• 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)
  • Levin ED, Bettegowda C, Blosser J and Gordon J: AR-R17779, and alpha7 nicotinic agonist, improves learning and memory in rats. (spandidos-publications.com)
  • The agonist ligand nicotine shows an up to 30-fold higher affinity to nACHRs than acetylcholine (ACh). (biomedcentral.com)
  • 3-Bromocytisine is a potent agonist of α 4 β 4, α 4 β 2 and α 7 nACh receptors (IC 50 values are 0.28, 0.30 and 31.6 nM respectively). (tocris.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)
  • This double-blind, placebo-controlled crossover study in two adult patients investigated whether an investigational receptor-specific partial agonist drug would increase the inhibitory functions of the gene and thereby increase patients' attention. (epiphanyasd.com)
  • However, literature shows that nicotine, a pharmacological agonist of these receptors, promotes a reduction in body weight and food intake. (fapesp.br)
  • Hence, recent studies have investigated the role of acetylcholine, the physiological agonist of these receptors, in controlling central energy homeostasis. (fapesp.br)
  • Methods: The expression of neuropeptides involved in homeostasis regulation will be assessed in vitro after treatment with the agonist and the antagonist of the ±7nAChR receptor and with leptin. (fapesp.br)
  • Some of the animals will undergo intracerebroventricular injection of ±7nAChR receptor agonist, antagonist and siRNA and will also be treated with leptin. (fapesp.br)
  • Nicotinic acetylcholine receptors are ligand-gated ion channels, a large family of multimeric membrane-bound proteins that open an ionic channel when the appropriate agonist binds. (northeastern.edu)
  • Novel biotinylated phenyl-arsonous acids as bifunctional reagents for spatially close thiols: studies on reduced antibodies and the agonist binding site of reduced Torpedo nicotinic receptors. (northeastern.edu)
  • Using saccharin as a taste stimulus in a taste preference paradigm, we examined the effects of injecting the GABA A receptor agonist muscimol or the GABA A receptor antagonist bicuculline into the IC or NBM during learning or retrieval of an appetitive taste memory on taste preference in male Sprague Dawley rats. (jneurosci.org)
  • TC-5619: an alpha7 neuronal nicotinic receptor-selective agonist that demonstrates efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia. (guidetopharmacology.org)
  • A randomized exploratory trial of an α-7 nicotinic receptor agonist (TC-5619) for cognitive enhancement in schizophrenia. (guidetopharmacology.org)
  • Laboratory studies show that SLURP-1 can bind to nicotinic acetylcholine receptors (nAChRs). (medlineplus.gov)
  • SLURP-1 specifically interacts with the alpha7 (α7) subunit, which is a piece of some nAChRs. (medlineplus.gov)
  • Several investigators could demonstrate that the SARS-CoV-2 related spike glycoprotein (SGP) attaches not only to ACE-2 receptors but also shows DNA sections highly affine to nicotinic acetylcholine receptors (nAChRs). (biomedcentral.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)
  • GABAergic interneurons in the CA1 subregion of the hippocampus expressed functional α7β2-nAChRs, which were characterized by relatively slow whole-cell current kinetics, pharmacological sensitivity to dihydro-β-erythroidine (DHβE), a nAChR β2* subunit selective blocker, and α7 and β2 subunit interaction using immunoprecipitation assay. (biomedcentral.com)
  • Part of the work will be devoted to studying the interaction of these compounds with nicotinic acetylcholine receptors (nAChRs). (sfbi.fr)
  • Information on the three-dimensional structure of the binding site is available, notably for the alpha7 isotype of the human nAChR ( 1 ) ( Figure 1 ), and in the case of a model of the extracellular binding domain of nAChRs, AChBP (Acetylcholine Binding Protein) cocrystallized with several neonicotinoids. (sfbi.fr)
  • In addition to the bee nAChRs, the alpha4beta2 rat receptors will be modeled in order to rationalize the electrophysiology measurements performed at the University of Orleans. (sfbi.fr)
  • This information will allow us to estimate the binding energies of each neonicotinoid to the targeted nAChRs and to establish a relative ranking of these insecticides for these receptors. (sfbi.fr)
  • RT-PCR was used to show that the beta3 and alpha2 subunit RNAs were present in zebrafish embryos only 2-5hours post-fertilization (hpf) while alpha7 subunit RNA was not detected until 8hpf, supporting the differential regulation of nAChRs during development. (zfin.org)
  • Nicotinic acetylcholine receptors (nAChRs) have long been considered to solely mediate neurotransmission. (bvsalud.org)
  • Cahill K, Stead LF, Lancaster T . Nicotine receptor partial agonists for smoking cessation. (nature.com)
  • It is known that α7 nicotinic acetylcholine receptor (α7 nAChR) agonists can correct the impaired P50 gating. (epiphanyasd.com)
  • Alpha7-nicotinic receptor agonists, currently the target of drug development in schizophrenia and Alzheimer Disease, may also have positive clinical effects in autism spectrum disorder. (epiphanyasd.com)
  • Extended exposure to nicotinic agonists causes increased surface expression (up-regulation) of many nicotinic receptor subtypes, a phenomenon that has been implicated in the addictive property of nicotine. (northeastern.edu)
  • Multiple subunits for nicotinic acetylcholine receptors exist in neurons, and different combinations of subunits can assemble into many different functional receptor subtypes. (northeastern.edu)
  • Transfections with a reporter gene under the control of the alpha7 promoter demonstrated that a sharp developmental divide occurred at E11-12, after which stage the promoter was activatable in neurons exclusively. (unige.ch)
  • A major thrust of my laboratory is to determine the composition and function of neuronal nicotinic receptor subtypes and what regulates their expression in neuronal tissues. (northeastern.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)
  • Association of the neuronal nicotinic receptor beta2 subunit gene (CHRNB2) with subjective responses to alcohol and nicotine. (nature.com)
  • Zaveri N, Jiang F, Olsen C, Polgar W and Toll L: Novel α3β4 nicotinic acetylcholine receptor-selective ligands. (spandidos-publications.com)
  • We conclude that using an image-derived input function for kinetic modeling of nicotinic PET ligands provides suitable results compared to reference tissue-based methods and that the chemical properties of 2-FA and Nifene are suitable to study receptor response to nicotine addiction and smoking cessation therapies. (bvsalud.org)
  • Abnormalities in CHRNA7, the alpha7-nicotinic receptor gene, have been reported in autism spectrum disorder. (epiphanyasd.com)
  • The monomeric form binds with high affinity to muscular and neuronal alpha-7/CHRNA7 nicotinic acetylcholine receptors (nAChR). (snakevenomdb.org)
  • Here we report that the nicotinic acetylcholine receptor alpha7 subunit is required for acetylcholine inhibition of macrophage TNF release. (bioseek.eu)
  • Our previous research confirmed that electroacupuncture (EA) stimulus elicits neuroprotective effects against cerebral ischemic injury through α7 nicotinic acetylcholine receptor (α7nAChR)-mediated inhibition of high-mobility group box 1 release mechanism. (biomedcentral.com)
  • Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission. (drugbank.com)
  • BMP receptor blockade overcomes extrinsic inhibition of remyelination and restores neurovascular homeostasis. (neurotree.org)
  • Cholinergic signaling is mediated by activation of muscarinic and nicotinic receptors and has been described in the literature as a classical and important signaling in the regulation of inflammatory response. (fapesp.br)
  • structural organization of an nAChR a) overview showing, from top to bottom, the extracellular, transmembrane and intracellular domains, b) detail showing the ligand binding zone, located at the interface of subunits of the extracellular domain. (sfbi.fr)
  • RESULTS: alpha7 and gamma nAChR genes were significantly upregulated in burn patients, whereas alpha1 and epsilon nAChR genes were minimally affected, showing no significant changes over time. (druglib.com)
  • Because gene expression is the basis of protein production, the upregulation of alpha7 and gamma genes might translate into more alpha7 and gamma protein subunits. (druglib.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)
  • Resequencing of nicotinic acetylcholine receptor genes and association of common and rare variants with the Fagerström test for nicotine dependence. (nature.com)
  • 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)
  • The superior cervical and ciliary ganglia were investigated in detail because they accumulated relatively abundant transcripts of the alpha3, beta4, alpha5 and alpha7 genes. (unige.ch)
  • Electrical stimulation of the vagus nerve inhibits TNF synthesis in wild-type mice, but fails to inhibit TNF synthesis in alpha7-deficient mice. (bioseek.eu)
  • 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)
  • 0.05) decreased mRNA and protein expression of retinoic acid signaling pathway elements, including retinoic acid receptor alpha and retinoic acid receptor beta, with the greatest number of changes observed between postnatal days 3-5. (biomedcentral.com)
  • however, the identity of the essential macrophage acetylcholine-mediated (cholinergic) receptor that responds to vagus nerve signals was previously unknown. (bioseek.eu)
  • Thus, the nicotinic acetylcholine receptor alpha7 subunit is essential for inhibiting cytokine synthesis by the cholinergic anti-inflammatory pathway. (bioseek.eu)
  • These cells express nicotinic acetylcholine receptors, with the α7-nAChR being extensively studied due to its involvement in activating the cholinergic anti-inflammatory pathway. (bvsalud.org)
  • Nicotinic acetylcholine receptor gene expression is altered in burn patients. (druglib.com)
  • Gene expression of the nAChR subunits alpha1, alpha7, gamma, and epsilon were performed using real-time reverse transcriptase polymerase chain reaction. (druglib.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)
  • No studies have been performed that show the upregulation and/or alteration of nAChR subunit composition in human burn patients. (druglib.com)
  • It displays the differences in expression of each nAChR subunit between normal and cancer cells for selected cancer types, highlighting their possible involvement in specific cases. (bvsalud.org)
  • 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)
  • Below we discuss the role of early neurotransmitters and their receptors prior to the formation of circuits that mediate vision. (org.es)
  • α4β2 Nicotinic Receptors Partially Mediate Anti-Inflammatory Effects through Janus Kinase 2 (JAK2) - Signal Transducer and Activator of Transcription 3 (STAT3) but Not Calcium or cAMP Signaling. (northeastern.edu)
  • The understanding of the toxicity of these insecticides requires the characterization of their lipophilicity, an essential parameter to understand their effect on the cellular membrane system, and the precise description of their interactions with their target receptors. (sfbi.fr)
  • The effect of thermal injury on nAChR gene subunits can be studied using a minimally invasive method (buccal mucosal scraping) and a highly sensitive technology (real-time reverse transcriptase polymerase chain reaction) obviating the need for more invasive methods. (druglib.com)
  • Amphetamine enantiomers inhibit homomeric α7 nicotinic receptor through a competitive mechanism and within the intoxication levels in humans. (nachrs.org)
  • Gene regulation of α4β2 nicotinic receptors: Microarray analysis of nicotine-induced α4β2 up-regulation and anti-inflammatory effects. (northeastern.edu)
  • Ginkgolide B is normally a powerful antagonist from the platelet-activating aspect receptor. (bioinf.org)
  • Receptor-mediated tobacco toxicity: alterations of the NF-kappaB expression and activity downstream of alpha7 nicotinic receptor in oral keratinocytes. (famri.org)
  • In addition, mice in which the receptor gene for TNFα has been knocked out are resistant to alcohol-induced liver injury[ 5 ]. (wjgnet.com)
  • Time-activity curves of the left ventricle of the heart displayed similar distribution across wild type mice, mice lacking the ß2-subunit for ligand binding, and acute nicotine-treated mice, whereas reference tissue binding displayed high variation between groups. (bvsalud.org)
  • The presence of ±7nAChR receptor in energy homeostasis regulatory cells (POMC and NPY) will be evaluated by immunofluorescence of brain slices of male swiss mice. (fapesp.br)
  • 2009 ) and regulate the Reperfusion Injury Salvage Kinase (RISK) signaling pathway (ERKε, PKC, GSK-3β, STAT3) via cannabinoid receptor 1 (CB1R)(Wang et al. (biomedcentral.com)
  • We are investigating how nicotinic receptors affect STAT3 and NFkB signaling in nicotine-mediated anti-inflammatory effects. (northeastern.edu)
  • Metharbital binds at a distinct binding site associated with a Cl - ionopore at the GABA A receptor, increasing the duration of time for which the Cl - ionopore is open. (drugbank.com)
  • PubChem]Hexobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABA-A receptor, increasing the duration of time for which the Cl- ionopore is open. (t3db.ca)
  • The SARS-CoV-2 spike protein binds and modulates estrogen receptors. (medicatrix.be)
  • Nicotinic receptor modulation. (inra.fr)
  • 2018 ). NLRP3 inflammasome is composed of NLRP3 (nucleotide-binding oligomerization domain (NOD)-like receptor (NLR) pyrin domain-containing 3), ASC (apoptosis-associated speck-like protein containing a caspase recruitment domain) and procaspase-1, subsequently amplifying the production and secretion of proinflammatory cytokines, apoptotic and pyroptotic cell deaths(Zhong et al. (biomedcentral.com)
  • In addition, the alpha7 nicotinic receptor protein is heterologously expressed in almost all cell types in culture but only folds and forms a functional receptor in very few. (northeastern.edu)
  • Like other Ly6/uPAR-related proteins, SLURP-1 folds into a particular shape and is thought to attach (bind) to other proteins called receptors to carry out signaling within cells. (medlineplus.gov)
  • Positron emission tomography (PET) radioligands that bind with high-affinity to α4ß2-type nicotinic receptors (α4ß2Rs) allow for in vivo investigations of the mechanisms underlying nicotine addiction and smoking cessation. (bvsalud.org)
  • Aprobarbital also appears to bind neuronal nicotinic acetylcholine receptors. (illumina.com)
  • Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. (illumina.com)
  • In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. (illumina.com)
  • GABA A receptor agonism and antagonism had opposite effects on cortical ACh levels in novel taste presentation versus familiar taste recognition and ACh levels were associated with the propensity to acquire or retrieve a taste memory. (jneurosci.org)
  • GABA A receptors must be inactive during novel tasting to enable new memory formation, but must be active and inhibiting acetylcholine release in the cortex to allow memory retrieval. (jneurosci.org)
  • Through its interaction with these receptors, SLURP-1 may be involved in skin growth and development. (medlineplus.gov)
  • Studies show that animals that do not express acetylcholine in brain regions that control energy homeostasis display excessive body weight gain and hyperphagia. (fapesp.br)
  • We have also demonstrated the presence of ±7nAChR receptor in energy homeostasis regulatory cells by immunofluorescence of hypothalamic brain slices. (fapesp.br)
  • 3 beta ( GSK-3β), N-methyl-D-aspartate (NMDA) receptor, monoamine oxidases (MAOs), metal ions in the brain, 5-hydroxytryptamine (5-HT) receptors, the third subtype of histamine receptor (H 3 receptor), to phosphodiesterases (PDEs), along with a summary of their respective relationship to the disease network. (encyclopedia.pub)
  • Risk factors for depression initiate an infection-like inflammation in the brain that involves activation microglial Toll-like receptors and glycogen synthase kinase-3β (GSK3β). (mdpi.com)
  • In situ hybridization was used to localize zebrafish beta3, alpha2, and alpha7 RNA expression. (zfin.org)
  • It is also known that people with schizophrenia have less expression of this receptor in their brains than typical people. (epiphanyasd.com)
  • Our previous results have shown that ±7nAChR receptor modulates food intake by enhancing the expression of anorexigenic neuropeptides and suppressing the expression of orexigenic neuropeptides. (fapesp.br)
  • We are investigating the role of cell-line dependent factors such as Ric3 on alpha7 receptor assembly and expression. (northeastern.edu)
  • Sweileh W., Wenberg K., Xu J., Forsayeth J., Hardy S., and Loring, R.H. Multistep Expression and Assembly of Neuronal Nicotinic Receptors is Both Host-Cell and Receptor-Subtype Dependent. (northeastern.edu)
  • Several compounds that interact with these receptors have been identified as potential therapeutic agents. (bvsalud.org)
  • It has also been suggested that histamine plays a role in sensory gating via the H1 and H3 receptors. (epiphanyasd.com)
  • 0.05) decreased retinoic acid-induced binding and activation of the retinoic acid receptor response element in A549 cells. (biomedcentral.com)
  • Evidence for Alpha 7 Nicotinic Receptor Activation During the Cough Suppressing Effects Induced by Nicotine and Identification of ATA-101 as a Potential Novel Therapy for the Treatment of Chronic Cough. (guidetopharmacology.org)