noxious thermal stimulation--the hot-plate and cold-plate tests--and persistent visceral irritation--the abdominal constriction writhing assay maximally-effective dose in each test 0.62 micromol/kg, i.p. (erowid.org)
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)
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)
Association of the neuronal nicotinic receptor beta2 subunit gene (CHRNB2) with subjective responses to alcohol and nicotine. (nature.com)
Dani JA: Neuronal nicotinic acetylcholine receptor structure and function and response to nicotine. (spandidos-publications.com)

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)
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)
Recent work with more selective nicotinic receptor agonists and antagonists in animal models is providing important information concerning the neural mechanisms for nicotinic involvement in cognitive function and opening avenues for development of safe and effective nicotinic treatments for clinical use. (duke.edu)

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)
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)

Nicotinic acetylcholine receptor partial agonist. (drugs.com)
Varenicline, an α4β2 Nicotinic Acetylcholine Receptor Partial Agonist, vs Sustained-Release Bupropion and Placebo for Smoking Cessation. (mims.co.uk)

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)
Zaveri N, Jiang F, Olsen C, Polgar W and Toll L: Novel α3β4 nicotinic acetylcholine receptor-selective ligands. (spandidos-publications.com)
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)

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)
The plant, Cytisus laburnum , contains an alkaloid cytisine which is a nicotine analogue, acting as a partial nicotinic acetylcholine receptor agonist. (bmj.com)
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)
The nicotinic alpha-7 receptor agonist alliance with Roche will also remain as one of Memory Pharmaceuticals' foci. (genengnews.com)

Varenicline was developed as a nicotine receptor partial agonist from cytisine, a drug widely used in central and eastern Europe for smoking cessation. (who.int)
SEARCH STRATEGY: We searched the Cochrane Tobacco Addiction Group's specialised register for trials, using the terms ('varenicline' or 'cytisine' or 'Tabex' or 'nicotine receptor partial agonist') and 'smoking' in the title or abstract, or as keywords. (who.int)
Varenicline is a nicotine receptor partial agonist available only by prescription. (cdc.gov)

BACKGROUND: Nicotine receptor partial agonists may help people to stop smoking by a combination of maintaining moderate levels of dopamine to counteract withdrawal symptoms (acting as an agonist) and reducing smoking satisfaction (acting as an antagonist). (who.int)
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)

GAT107 is an allosteric agonist and positive allosteric modulator (ago-PAM) of α7 nAChR that can produce persistent activation of this receptor. (listlabs.com)
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 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)
We have found in lesion and local infusion studies with rats that the hippocampus is an important substrate for nicotinic effects on working memory function. (duke.edu)
Levin ED, Bettegowda C, Blosser J and Gordon J: AR-R17779, and alpha7 nicotinic agonist, improves learning and memory in rats. (spandidos-publications.com)
Effects of acute administration of nicotinic and muscarinic cholinergic agonists and antagonists on performance in different cost-benefit decision making tasks in rats. (ufl.edu)

OBJECTIVES: The primary objective of this review is to assess the efficacy and tolerability of nicotine receptor partial agonists, including varenicline and cytisine, for smoking cessation. (who.int)
The researchers found that cytisine, a partial agonist-binding nicotine acetylcholine receptor, is a promising cessation intervention. (scitechdaily.com)

Cahill K, Stead LF, Lancaster T . Nicotine receptor partial agonists for smoking cessation. (nature.com)
Partial agonists exert both agonist and antagonistic effects. (mims.co.uk)

to stabilize the open form of nAChRs, both binding sites must be occupied by agonist, such as nicotine or ACh. (wikipedia.org)
α4β2 nAChRs contain two α4 subunits and three β2 subunits, therefore it has two binding sites for ACh and other agonists. (wikipedia.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)

Functional magnetic resonance imaging of effects of a nicotinic agonist in schizophrenia. (druglib.com)
Imaging of drug response is useful in planning future clinical tests of this compound and other nicotinic agonists for schizophrenia. (druglib.com)
Alpha 7 nicotinic acetylcholine receptor (α7nAChR) agonists have been developed to treat schizophrenia but failed in clinical trials due to rapid desensitization. (bvsalud.org)
Nicotine, as well as other nicotinic drugs, may provide useful therapeutic treatment for a variety of cognitive impairments including those found in Alzheimer's disease, schizophrenia and attention deficit hyperactivity disorder (ADHD). (duke.edu)

COLLINS, A.C. RJR-2403: a nicotinic agonist with CNS selectivity II. (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)

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)
Nicotinic acetylcholine receptor beta2 subunit gene implicated in a systems-based candidate gene study of smoking cessation. (nature.com)
Varenicline is a partial agonist of the nicotinic acetylcholine receptor and is used to help in smoking cessation. (nih.gov)

The development of nAChR agonists began in the early 1990s after the discovery of nicotine's positive effects. (wikipedia.org)
Animal models are critical for determining the neurobehavioral bases for nicotinic effects on cognitive function. (duke.edu)

Scholars@Duke publication: Development of nicotinic drug therapy for cognitive disorders. (duke.edu)
Further work has investigated the relationship of nicotinic systems with dopaminergic and glutaminergic systems in the basis of cognitive function. (duke.edu)

Nicotinic Agonists" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (cdrewu.edu)

Nicotine has proven to be a useful prototypic compound for the family of nicotinic compounds. (duke.edu)

It is shown that the studied agonists and antagonists can be discriminated according to their higher affinities for structures respectively obtained in the presence of agonists or antagonists, highlighting the fact that AChBP structures retain a pharmacological footprint of the compound used in crystallography experiments. (pasteur.fr)

This well-validated pre-clinical model is predictive of changes in PD, and is thus a very useful and economical model for initial studies to evaluate the antidyskinetic potential of nicotinic drugs. (michaeljfox.org)

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)

Anatomy6

Organisms2

Chemicals and Drugs65

Analytical, Diagnostic and Therapeutic Techniques and Equipment2

Phenomena and Processes2

Disciplines and Occupations1

Receptors32

NAChR agonist3

Neuronal6

Selective nicotinic3

Alpha4beta2 nicotinic3

Acetylcholine receptor partial2

Ligands5

Receptor agonist4

Nicotine receptor partial agonist3

Antagonist2

Allosteric agonist3

Rats4

Cytisine2

Partial agonists2

NAChRs3

Schizophrenia4

Selectivity1

Subunit mRNA1

Cessation3

Effects2

Cognitive2

Subject Headings1

Compounds1

Affinities1

Drugs1

Parkinson's1