Activation of nicotinic receptors. Medical search. Frequent questions

Fetal brain regions and peripheral tissues were examined for nAChR subtypes, other neurotransmitter receptors, and indices of cell signaling and cell damage. (nature.com)
However, it is controversial whether the antidepressant-like effect of nAChR modulation is induced by activation, desensitization or inhibition of central nAChRs. (nih.gov)
When released in the synaptic cleft, ACh binds to two distinct types of receptors: Ionotropic nicotinic acetylcholine receptors (nAChR) and metabotropic muscarinic acetylcholine receptors (mAChRs). (genome.jp)
The activation of nAChR by ACh leads to the rapid influx of Na+ and Ca2+ and subsequent cellular depolarization. (genome.jp)
Tobacco smoke contains nicotine, which activates the nicotinic acetylcholine receptors (nAChR) expressed by the human body. (helsinki.fi)
The α7 nicotinic acetylcholine receptor (α7 nAChR) negatively regulates the synthesis and release of pro-inflammatory cytokines by immune cells. (listlabs.com)
Our previous studies showed that in encephalitogenic T cells, α7 nAChR expression is upregulated and that activation of the cholinergic system can attenuate experimental autoimmune encephalomyelitis (EAE). (listlabs.com)
GAT107 is an allosteric agonist and positive allosteric modulator (ago-PAM) of α7 nAChR that can produce persistent activation of this receptor. (listlabs.com)
Following activation of the α7 nAChR by GAT107 during EAE, disease severity was significantly reduced by 70% and was correlated with a reduction in the extent of neuroinflammation in the CNS. (listlabs.com)
[ 1 , 2 ] Although the chief target of the autoimmune attack in most cases is the skeletal muscle nicotinic acetylcholine receptor (nAChR), other antigenic targets that are components of the neuromuscular junction (NMJ) have also been implicated. (medscape.com)

The activation of heteromeric and homomeric nicotinic acetylcholine receptors was studied in Xenopus laevis oocytes to identify key structures of putative agonist molecules associated with the selective activation of homomeric α7 receptors. (aspetjournals.org)
Tetraethylammonium (TEA) is a molecule found to be a weak agonist of the muscle‐type nicotinic receptor. (wikipedia.org)
Coniine has direct effects on nicotinic (cholinergic) receptors, both agonist and antagonist. (medscape.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)
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)
They show that treating cultured mouse neurons expressing human APP with the acetylcholine receptor agonist carbachol increased the production of α-secretase cleavage products, but no such effect occurred in cells from M1 knockout mice. (alzforum.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)
Vallöf D, Maccioni P, Colombo G, Mandrapa M, Jörnulf JW, Egecioglu E, Engel JA , Jerlhag E. The glucagon-like peptide 1 receptor agonist liraglutide attenuates the reinforcing properties of alcohol in rodents. (neurotree.org)

2,6-Dimethylaniline (DMA), a molecule that mimics the hydrophobic moiety of lidocaine, has been found to bind the receptor at inter-subunit crevices of the trans-membrane spanning domain thereby causing non-competitive inhibition and restricting the channel from opening. (wikipedia.org)
In summary, the present work describes sequence elements critical in both cocaine inhibition and acetylcholine activation of nAChRs and indicates that nAChRs may provide a site of interaction for the effects of nicotine and cocaine in the nervous system. (aspetjournals.org)
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)
Engel JA , Jerlhag E, Svensson L, Smith RG, Egecioglu E. Blockade of growth hormone secretagogue receptor 1A signaling by JMV 2959 attenuates the NMDAR antagonist, phencyclidine-induced impairments in prepulse inhibition. (neurotree.org)

Water hemlock contains cicutoxin, a potent, noncompetitive gamma-aminobutyric acid (GABA) receptor antagonist. (medscape.com)
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 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)
Engel JA , Nylander I, Jerlhag E. A ghrelin receptor (GHS-R1A) antagonist attenuates the rewarding properties of morphine and increases opioid peptide levels in reward areas in mice. (neurotree.org)
4. The δ-receptor antagonist, naltrindole (30 nM), blocked the elevations of [Ca 2+ ](i) by DPDPE (100 nM) without affecting those caused by DAMGO while the μ-receptor antagonist, CTAP (D-Phe-Cys-Tyr-D-Trp-Arg-Pen-Thr-NH 2 ) (100 nM-1 μM) blocked the elevations of [Ca 2+ ](i) caused by DAMGO (1 μM) without affecting those caused by DPDPE. (edu.au)
The nicotinic receptor antagonist, mecamylamine (10 μM), did not affect the elevations of [Ca 2+ ](i) caused by opioids in the presence of carbachol. (edu.au)

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)

In physiological and behavioral studies, activation of nicotinic acetylcholine receptors (nAChRs) has been implicated in mediating cholinergic signaling. (oregonstate.edu)
Studies in developing rodents indicate that nicotine is a neuroteratogen that disrupts brain development by stimulating nicotinic acetylcholine receptors (nAChRs) that control neural cell replication and differentiation. (nature.com)
Current literature suggests involvement of nicotinic acetylcholine receptors (nAChRs) in major depression. (nih.gov)
Neuronal nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels of the central and peripheral nervous system that regulate synaptic activity from both pre- and postsynaptic sites. (aspetjournals.org)
We have studied if Pm affects nicotinic acetylcholine receptors (nAChRs), since they play broad functional roles, both in the nervous system and non-neuronal tissues. (mdpi.com)
Aβ perturbs a number of synaptic components including nicotinic acetylcholine receptors containing α7 subunits (α7-nAChRs), which are abundantly expressed in the hippocampus and found on GABAergic interneurons. (biomedcentral.com)
Spinosad targets activation of nicotinic acetylcholine receptors (nAChRs) in insects. (petstopclinic.com)

Activation of muscarinic acetylcholine receptors is known to steer APP down the non-amyloidogenic, α-secretase pathway, but it has been difficult to pin the effect on a specific receptor subtype: There are five different muscarinic receptors (M1-M5) and knowing which one is involved is critical for making selective drugs and minimizing cholinergic side effects. (alzforum.org)
Selectivity is important on both counts: Non-specific muscarinic receptor agonists can produce side effects due to peripheral cholinergic effects including gastrointestinal disturbances, changes in blood pressure, and excessive sweating. (alzforum.org)
Dopamine D2-receptor activation elicits akinesia, rigidity, catalepsy, and tremor in mice expressing hypersensitive {alpha}4 nicotinic receptors via a cholinergic-dependent mechanism. (umassmed.edu)

Based on structural comparisons of previously characterized selective and nonselective agonists, we hypothesize at least three chemical motifs exist that, when present in molecules containing an appropriate cationic center, could be associated with the selective activation of α7 receptors. (aspetjournals.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)
Zaveri N, Jiang F, Olsen C, Polgar W and Toll L: Novel α3β4 nicotinic acetylcholine receptor-selective ligands. (spandidos-publications.com)
Understanding what other subunits combine with beta2 to form the critical receptors that regulate anxiety could lead to selective therapeutics with fewer side effects," she said. (sciencedaily.com)
The selective toxicity of isoxazolines between insects, acarines, and mammals is due to the differential sensitivity of the GABA receptors in the respective species. (merckvetmanual.com)

The expression levels of Gα subunits influence the biased profiling of β-agonists and antagonists in that they determine both their activity and efficacy by affecting different membrane distribution of receptor-G protein populations. (mdpi.com)
Furthermore, all ACh-induced cellular and network changes were blocked by muscarinic, but not nicotinic receptor antagonists. (springer.com)
Furthermore, it has been observed that nicotine's rewarding effects can be reduced with opioid receptor antagonists. (helsinki.fi)
They are noncompetitive GABA receptor antagonists, bind to chloride channels in nerve and muscle cells, blocking signal transmission, and cause hyperexcitation, resulting in uncontrolled activity in the CNS and death of the target. (merckvetmanual.com)

These receptors are found in neuromuscular junctions, where activation leads to an excitatory postsynaptic potential (EPSP), mainly by increased Na+ and K+ permeability. (wikipedia.org)
Unwin N: Nicotinic acetylcholine receptor and the structural basis of neuromuscular transmission: Insights from Torpedo postsynaptic membranes. (spandidos-publications.com)
The autoimmune attack occurs when autoantibodies form against the nicotinic acetylcholine postsynaptic receptors at the neuromuscular junction of skeletal muscles (see the image below). (medscape.com)
Normal neuromuscular junction showing a presynaptic terminal with a motor nerve ending in an enlargement (bouton terminale): Synaptic cleft and postsynaptic membrane with multiple folds and embedded with several acetylcholine receptors. (medscape.com)
The rest are sensory in nature, although the largest sensory receptors, the neuromuscular spindles, have a motor supply of their own. (medscape.com)

In addition, Davis and coworkers show that treating neurons from M1 knockout mice with carbachol increased Aβ production, probably via stimulation of other non-M1 muscarinic receptor subtypes. (alzforum.org)
Gotti C, Zoli M and Clementi F: Brain nicotinic acetylcholine receptors: Native subtypes and their relevance. (spandidos-publications.com)
Activation of mAChRs is relatively slow (milliseconds to seconds) and, depending on the subtypes present (M1-M5), they directly alter cellular homeostasis of phospholipase C, inositol trisphosphate, cAMP, and free calcium. (genome.jp)

This work is unique because it suggests that nicotine may be acting through inactivation, rather than activation, of the high affinity nicotinic receptors," said Darlene Brunzell, Ph.D., assistant professor in the Department of Pharmacology and Toxicology in the VCU School of Medicine. (sciencedaily.com)

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)
In addition, the rewarding effect of nicotine attenuates in opioid receptor knock-out rodents. (helsinki.fi)
1. In this study we have investigated δ and μ opioid receptor-mediated elevation of intracellular Ca 2+ concentration ([Ca 2+ ](i)) in the human neuroblastoma cell line, SH-SY5Y. (edu.au)
6. Muscarinic receptor activation, not a rise in [Ca 2+ ](i), was required to reveal the opioid response. (edu.au)

Activation of α2A-containing nicotinic acetylcholine receptors mediates nicotine-induced motor output in embryonic zebrafish. (oregonstate.edu)
Nicotine may also activate thyroid receptor signaling pathways to improve memory impairment caused by hypothyroidism. (spandidos-publications.com)
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)
Dani JA: Neuronal nicotinic acetylcholine receptor structure and function and response to nicotine. (spandidos-publications.com)
In a study, published online this week in PLoS ONE , researchers observed that low doses of nicotine and a nicotinic receptor blocker had similar effects to reduce anxiety-like behavior in an animal model. (sciencedaily.com)
They found that inactivation of beta2 subunit, a specific sub-class of nicotinic receptors that bind nicotine, appears to reduce anxiety. (sciencedaily.com)
Nicotine acts like a key that unlocks nicotine receptors in the brain. (sciencedaily.com)
Usually that key opens the receptor, but at other times nicotine is like a key that has gotten broken inside of the lock. (sciencedaily.com)
Our findings suggest that low-dose nicotine may block a specific subtype of receptor from opening that is important for regulating anxiety behavior," she said, adding that anxiety is a major reason why people relapse to smoking. (sciencedaily.com)
The rewarding effects of nicotine are mediated through the activation of the mesolimbic dopamine pathway. (helsinki.fi)

Acetylcholine Carbachol Suxamethonium α-Bungarotoxin α-Conotoxin Hexamethonium Pancuronium Tubocurarine Nicotinic acetylcholine receptor Ganglion type nicotinic receptor Rang HP, Dale MM, Ritter JM, Moore PK, et al. (wikipedia.org)
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)

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

Expressing M1 receptor in knockout cells restored carbachol-induced α-secretase processing. (alzforum.org)
5. Block of carbachol activation of muscarinic receptors with atropine (10 μM) abolished the elevation of [Ca 2+ ](i) by the opioids. (edu.au)

G protein-coupled receptors (GPCR) have recently been implicated in intracellular crosstalk pathways with IR. (mdpi.com)
2019). In the last decades, it was widely demonstrated how these two pivotal determinants of human pathologies are strongly associated with each other in a dual relationship where aging induces a pro-inflammatory state in the organism and inflammation, in turn, leads to the activation of cellular and molecular pathways involved in cell senescence and aging (Chung et al. (researchgate.net)

Skok VI: Nicotinic acetylcholine receptors in autonomic ganglia. (spandidos-publications.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)
Peimine (Pm), an anti-inflammatory compound from Fritillaria , is known to inhibit some voltage-dependent ion channels and muscarinic receptors, but its interaction with ligand-gated ion channels remains unexplored. (mdpi.com)

Suchankova P, Engel JA , Jerlhag E. Sub-chronic Ghrelin Receptor Blockade Attenuates Alcohol- and Amphetamine-Induced Locomotor Stimulation in Mice. (neurotree.org)

DA neuron activation lags behind GABA neurons and is dependent on scratching of the itchy site. (iasp-pain.org)

Responses were compared with those in mice deficient in the cold/menthol receptor, TRPM8, expressed in trigeminal sensory neurons innervating the oral cavity. (bmj.com)
Allan Levey and colleagues at Emory University, Atlanta, Georgia, have now used knockout mice to show that the M1 receptor is responsible for regulating APP processing in vivo. (alzforum.org)

The integration of GPCR and receptor tyrosine kinase (RTK) signaling, including IR upon ligand stimulation, is eloquently reviewed. (mdpi.com)

It is thus of great interest to understand at the molecular level how the action of ACh on its receptors eventually leads to changes in system-level functions. (springer.com)
Using genetic strategies, they are attempting to determine the specific molecular make-up of the nicotinic receptors that regulate anxiety. (sciencedaily.com)

Structural Diversity and Dynamics of Human Three-Finger Proteins Acting on Nicotinic Acetylcholine Receptors. (nih.gov)

Nicotinic acid adenine dinucleotide phosphate (NAADP) is the most potent Ca(2+)-mobilizing intracellular messenger and is linked to a variety of stimuli and cell surface receptors. (ox.ac.uk)

Functional interaction between Lypd6 and nicotinic acetylcholine receptors. (nih.gov)
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)

Our results provide insight for the further development of nicotinic therapeutics and will be useful to direct future experiments with protein structure-based modeling and site-directed mutagenesis. (aspetjournals.org)

G protein stoichiometry can dictate biased agonism through distinct receptor-G protein partitioning. (mdpi.com)

Intriguingly, our results showed that EA stimulation at the Zusanli (ST36) acupoint activated α7 nicotinic acetylcholine receptor (α7nAchR) in lung tissue mainly through the sciatic nerve and cervical vagus nerve, thus exerting anti-ferroptosis and pulmonary protective effects. (figshare.com)

Thus, in SH-SY5Y cells, opioids can mobilize Ca 2+ from intracellular stores but they require ongoing muscarinic receptor activation. (edu.au)

An upregulation of IR expression and its activation is significantly associated with higher downstream G protein signaling cascades. (mdpi.com)
The muscarinic acetylcholine receptor has been a target for AD therapies for decades, based first on the loss of acetylcholine in the disease and the role of M1 receptors in memory and cognition, and then on the finding that the receptors control the processing of amyloid precursor protein to Aβ peptides. (alzforum.org)
Background As carcinoma progresses, the stroma undergoes a variety of phenotypic changes, including the presence of carcinoma-associated fibroblasts (CAFs) that express fibroblast activation protein (FAP). (hoot4owls.org)

Direct activation of PVA neurons using optogenetics and pharmacological approaches were sufficient to induce persistent mechanical hyperalgesia in naive animals. (iasp-pain.org)

Preclinical data suggests inactivation of a specific sub-class of nicotinic receptors may be an effective strategy to help smokers quit without feeling anxious, according to researchers. (sciencedaily.com)

The ecto-enzyme CD38 is a nicotinic acid adenine dinucleotide phosphate (NAADP) synthase that couples receptor activation to Ca2+ mobilization from lysosomes in pancreatic acinar cells. (ox.ac.uk)

Since receptor activation occurs as isolated bursts, it has been proposed that the receptors have a very low channel‐opening rate constant when bound to TEA. (wikipedia.org)
Metabolic activation occurs predominantly in the liver. (cdc.gov)

We propose that CD38 is an NAADP synthase required for coupling receptor activation to NAADP-mediated Ca(2+) release from lysosomal stores in pancreatic acinar cells. (ox.ac.uk)

Several signaling molecules have been identified as critical players in the regulation of insulin-induced IR activation. (mdpi.com)

Hone AJ and McIntosh JM: Nicotinic acetylcholine receptors in neuropathic and inflammatory pain. (spandidos-publications.com)
Lipid mediators contribute to inflammation providing both pro-inflammatory signals and terminating the inflammatory process by activation of macrophages. (hoot4owls.org)

In the naïve state, the level of Gα expression influences the partitioning of not only Gα but also the co-expressed receptor in different membrane domains. (mdpi.com)

Analysis of the effects of incorporation of mutant and chimeric subunits also permitted identification of sequence elements important in receptor activation. (aspetjournals.org)

Anatomy33

Organisms12

Diseases4

Chemicals and Drugs97

Analytical, Diagnostic and Therapeutic Techniques and Equipment8

Psychiatry and Psychology7

Phenomena and Processes20

Disciplines and Occupations1

Information Science2

Health Care1

NAChR10

Agonist8

Inhibition4

Antagonist7

Acetylcholine receptor subunit1

NAChRs7

Cholinergic3

Selective5

Antagonists4

Neuromuscular5

Subtypes3

Pharmacology1

Opioid4

Nicotine10

Ganglion2

Antagonism1

Carbachol2

Pathways2

Autonomic1

Inhibit2

Blockade1

GABA1

Mice2

Ligand1

Molecular2

Structural1

Potent1

Functional2

Therapeutics1

Distinct1

Stimulation1

Intracellular1

Protein3

Neurons1

Inactivation1

Mobilization1

Occurs2

Pancreatic1

Regulation1

Inflammatory2

Membrane1

Effects1