• As well as the endogenous agonist acetylcholine, agonists of the nAChR include nicotine, epibatidine, and choline. (wikipedia.org)
  • Incorporation of unnatural amino acids into two acetylcholine receptors-the nicotinic acetylcholine receptor (nAChR) and the M₂ muscarinic acetylcholine receptor (M₂AChR)-and an electrophysiology assay of receptor function were performed in each of the studies. (caltech.edu)
  • The nAChR is a ligand-gated ion channel (LGIC) and the M₂AChR is a G-protein-coupled receptor (GPCR). (caltech.edu)
  • The α7 nicotinic acetylcholine receptor (α7 nAChR) negatively regulates the synthesis and release of pro-inflammatory cytokines by immune cells. (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)
  • Changes in nicotinic acetylcholine receptor (nAChR) subunit composition may alter electrophysiologic, pharmacologic, and metabolic characteristics of the receptor inducing hyperkalemia on exposure to succinylcholine. (druglib.com)
  • Across evolution nociceptors express subunits of the nicotinic acetylcholine receptor (nAChR) family, a family of ACh-gated ion channels. (huji.ac.il)
  • Here we asked the question whether fluorescence labelled small molecule agonists of the α7 nicotinic acetylcholine receptor (nAChR) might be identified to enhance receptor studies. (unibe.ch)
  • Using patch-clamp recording of human α6*-nicotinic acetylcholine receptor (α6*-nAChR) function when heterologously expressed in SH-EP1 human epithelial cells, we found that 0.1-5 mM EtOH significantly enhances α6*-nAChR-mediated currents with effects that are dependent on both EtOH and nicotine concentrations. (arizona.edu)
  • Naturally expressed nicotinic acetylcholine receptors composed of α4 and β2 subunits (α4β2-nAChR) are the predominant form of high affinity nicotine binding site in the brain implicated in nicotine reward, mediation of nicotinic cholinergic transmission, modulation of signaling through other chemical messages, and a number of neuropsychiatric disorders. (barrowneuro.org)
  • The CHRNB2 gene provides instructions for making one part (subunit) of a larger protein called a neuronal nicotinic acetylcholine receptor (nAChR). (medlineplus.gov)
  • CHRNB2 mutations make nAChR channels more sensitive to the neurotransmitter acetylcholine, allowing the channels to open more easily than usual. (medlineplus.gov)
  • Fetal brain regions and peripheral tissues were examined for nAChR subtypes, other neurotransmitter receptors, and indices of cell signaling and cell damage. (nature.com)
  • Bionomics has a long-standing collaboration with MSD to identify novel α7 nAChR PAMs suitable for the treatment of cognitive disorders that address the limitations seen with nAChR agonists, such as lack of selectivity against related ligand-gated ion channels, desensitization of the receptor with sustained exposure, and an inverted U-shaped dose response function," said Spyros Papapetropoulos, M.D., Ph.D., President and CEO of Bionomics. (bionomics.com.au)
  • Though the nicotinic acetylcholine receptor (nAChR) subunits α9 and α 10 have been thoroughly characterized within hair cells of the organ of Corti in the inner ear, prior studies have shown that they are also expressed in lymphocytes. (johnshopkins.edu)
  • Several nicotinic acetylcholine receptor (nAChR) subtypes are expressed in mitochondria to regulate the internal pathway of apoptosis in ion channel-independent manner. (okstate.edu)
  • The neuronal subtypes are various homomeric (all one type of subunit) or heteromeric (at least one α and one β) combinations of twelve different nicotinic receptor subunits: α2−α10 and β2−β4. (wikipedia.org)
  • In neuronal nAChRs, the binding site is located at the interface of an α and a β subunit or between two α subunits in the case of α7 receptors. (wikipedia.org)
  • We demonstrated an incorporation of two alpha 3 subunits in approximately 98% of plasma membrane receptor pentamers, indicating a 2/3 subunit expression ratio of alpha 3 to beta 4 alone or to coexpressed beta 4 and alpha 5. (rti.org)
  • Whereas alpha 5 subunit expression decreased the cell calcium response to nicotine and reduced plasma membrane receptor number, it partially protected receptors from nicotine mediated desensitization. (rti.org)
  • Conversely, the 13′ residue of the β4 subunit M2 region is important in determining acetylcholine potency, indicating a role for this residue in agonist binding/gating processes. (aspetjournals.org)
  • Effects of thujone, a major ingredient of absinthe, wormwood oil and some herbal medicines, were tested on the function of α7 subunit of the human nicotinic acetylcholine (α7 nACh) receptor expressed in Xenopus oocytes using the two-electrode voltage-clamp technique. (chapman.edu)
  • In the present study, we used FISH to determine which neuronal types express the most prevalent beta2 nicotinic subunit in the mouse striatum. (cas.cz)
  • Surprisingly though, cholinergic interneurons were identified as a population with the highest expression of beta2 nicotinic subunit. (cas.cz)
  • The protein encoded by this gene is a nicotinic acetylcholine receptor subunit and a member of a superfamily of ligand-gated ion channels that mediate fast signal transmission at synapses. (nih.gov)
  • The effect of the endogenous cannabinoid ligand anandamide on the function of the cloned α 7 subunit of the nicotinic acetylcholine (ACh) receptor expressed in Xenopus oocytes was investigated by using the two-electrode voltage-clamp technique. (uaeu.ac.ae)
  • 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)
  • Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. (wikipedia.org)
  • As ionotropic receptors, nAChRs are directly linked to ion channels. (wikipedia.org)
  • In muscle-type nAChRs, the acetylcholine binding sites are located at the α and either ε or δ subunits interface. (wikipedia.org)
  • 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)
  • 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)
  • In physiological and behavioral studies, activation of nicotinic acetylcholine receptors (nAChRs) has been implicated in mediating cholinergic signaling. (oregonstate.edu)
  • 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)
  • In this thesis, I have examined the role of nicotinic acetylcholine receptors (nAChRs), known molecular targets for nicotine addiction, in mediating the initial rewarding properties of alcohol. (umassmed.edu)
  • In an effort to develop selective radioligands for in vivo imaging of neuronal nicotinic acetylcholine receptors (nAChRs), we synthesized 5-iodo-3- (2(S)-azetidinylmethoxy)pyridine (5-iodo-A-85380) and labeled it with 125 I and 123 I. Here we present the results of experiments characterizing this radioiodinated ligand in vitro. (johnshopkins.edu)
  • abstract = "In an effort to develop selective radioligands for in vivo imaging of neuronal nicotinic acetylcholine receptors (nAChRs), we synthesized 5-iodo-3- (2(S)-azetidinylmethoxy)pyridine (5-iodo-A-85380) and labeled it with 125I and 123I. (johnshopkins.edu)
  • 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)
  • A large variety of nicotinic acetylcholine receptors (nAChRs) are expressed in the striatum, a brain region that is crucial in the control of behaviour. (cas.cz)
  • 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)
  • 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)
  • Bertrand S, Weiland S, Berkovic SF, Steinlein OK, Bertrand D. Properties of neuronal nicotinic acetylcholine receptor mutants from humans suffering from autosomal dominant nocturnal frontal lobe epilepsy. (medlineplus.gov)
  • Nicotinic receptors, with a molecular mass of 290 kDa, are made up of five subunits, arranged symmetrically around a central pore. (wikipedia.org)
  • In both muscle-type and neuronal-type receptors, the subunits are very similar to one another, especially in the hydrophobic regions. (wikipedia.org)
  • This protein carries anywhere from 2 to 5 acetylcholine binding sites which are located at the interface between two subunits. (proteopedia.org)
  • In this study, we describe the development of homogeneous HEK-293 cell clones of alpha 3 beta 4 and alpha 3 beta 4 alpha 5 receptors appropriate for drug screening and characterizing biochemical and pharmacological properties of incorporated alpha 5 subunits. (rti.org)
  • Clones were assessed for plasma membrane expression of the individual receptor subunits by mass spectrometry and immunochemistry, and their calcium flux was measured in the presence of a library of kinase inhibitors and a focused library of acetylcholine receptor ligands. (rti.org)
  • Hit compounds from both libraries suggest the alpha 5 and alpha 5-D398N subunits allosterically modify the behavior of nicotine at the parent alpha 3 beta 4 nicotinic acetylcholine receptor. (rti.org)
  • The developmental expression patterns of ten genes encoding nicotinic acetylcholine receptor subunits were analyzed using Northern blots and in situ hybridization in chick peripheral ganglia of neural crest, placodal and dual embryonic origin. (unige.ch)
  • Chimeric receptor subunits and site-directed mutants were used to localize sequence determinants of cocaine affinity to: 1) a region of α4 located between residues 128 and 267 and 2) a site within the pore-lining M2 domain of β4 that includes the 13′ phenylalanine residue. (aspetjournals.org)
  • Analysis of the effects of incorporation of mutant and chimeric subunits also permitted identification of sequence elements important in receptor activation. (aspetjournals.org)
  • For α3-containing receptors, a region or regions contained within the N-terminal extracellular domain of neuronal β subunits influence the time course of responses to acetylcholine. (aspetjournals.org)
  • Abstract Muscle nicotinic acetylcholine receptors are a class of heteropentameric ligand-gated cation channels with constituent subunits adopting a fixed stoichiometric arrangement. (ox.ac.uk)
  • These receptors are thought to be heteropentamers composed of separate but similar subunits. (nih.gov)
  • 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)
  • These results clearly demonstrate the presence of these nicotinic receptor subunits within several populations of human lymphocytes, implicating their role in the immune response. (johnshopkins.edu)
  • Nicotinic receptors also respond to drugs such as the agonist nicotine. (wikipedia.org)
  • Several different terms are used to refer to the molecules that bind receptors, such as ligand, agonist, or transmitter. (wikipedia.org)
  • 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)
  • After a reliable means to assay M₂AChR function was found, we performed a preliminary search for tryptophan residues in the agonist binding site that form a cation-pi interaction with acetylcholine. (caltech.edu)
  • Furthermore, functional differences observed in α 2 δ 2 β receptors can be rationalized by changes in dynamical behavior that manifest themselves at the agonist binding site. (ox.ac.uk)
  • Coniine has direct effects on nicotinic (cholinergic) receptors, both agonist and antagonist. (medscape.com)
  • It is an agonist at both muscarinic and nicotinic acetylcholine receptors. (bvsalud.org)
  • 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)
  • In competition studies, nicotinic agonists were more than 1000 times more potent than ganglionic and neuromuscular blocking drugs in displacing [ 3 H]acetylcholine binding. (northwestern.edu)
  • The paper Fluorescent Agonists of the α7 Nicotinic Acetylcholine Receptor Derived from 3-Amino-Quinuclidine has been accepted for publication by Helvetica Chemica Acta. (unibe.ch)
  • H-EBDN binding competition studies reveal high affinity for nicotinic agonists and lower affinity for nicotinic antagonists. (barrowneuro.org)
  • 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)
  • Nicotinic receptors get their name from nicotine which does not stimulate the muscarinic acetylcholine receptors but selectively binds to the nicotinic receptors instead. (wikipedia.org)
  • The principle side binding nicotine with a high degree of specificity and the complimentary side binding a wide variety of acetylcholine like molecules. (proteopedia.org)
  • Nicotinic acetylcholine receptors regulate the nicotine dependence encountered with cigarette smoking, and this has stimulated a search for drugs binding the responsible receptor subtypes. (rti.org)
  • Studies link a gene cluster encoding for alpha 3 beta 4 alpha 5-D398N nicotinic acetylcholine receptors to lung cancer risk as well as link a second mutation in this cluster to an increased risk for nicotine dependence. (rti.org)
  • With prolonged nicotine exposure, the plasma membrane expression of receptors with and without incorporated alpha 5 increased. (rti.org)
  • Activation of α2A-containing nicotinic acetylcholine receptors mediates nicotine-induced motor output in embryonic zebrafish. (oregonstate.edu)
  • Cytisine and (-)-nicotine had the highest affinity (K(I) = 1-6 nM) for the [ 3 H]acetylcholine binding site. (northwestern.edu)
  • Cytisine and (-)-nicotine had the highest affinity (K(I) = 1-6 nM) for the [3H]acetylcholine binding site. (northwestern.edu)
  • Anandamide decreased the maximal nicotine-induced responses without significantly affecting its potency, indicating that it acts as a noncompetitive antagonist on nicotinic acetylcholine (nACh) a 7 receptors. (uaeu.ac.ae)
  • 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)
  • The muscarinic acetylcholine receptor likewise gets its name from a chemical that selectively attaches to that receptor - muscarine. (wikipedia.org)
  • 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)
  • Bionomics is advancing its lead drug candidate, BNC210, an oral, proprietary, selective negative allosteric modulator of the α7 nicotinic acetylcholine receptor, for the acute treatment of Social Anxiety Disorder (SAD) and chronic treatment of Post-Traumatic Stress Disorder (PTSD). (bionomics.com.au)
  • See also Binding site of AChR and Acetylcholine Receptor and its Reaction to Cobra Venom . (proteopedia.org)
  • Since the muscle nicotinic acetylcholine receptor (AChR) has been the model for studying structure-function relationships of LGICs, we analyzed the action of tricyclic antidepressants on this type of AChR at both single-channel and macroscopic current levels. (uchile.cl)
  • The US Food and Drug Administration (FDA) has approved efgartigimod ( Vyvgart , argenx), a first-in-class, targeted therapy for adults with generalized myasthenia gravis (gMG) who test positive for the antiacetylcholine receptor (AChR) antibody. (medscape.com)
  • Tests to detect serum ganglionic nicotinic acetylcholine receptor antibody alpha-3 (anti-ganglionic AChR [α3-AChR ] antibody) may be done. (msdmanuals.com)
  • The nicotinic receptors are cylindrically-shaped proteins imbedded in synaptic walls that act as chemically-controlled sodium channels (also called ligand-gated sodium channels) that penetrate through the cell walls of post-synaptic nerves and myocytes at the skeletal neuromuscular junctions. (cdc.gov)
  • Since channel opening is triggered by the attachment of a chemical (or "ligand") - in this case, acetylcholine - these channels are called chemical- or ligand-gated channels . (cdc.gov)
  • The receptor acts as a chemically controlled sodium (Na) channel also known as a ligand gated channel . (proteopedia.org)
  • A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family . (online-medical-dictionary.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)
  • α7 nicotinic ACh receptors as a ligand-gated source of Ca(2+) ions: the search for a Ca(2+) optimum. (bvsalud.org)
  • In addition, inhibition of nicotinic responses by anandamide was not sensitive to either pertussis toxin treatment or to the membrane permeable cAMP analog 8-Br-cAMP (0.2 mM). (uaeu.ac.ae)
  • Inhibitors of enzymes involved in anandamide metabolism including phenylmethylsulfonyl fluoride, superoxide dismutase, and indomethacin, or the anandamide transport inhibitor AM404 did not prevent anandamide inhibition of nicotinic responses, suggesting that anandamide itself acted on nicotinic receptors. (uaeu.ac.ae)
  • In conclusion, these results demonstrate that the endogenous cannabinoid anandamide inhibits the function of nACh α 7 receptors expressed in Xenopus oocytes in a cannabinoid receptor-independent and non-competitive manner. (uaeu.ac.ae)
  • When the neurotransmitter, acetylcholine, attaches to the portion of the nicotinic receptor outside of the cell wall, it induces a conformational change that selectively opens up the channel to sodium ions. (cdc.gov)
  • For those interested in learning about the molecular physiology of nicotinic receptors, the subject is discussed as optional reading below. (cdc.gov)
  • 3. Adcock C, Smith GR, Sansom MS. The nicotinic acetylcholine receptor: from molecular model to single-channel conductance. (proteopedia.org)
  • In vertebrates, nicotinic receptors are broadly classified into two subtypes based on their primary sites of expression: muscle-type nicotinic receptors and neuronal-type nicotinic receptors. (wikipedia.org)
  • The nicotinic receptors are considered cholinergic receptors, since they respond to acetylcholine. (wikipedia.org)
  • On the basis of its ability to bind to nicotinic cholinergic receptors in electric tissue and at the neuromuscular junction, α-bungarotoxin has been widely used to identify central nicotinic receptors. (northwestern.edu)
  • However, the suitability of this ligand as a probe for nicotinic cholinergic receptors in the central nervous system has been questioned. (northwestern.edu)
  • In the presence of a cholinesterase inhibitor to prevent hydrolysis and atropine to block muscarinic cholinergic receptors, [ 3 H]acetylcholine bound rapidly, reversibly, and with high affinity to rat brain membranes (K(D) = 12.3 ± 0.8 nM, B(max) = 4.6 ± 0.1 pmoles/g of tissue). (northwestern.edu)
  • In the peripheral nervous system: (1) they transmit outgoing signals from the presynaptic to the postsynaptic cells within the sympathetic and parasympathetic nervous system, and (2) they are the receptors found on skeletal muscle that receive acetylcholine released to signal for muscular contraction. (wikipedia.org)
  • Most patients with gMG have immunoglobulin G (IgG) antibodies, which are most often directed against skeletal muscle nicotinic acetylcholine receptors. (medscape.com)
  • Since nicotinic receptors help transmit outgoing signals for the sympathetic and parasympathetic systems, nicotinic receptor antagonists such as hexamethonium interfere with the transmission of these signals. (wikipedia.org)
  • Thus, for example, nicotinic receptor antagonists interfere with the baroreflex that normally corrects changes in blood pressure by sympathetic and parasympathetic stimulation of the heart. (wikipedia.org)
  • Nicotinic antagonists that block the receptor include mecamylamine, dihydro-β-erythroidine, and hexamethonium. (wikipedia.org)
  • Further experiments in SH-EP1 cells expressing human α7 nACh receptor indicated that thujone suppressed choline induced Ca2+ transients in a concentration-dependent manner. (chapman.edu)
  • 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)
  • 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)
  • Acetylcholine is an important modulator of striatal activity, and it is vital to controlling striatal-dependent behaviours, including motor and cognitive functions. (cas.cz)
  • Collectively, our results indicate that thujone inhibits the function of the α7-nACh receptor and impairs cellular and behavioral correlates of cholinergic modulation of learning and memory. (chapman.edu)
  • Thus, the small population of nicotinic receptors represents an interesting target for modulation of response to stimulant drugs and other striatal-based behaviour. (cas.cz)
  • Identify the key physiological effects that result from stimulation of nicotinic receptors by excessive amounts of acetylcholine. (cdc.gov)
  • 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)
  • 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)
  • 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)
  • Immunohistochemical staining of rat dorsal root ganglion (DRG) frozen sections using Anti-Nicotinic Acetylcholine Receptor β4 (CHRNB4) (extracellular)-ATTO Fluor-594 Antibody (#ANC-014-AR), (1:100). (alomone.com)
  • As reported by Medscape Medical News, efgartigimod was effective and well-tolerated in the phase 3, randomized, placebo-controlled ADAPT trial, which enrolled 187 adults with gMG regardless of acetylcholine receptor antibody status. (medscape.com)
  • Guyton and Hall 2006) (See Figure 6 below) ( Smooth muscle contraction is controlled by muscarinic receptors, which are different and will be discussed later. (cdc.gov)
  • Acetylcholine itself binds to both muscarinic and nicotinic acetylcholine receptors. (wikipedia.org)
  • The novel agent binds to the neonatal Fc receptor (FcRn), which is widely expressed throughout the body and plays a central role in rescuing IgG antibodies from degradation. (medscape.com)
  • Nicotinic AChRs may exist in different interconvertible conformational states. (wikipedia.org)
  • A Novel Vaccine Employing Non-Replicating Rabies Virus Expressing Chimeric SARS-CoV-2 Spike Protein Domains: Functional Inhibition of Viral/Nicotinic Acetylcholine Receptor Complexes. (cdc.gov)
  • When in the presence of acetylcholine , the receptor undergoes a conformational change opening up the channel to an influx of sodium (Na) within the cell. (proteopedia.org)
  • However, a lack of demonstrated response to applied acetylcholine using standard single-cell recording techniques suggests a physiology different than that seen in hair cells of the inner ear. (johnshopkins.edu)
  • A series of N,N-disubstituted piperazines were prepared and evaluated for binding to α4β2 * and α7 * neuronal nicotinic acetylcholine receptors using rat striatum and whole brain membrane preparations, respectively. (uky.edu)
  • These channels open when attached to a brain chemical (neurotransmitter) called acetylcholine. (medlineplus.gov)
  • 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)
  • 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)
  • This channel also contributes to the receptor function in three critical aspects: it contains a gating mechanism, it contains a water pore to stabilize ions, and it has a selectivity filter for ion charge. (proteopedia.org)
  • The receptor is a transmembrane pentameric glycoprotein. (proteopedia.org)
  • As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric [(α3) m (β4) n where m + n = 5]. (wikipedia.org)