During neuromuscular junction formation ACh receptors accumulate at the nerve-contact region. It has been shown that this is at least partly due to lateral migration of existing receptors in the membrane (Anderson et al., 1977). Randomly diffusing ACh receptor molecules in the membrane may be ...

Human keratinocytes synthesize and secrete non-neuronal acetylcholine, which acts as a local cell signaling molecule, regulating functions like proliferation, cell adhesion, motility, desmosomal cell contact, and glandular activity. The keratinocyte acetylcholine axis is composed of the enzymes mediating acetylcholine synthesis (acetyltransferase) and degradation (acetylcholinesterase), and two ...

Imidacloprid (IMI) is an insecticide that interferes with the transmission of stimuli in the nervous system of insects. It is neurotoxic by mimicking nicotine through its binding to the nicotinic acetylcholine receptor. In this work, experiments comprising 96 h exposure followed by 48 h in clean medium were conducted to evaluate the toxicity of IMI to Chironomus riparius and ...

be the homologof the Torpedo 87 kDa AChR-associated protein(Ervasti et al., 1990; Yoshida and Ozawa, 1990. Biochemical analysis of Torpedo electric organ postsynaptic membranessuggests a 1:l stoichiometry of ACh). ldentificationand purificationof an agrin receptor from Torpedo post- synaptic membranes:a heteromericcomplex

AbstractProtein motions in the Cys-loop ligand-gated ion receptors that govern the gating mechanism are still not well understood. The details as to how motions in the ligand-binding domain are translated to the transmembrane domain and how subunit rotations are linked to bring about the cooperative movements involved in gating are under investigation. ...

extensively investigated. In this study, we analyzed the effects of inhibiting the acetylcholinesterase (AChE of acetylcholine (ACh) release in the leech ganglion that is powerfully counteracted by endogenous AChE activity cholinergic signals on the Retzius neurons by inhibiting the acetylcholinesterase (AChE) ...

Nerve-evoked contractions were studied in vitro in phrenic nerve- hemidiaphragm preparations from strain 129X1 acetyloholinesterase knockout (AChE-/-) mice and their wild-type littermates (AChE+/+). The AChE-/- mice fail to express AChE but have normal le...

.3 Acetylcholinesterase (AChE)..........................................................................13 1.3.1 Role acetylcholine AChE acetylcholinesterase AChR acetylcholine receptor ADP,ATP adenosine diphosphate extracytoplasmicions,respectively #12;vii EeAChE Electrophorus electricus ...

A major hurdle in defining the molecular biology of nicotine addiction has been characterizing the different nicotinic acetylcholine receptor (nAChR) subtypes in the brain and how nicotine alters their function. Mounting evidence suggests that the addictive effects of nicotine, like other drugs of abuse, occur through interactions with its ...

Muscarinic acetylcholine receptors (mAChR) are glycoproteins. Experiments were conducted to determine whether active glycosylation of proteins in N4TG1 neuroblastoma cells could affect the expression of muscarinic receptors on the cell surface. The binding of radioactive N-methylscopolamine, a membrane impermeable ligand, to intact ...

Amyloid-? (A?) peptides in the brain of patients with Alzheimer's disease (AD) assemble into various aggregation forms that differ in size, structure, and functional properties. Previous studies have shown that A? binds to nicotinic acetylcholine receptors (nAChRs) and activates signaling cascades that result in the disruption of synaptic functions. These ...

The mammalian olfactory epithelium is made up of ciliated olfactory sensory neurons (OSNs), supporting cells, basal cells and microvillous cells. Previously, we reported that a population of non-neuronal microvillous cells expresses transient receptor potential channel M5 (TRPM5). Using transgenic mice and immunocytochemical labeling, we identify that these cells are ...

We have demonstrated previously that diisopropylfluorophosphate (DFP) causes a preferential loss of low spatial frequency information in the visual evoked response (VER) of the adult cat. The effect is dose related, can be reversed with atropine, is closely related to acetylcholinesterase (AChE) activity, and shows spontaneous recovery to baseline conditions over 15-20 hours ...

BackgroundPostsynaptic enrichment of acetylcholine receptors (AChRs) at the vertebrate neuromuscular junction (NMJ) depends on the activation of the muscle receptor tyrosine MuSK by neural agrin. Agrin-stimulation of MuSK is known to initiate an intracellular signaling cascade that leads to the clustering of AChRs ...

1. The ACh-activated K+ current (IK,ACh) has been investigated in guinea-pig atrial cells at 36 degrees C using the whole-cell patch-clamp technique. 2. During an exposure to ACh, IK,ACh faded as a result of desensitization. Throughout the fade of the current, the current reversed at EK and showed inward-going ...

Cholinergic neurons and nicotinic acetylcholine receptors (nAChRs) in the brain participate in diverse functions: reward, learning and memory, mood, sensory processing, pain, and neuroprotection. Nicotinic systems also have well-known roles in drug abuse. Here, we review recent insights into nicotinic function, linking exogenous and ...

BackgroundP2X₂ and nicotinic acetylcholine receptors (nAChRs) mediate fast synaptic excitation in the enteric nervous system. P2X receptors and nAChRs are functionally linked. This study examined the mechanisms responsible for interactions between P2X2 and ...

By targeting the dual active sites of acetylcholinesterase (AChE), a new series of berberine derivatives was designed, synthesized, and evaluated as AChE inhibitors. Most of the derivatives inhibited AChE in the sub-micromolar range. Compound 8c, berberine linked with phenol by a 4-carbon spacer, showed the most ...

Alpha7 neuronal nicotinic acetylcholine receptors (alpha7-nAChR) form Ca(2+)-permeable homopentameric channels modulating cortical network activity and cognitive processing. They are located pre- and postsynaptically and are highly abundant in hippocampal GABAergic interneurons. It is unclear how alpha7-nAChRs are positioned in ...

?7 neuronal nicotinic acetylcholine receptors (?7-nAChR) form Ca²⁺-permeable homopentameric channels modulating cortical network activity and cognitive processing. They are located pre- and postsynaptically and are highly abundant in hippocampal GABAergic interneurons. It is unclear how ?7-nAChRs are positioned ...

Muscarinic acetylcholine receptors (mAChRs) are drug targets for multiple neurodegenerative and neuropsychiatric disorders, but the full therapeutic potential of mAChR-targeted drugs has not been realized, mainly because of a lack of subtype-selective agonists. Recent advances have allowed the development of highly selective agonists ...

Muscarinic acetylcholine receptors (mAChRs) are drug targets for multiple neurodegenerative and neuropsychiatric disorders, but the full therapeutic potential of mAChR-targeted drugs has not been realized, mainly because of a lack of subtype-selective agonists. Recent advances have allowed the development of highly selective agonists ...

Acetylcholine (Ach) reversibly reduces the high voltage-activated (HVA) calcium (Ca) current in hippocampal neurons. Pretreatment of the cells with pertussis toxin (PTX) abolishes the Ach effect, suggesting that PTX-sensitive GTP-binding regulatory proteins (G-proteins) are involved in the signal transduction mechanism that links ...

The fundamental abnormality affecting the neuromuscular junctions of myasthenic patients is a reduction of available AChRs, due to an autoimmune attack directed against the receptors. Antibodies to AChR are present in most patients, and there is evidence that they have a predominant pathogenic role in the disease, aided by complement. ...

To further the understanding of functional ?6?5*-nicotinic acetylcholine receptors (nAChR; * indicates known or possible presence of other subunits), we have heterologously expressed in oocytes different, mouse or human, nAChR subunit combinations. Coexpression with wild-type ?5 subunits or chimeric ?5/?3 subunits (in which the human ...

Endocytosis of the nicotinic acetylcholine receptor (AChR) is a proposed major mechanism of neuromodulation at neuromuscular junctions and in the pathology of synapses in the central nervous system. We show that binding of the competitive antagonist ?-bungarotoxin (?BTX) or antibody-mediated cross-linking induces the internalization of ...

The alpha-7 nicotinic acetylcholine receptor (?7nAChR) and the dopamine D(2) receptor (D(2) R) are both implicated in attentional processes and cognition, mediated in part through the prefrontal cortex (PFC). We examined the dual electron microscopic immunolabeling of ?7nAChR and either D(2) R or the vesicular ...

Acetylcholine (ACh) is a neurotransmitter/neuromodulator in the nematode nervous system and induces its effects through interaction with both ligand-gated ion channels (LGICs) and G protein-coupled receptors (GPCRs). The structure, pharmacology and physiological importance of LGICs have been appreciably elucidated in model nematodes, including parasitic ...

A photoactivatable derivative of neurotoxin II from Naja naja oxiana containing a 125I-labeled p-azidosalicylamidoethyl-1,3'-dithiopropyl label at Lys-25 forms a photo-induced cross-link with the delta subunit of the membrane-bound Torpedo californica nicotinic acetylcholine receptor (AChR). The cross-linked ...

In the twenty-five years since the observation that chronic exposure to nicotine could regulate the number and function of high affinity nicotine binding sites in the brain there has been a major effort to link alterations in nicotinic acetylcholine receptors (nAChRs) to nicotine-induced behaviors that drive the addiction to tobacco ...

We employed a pH-sensitive GFP analog, superecliptic phluorin, to observe aspects of nicotinic acetylcholine receptor (nAChR) trafficking to the plasma membrane (PM) in cultured mouse cortical neurons. The experiments exploit differences in the pH among endoplasmic reticulum (ER), trafficking vesicles, and the extracellular solution. The data confirm that ...

One of the earliest descriptions of non-neuronal ACh synthesis was by Morris who reported that ACh was synthesized in the placenta [1]; furthermore, Falugi et al. showed the presence of AChE in human fibrosarcoma cells [2]. Afterward, the expression of ACh, AChE, and cholinergic ...

Mice deficient in the glycosyltransferase Large are characterized by severe muscle and central nervous system abnormalities. In this study, we show that the formation and maintenance of neuromuscular junctions in Large^myd mice are greatly compromised. Neuromuscular junctions are not confined to the muscle endplate zone but are widely spread and are frequently accompanied by ...

The experimental question is whether hypothalamic opioids, known to stimulate consummatory behavior, control a link to the nucleus accumbens (NAc). It was hypothesized that opioids injected in the hypothalamic paraventricular nucleus (PVN) alter the balance of dopamine (DA) and acetylcholine (ACh) in the NAc in a manner that fosters appetite for food or ...

Previous studies have reported that activation of nicotinic ACh receptors on cultured pig retinal ganglion cells (RGCs) has a neuroprotective effect against glutamate-induced excitotoxicity (Wehrwein et al., 2004; Thompson et al., 2006). However, the mechanism linking nAChRs to neuroprotection is unknown. Here we ...

Neonicotinoid insecticides target nicotinic acetylcholine receptors (nAChRs), which, in both vertebrates and invertebrates, mediate fast-acting synaptic neurotransmission in the nervous system. Recently, Kagabu et al. synthesized bis-neonicotinoids. The neural activities of bis-neonicotinoids have been evaluated on the central nerve cord of American ...

Recombinant DNA techniques have been used to identify the family of molecules that mediate nicotine's effects on the brain. Nicotine binds and activates nicotinic acetylcholine receptors (nAChRs) which are made up of combinations of individual nicotinic subunits. It is important to determine which of the many possible subunit combinations are responsible ...

Tubal ectopic pregnancy (EP) is the most common cause of maternal mortality in the first trimester of pregnancy; however, its etiology is uncertain. In EP, embryo retention within the Fallopian tube (FT) is thought to be due to impaired smooth muscle contractility (SMC) and alterations in the tubal microenvironment. Smoking is a major risk factor for EP. FTs from women with EP exhibit altered ...

... 3H]ACh recognition sites in brain. Repeated injections of nicotine for 5-21 days increase the number of [ 3H]ACh recognition ...

... A solid phase radioassay was developed alpha-bungarotoxin in (BTX) to purified Torpedo AChR and membrane-bound AChR as a model. ...

... principal piece of human and mouse sperm [49]. Physostigmine, an AChE inhibitor (and thus an indirect agonist ... ...

Achondroplasia (ACH), the most common type of genetic dwarfism, is characterized by a variety of skeletal anomalies including disproportionate short stature and rhizomelic shortening of the extremities. The disorder is inherited as an autosomal dominant trait, with a prevalence of 1-15 per 100,000 live births. The etiology of ACH remains unknown, although ...

The widespread non-neuronal synthesis of acetylcholine (ACh) has changed the paradigm of ACh acting solely as a neurotransmitter. Indeed, the presence of ACh in many types of proliferating cells suggests a role for this neurotransmitter in the control of cell division. The parasympathetic system is a major pathway regulating ...

Age-related hearing loss (presbycusis) is a major health concern for the elderly. Loss of spiral ganglion neurons (SGNs), the primary sensory relay of the auditory system, is associated consistently with presbycusis. The causative molecular events responsible for age-related loss of SGNs are unknown. Recent reports directly link age-related neuronal loss in cerebral cortex ...

The class of diterpenoids with a 14-carbon cembrane ring, the cembranoids, includes both competitive and noncompetitive inhibitors of the nicotinic acetylcholine receptor (AChR). All 20 coelenterate-derived cembranoids studied in this report inhibited [piperidyl-3,4-3H]-phencyclidine ([3H]-PCP) binding to its high-affinity site on the electric organ ...

The C. elegans eat-6 gene encodes a Na⁺, K⁺-ATPase ? subunit and is a homolog of the familial hemiplegic migraine candidate gene FHM2. Migraine is the most common neurological disorder linked to serotonergic dysfunction. We sought to study the pathophysiological mechanisms of migraine and their relation to serotonin (5-HT) ...

BackgroundEpidemiological studies link organophosphorus pesticide (OP) exposures to asthma, and we have shown that the OPs chlorpyrifos, diazinon and parathion cause airway hyperreactivity in guinea pigs 24 hr after a single subcutaneous injection. OP-induced airway hyperreactivity involves M2 muscarinic receptor dysfunction on airway nerves independent of ...

Several lines of evidence suggest a link between the alpha7 neuronal nicotinic acetylcholine receptor (nAChR) and brain disorders including schizophrenia, Alzheimer's disease, and traumatic brain injury. The present work describes a novel molecule, 1-(5-chloro-2,4-dimethoxy-phenyl)-3-(5-methyl-isoxazol-3-yl)-urea (PNU-120596), which ...

Circulating immunoglobulin (Ig)G antibodies against M(2) muscarinic acetylcholine receptors (M(2) mAChR) have been implicated in Chagas' disease (ChD) pathophysiology. These antibodies bind to and activate their target receptor, displaying agonist-like activity through an unclear mechanism. This study tested the ability of serum ...

This article examines the role of innervation in regulating expression of acetylcholinesterase (AchE), butylcholinesterase (BuchE), and the muscarinic acetylcholine receptor (mAchR) in avian heart. Two distinct approaches are taken. The first approach exa...

To establish the functional modification produced by phosphorylation of the nicotinic acetylcholine receptor (AChR) single channel currents activated by acetylcholine (ACh) from purified Torpedo californica AChR reconstituted in lipid bilayers were record...

Examination of the binding characteristics of acetylcholine receptor (AchR) and either tritium labeled acetylcholine ((3H)-Ach) or calcium 45 (45Ca) via a modified Hill plot revealed a decrease in synergistic binding for both acetylcholine (Ach) and calci...

The lethal biochemical lesion of organophosphate (OP) poisoning in animals is the inactivation of acetylcholinesterase (AChE), an enzyme responsible for terminating the action of the neurotransmitter, acetylcholine (ACh), on the acetylcholine receptor (AC...

Behavioral effects of organophosphates (OPs) typically decrease with repeated exposure, despite persistence of OP-induced inhibition of acetylcholinesterase (AChE) and downregulation of muscarinic acetylcholine (ACh) receptors. o characterize this tolerance phenomenon, rats were ...

Here we characterized the cross-inhibitory interactions between nicotinic and P2X receptors of celiac neurons from the guinea pig by recording whole-cell currents induced by 1mM ACh (I(ACh)), 1mM ATP (I(ATP)) and by the simultaneous application of both agonists (I(ACh)(+ATP)). I(ACh) and I(ATP) ...

�regulating or down�regulating role. According to the model, the major regulating genes are mGluR3, AChE, 5HT1b, GRa2 enzymes (AChE, GAD67, GAD65) and neurotransmitter receptors (mGluR3, 5HT1b, GRa2). mGluR3 is a member effectively be an inhibitor of those genes. #12; Acetylcholine esterase (AChE) is necessary ...

Alzheimer's disease (AD) is the leading cause of dementia affecting over 25 million people worldwide. Classical studies focused on the description and characterization of the pathological hallmarks found in AD patients including the neurofibrillary tangles and the amyloid plaques. Current strategies focus on the etiology of these hallmarks and the different mechanisms contributing to ...

Hierarchical in silico screening protocols against the agonist bound acetylcholine binding protein (AChBP) crystal structure were efficient in identifying novel chemotypes for AChBP and the human ?7 receptor. Two hit structures were cocrystallized with AChBP revealing intermolecular cation-? interactions with loop ...

the Lymnaea stagnalis acetylcholine binding protein (AChBP) and the trans- membrane (TM) domain of the TorpedoAChRs during the gating process is currently unclear. Recently, the structure of nAChR from Torpedo marmorata-bound AChBP structure into the electron density of Torpedo nAChR, Unwin et ...

Classically, sympathetic and parasympathetic systems act in opposition to maintain the physiological homeostasis. In this article, we report that both systems work together to restrain systemic inflammation in life-threatening conditions such as sepsis. This study indicates that vagus nerve and cholinergic agonists activate the sympathetic noradrenergic splenic nerve to control systemic ...

Classically, sympathetic and parasympathetic systems act in opposition to maintain the physiological homeostasis. In this article, we report that both systems work together to restrain systemic inflammation in life-threatening conditions such as sepsis. This study indicates that vagus nerve and cholinergic agonists activate the sympathetic noradrenergic splenic nerve to control systemic ...

Acetylcholine-based neurotransmission is regulated by cationic, ligand-gated ion channels called nicotinic acetylcholine receptors (nAChRs). These receptors have been linked to numerous neurological diseases and disorders such as Alzheimer's disease, Parkinson's disease, and nicotine addiction. Recently, a class of ...

Several acetylcholinesterase (AChE) inhibitors decrease muscarinic cholinergic (mACh) receptors in the brain, alteration of dopamine (DA) and ..gamma..-aminobutyric acid (GABA) receptors after AChE inhibition was also reported. In view of the important interactions among DA, GABA and ...

The enzyme acetylcholinesterase (AChE) which belongs to the family of alpha/beta hydrolases is well known for hydrolyzing the neurotransmitter acetylcholine (ACh). In addition to its catalytic function, AChE appears to play a significant non-catalytic role in development, regeneration and modulation of properties of neurons. However ...

The enzyme acetylcholinesterase (AChE) which belongs to the family of ?/? hydrolases is well known for hydrolyzing the neurotransmitter acetylcholine (ACh). In addition to its catalytic function, AChE appears to play a significant non-catalytic role in development, regeneration and modulation of properties of neurons. However ...

At the neuromuscular junction (NMJ), the dystrophin protein complex provides a scaffold that functions to stabilize acetylcholine receptor (AChR) clusters. Syntrophin, a key component of that scaffold, is a multi-domain adapter protein that links a variety of signaling proteins and ion channels to the dystrophin protein complex. ...

Neonicotinoid insecticides, such as imidacloprid, are selective agonists of insect nicotinic acetylcholine receptors (nAChRs) and are used extensively in areas of crop protection and animal health to control a variety of insect pest species. Here, we describe studies performed with nAChR subunits Nlalpha1 and Nlalpha2 cloned from the ...

We used single-channel recording and model-based kinetic analyses to quantify the effects of mutations in the extracellular domain (ECD) of the ?-subunit of mouse muscle�type acetylcholine receptors (AChRs). The crystal structure of an acetylcholine binding protein (AChBP) suggests that the ECD is comprised of a ?-sandwich core that ...

Cellular/Molecular Galantamine Activates Muscle-Type Nicotinic Acetylcholine Receptors without activate the nicotinic ACh receptor or modulate its activation by ACh. In this study, we have examined the ability of galantamine to directly activate the muscle-type nicotinic ACh ...

These studies examine the influence of inorganic lead on expression of dihydropyridine receptors and molecular forms of acetylcholinesterase (AchE) in primary cultures of avian skeletal muscles. Treatment of avian muscle cultures with Pb{sup ++} in the concentration range 0-100 {mu}M caused graded reductions in the amounts of dihydropyridine ...

Nicotinic acetylcholine receptor channel (AChR) gating is an organized sequence of molecular motions that couples a change in the affinity for ligands at the two transmitter binding sites with a change in the ionic conductance of the pore. Loop 5 (L5) is a nine-residue segment (mouse ?-subunit 92�100) that links the ...

The nicotinic acetylcholine receptor (nAChR) is a member of a family of ligand-gated ion channels that mediate diverse physiological functions, including fast synaptic transmission along the peripheral and central nervous systems. Several studies have made significant advances toward determining the structure and dynamics of the lipid-exposed domains of ...

We have investigated the role of acetylcholine receptors (AChRs) in an early step of postsynaptic assembly at the neuromuscular synapse, the clustering of postsynaptic proteins induced by nerve-released agrin. To achieve this, we used two variants of C2 myotubes virtually lacking AChRs and C2 cells in which surface ...

Poisoning via organophosphorus (OP) nerve agents occurs when the OP binds and inhibits the enzyme acetylcholinesterase (AChE). This enzyme is responsible for the metabolism of the neurotransmitter acetylcholine (ACh) which transmits signals between nerves and several key somatic regions. When AChE is inhibited, the signal initiated by ...

At Caenorhabditis elegans neuromuscular junctions (NMJs), synaptic clustering of the levamisole-sensitive acetylcholine receptors (L-AChRs) relies on an extracellular scaffold assembled in the synaptic cleft. It involves the secreted protein LEV-9 and the ectodomain of the transmembrane protein LEV-10, which are both expressed by muscle cells. ...

In developing antidotes to poisoning by cholinesterase (ChE) inhibitors, several potential target sites at the cholinergic synapse have been studied, including the postsynaptic receptor and acetylcholinesterase (AchE) itself. Muscarinic receptor blocking ...

Previous studies suggest that m2 muscarinic receptors serve as presynaptic autoreceptors. Blocking these receptors by selective antagonist may, therefore, lead to increased acetylcholine (ACh) release. This study assessed changes in extracellular ACh leve...

Alpha-Bungarotoxin (alphaBT) is a snake toxin which in vertebrate systems binds with great specificity to acetylcholine (ACh) receptors. The authors have studied the effects of alpha BT on the electrophysiological response to ACh of identifiable cells in ...

The neuromuscular junction has been recognized as a site for autoimmune and genetic disorders. Myasthenia gravis (MG) is mainly caused by postsynaptic nicotinic acetylcholine receptor (AChR) IgG1 antibodies that are directed against ?-subunit 67-76 and 125-147 and activate complement. Thymic abnormalities are present in the autoimmune background. A ...

) and islets have muscarinic ACh receptors � Stimulation of the vagus nerve, which connects to ganglia, induces

... Sweating and heart rate responses after acute PYR treatment are consistent ... accumulation of ACh at cholinergic receptors of the sweat gland and ...

... Title : Meproadifen Enhances Activitation and Desensitization of the Acetylcholine Receptor-Ionic Channel Complex (AChR): Single Channel ...

... specific receptors for acetylcholine (ACh), dopamine, octopamine, phenylethanolamine, histamine, gamma-aminobutyric acid (GABA), aspartic ...

Neonicotinoid agonists selectively act on the insect nicotinic acetylcholine receptor (nAChR). The molecular basis for this specificity is deciphered by comparisons of two acetylcholine binding proteins (AChBPs) with distinct pharmacological profiles that serve as structural homologues for the nAChR subtypes. ...

Acetylcholinesterase (AChE) anchors onto cell membranes by a transmembrane protein PRiMA (proline-rich membrane anchor) as a tetrameric form in vertebrate brain. The assembly of AChE tetramer with PRiMA requires the C-terminal "t-peptide" in AChE catalytic subunit (AChE(T)). Although mature ...

of these diVerential eVects on learning has been a challenge given that estrogen receptors are found in both, ovariectomies decrease NMDA receptor binding, and treatment with estrogen can restore the binding (Cyr et alACh, nicotinic cholinergic receptors. (A) Estrogen present (B) Low or no estrogen ...

Positive and negative regulation of neurotransmitter receptor aggregation on the postsynaptic membrane is a critical event during synapse formation. Acetylcholine (ACh) and agrin are two opposing signals that regulate ACh receptor (AChR) clustering during neuromuscular junction (NMJ) ...

The effects of various neuroleptics and of apomorphine on the metabolism of ACh were examined in the neostriatum of the rat. For this purpose, a specific radio-enzymatic assay for brain ACh was used. This method is based on the preliminary purification of the choline esters by liquid cation exchange, separation of choline and ACh on ...

Acetylcholine (ACh) has been shown to modulate neuronal differentiation during early development. Both muscarinic and nicotinic acetylcholine receptors (AChRs) regulate a wide variety of physiological responses, including apoptosis, cellular proliferation and neuronal differentiation. However, the intracellular mechanisms underlying ...

Cultures of spinal cord neurons and cocultures of rat embryo neurons and muscle cells have been studied in the presence of tetanus toxin (TT) at a concentration of 40 micrograms/ml of medium. TT strongly stimulated neurite outgrowth, notably branching from the cell bodies. In addition it induced a marked, overall increase in acetylcholine receptor (AChR), ...

Increasing evidence suggests excess illness in Persian Gulf War veterans (GWV) can be explained in part by exposure of GWV to organophosphate and carbamate acetylcholinesterase inhibitors (AChEis), including pyridostigmine bromide (PB), pesticides, and nerve agents. Evidence germane to the relation of AChEis to illness in GWV was assessed. Many ...

Increasing evidence suggests excess illness in Persian Gulf War veterans (GWV) can be explained in part by exposure of GWV to organophosphate and carbamate acetylcholinesterase inhibitors (AChEis), including pyridostigmine bromide (PB), pesticides, and nerve agents. Evidence germane to the relation of AChEis to illness in GWV was assessed. Many ...

, acetylcholine; AChBP, acetylcholine-binding pro- tein; CNS, central nervous system; ECD, extracellular domain, myasthenia gravis; MLA, methyllycaconi- tine; nAChR, nicotinic acetylcholine receptor; nAChR- ECD (ECDs) of nAChRs (20�27), (b) the 4 A� resolu- tion electron microscopy (EM) ...

Rapid synaptic transmission at the calyciform synapse in the embryonic chicken ciliary ganglion is mediated by two classes of nicotinic receptors; those containing ?3 subunits (?3-nAChRs) and those containing ?7 subunits (?7-nAChRs). ?3-nAChRs and ?7-nAChRs are differentially distributed on the ...

Environmental, congenital, and acquired immunological insults perturbing neuromuscular junction (NMJ) activity may induce a variety of debilitating neuromuscular pathologies. However, the molecular elements linking NMJ dysfunction to long-term myopathies are unknown. Here, we report dramatically elevated levels of mRNA encoding c-Fos and the "readthrough" (R) variant of ...

Alcohol abuse is a health problem throughout the world and alcohol consumption is linked to the occurrence of several pathological conditions. Acute ethanol administration exerts a variety of actions on the central nervous system (CNS). Zebrafish has been used as an attractive model system to investigate behavioral and neurochemical changes promoted by alcohol intoxication. ...

Smokers are less likely to develop some inflammatory and allergic diseases. In Brown-Norway rats, nicotine inhibits several parameters of allergic asthma including the production of Th2 cytokines and the cysteinyl leukotriene LTC₄. Cysteinyl leukotrienes are primarily produced by mast cells, and these cells play a central role in allergic asthma. Mast cells express a high ...

Previously, we have reported that the orexigenic peptide ghrelin activates the cholinergic-dopaminergic reward link, involving nicotinic acetylcholine receptors (nAChR). The alpha(3)-alpha(7) and beta(2)-beta(4) subunits of the nAChR can be combined into pentameric nAChRs, with different ...

Recently, a novel cholinergic channel modulator, (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), was shown to produce potent analgesia in a variety of rodent pain models when administered either systemically or centrally into the nucleus raphe magnus (NRM). The purpose of the present study was to investigate the possible supraspinal contribution of ABT-594 by assessing its ability to ...

Cell bodies of afferent neurons located in lumbosacral dorsal root ganglia (DRG) provide Adelta- and C-fibres to the urinary bladder, reporting bladder wall tension, volume and noxious stimuli. Recent studies suggested an involvement of muscarinic acetylcholine receptors (mAChRs) not only in detrusor contractility but also in modulating afferent function, ...

Muscarinic receptors of cardiac pacemaker and atrial cells are linked to a potassium channel (IK.ACh) by a pertussis toxin-sensitive GTP-binding protein. The dissociation of G-proteins leads to the generation of two potential transducing elements, alpha-GTP and beta gamma. IK.ACh is activated by G-protein alpha- ...

Nicotinic acetylcholine receptor (nAChR) genes form a highly conserved gene cluster at the lung cancer susceptibility locus 15q25.1. In this study, we show that the CHRN ? 3 gene encoding nAChR ? 3 subunit is a frequent target of aberrant DNA hypermethylation and silencing in lung cancer, whereas the adjacent CHRN ? 4 and CHRN ? 5 ...

The rostral portion of the nucleus of the solitary tract (rNST) is an obligatory relay for gustatory afferent input on its way to the forebrain. Previous studies have demonstrated excitation of rNTS neurons by glutamate and substance P and inhibition by gamma-aminobutyric acid (GABA) and met-enkephalin (ENK). Despite the existence of cholinergic neurons and putative terminals within the rNTS, ...

We have examined possible mechanisms of cross-talk between the G_q/11-linked M₃ muscarinic acetylcholine (mACh) receptor and the G_i/o-linked M₂ mACh receptor by stable ...

Functional studies of the ligand gated ion channel family (nicotinic acetylcholine, serotonin Type 3, glycine and GABA receptors) along with the crystal structure of the acetylcholine binding protein (AChBP) and molecular dynamics simulations of the nAChR structure have resulted in a structural model in which the agonist-binding pocket ...

The cholinergic system is crucial for cognitive processes and the deficient acetylcholine (ACh) function has been implicated in Alzheimer�s disease (AD). Inhibitors of acetylcholinesterase (AChE), which act to enhance cholinergic function by prolonging the action of endogenously released ACh, have been used as the major therapy of ...

The lateral mobility of surface receptors can define the signaling properties of a synapse and rapidly change synaptic function. Here we use single-particle-tracking with Quantum Dots to follow nicotinic acetylcholine receptors (nAChRs) on the surface of chick ciliary ganglion neurons in culture. We find that both heteropentameric ...

ACh, the main neurotransmitter in the neuronal cholinergic system, is synthesized by pre-ganglionic fibers of the sympathetic and parasympathetic autonomic nervous system and by post-ganglionic parasympathetic fibers. There is increasing experimental evidence that ACh is widely expressed in prokaryotic and eukaryotic non-neuronal cells. The neuronal and ...

Acetylcholine (ACh), the first neurotransmitter discovered, participates in many CNS functions including sensory and motor processing, sleep, nociception, mood, stress response, attention, arousal, memory, motivation and reward. These diverse cholinergic effects are mediated by nicotinic (nAChR) and muscarinic (mAChR) type cholinergic ...

We have developed idiotype-anti-idiotype monoclonal antibodies that provide evidence for rabies virus binding to the acetylcholine receptor (AChR). Hybridoma cell lines 7.12 and 7.25 resulted after fusion of NS-1 myeloma cells with spleen cells from a BALB/c mouse immunized with rabies virus strain CVS. Antibody 7.12 reacted with viral glycoprotein and ...

The core features of schizophrenia include deficits in cognitive processes, such as attention and working memory, subserved by the prefrontal cortex (PFC). These deficits are believed to involve deficient neurotransmission through NMDA receptors, particularly on parvalbumin-containing interneurons, and administration of the NMDA-antagonist phencyclidine (PCP) in rodents is a ...

Acetylcholinesterase (AChE) reactivators are crucial antidotes to organophosphate intoxication. A new series of 26 monooxime-monocarbamoyl xylene-linked bispyridinium compounds was prepared and tested in vitro, along with known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime, K107, K108 and K203), on a model of tabun- and paraoxon-, ...

Research conducted in this terminal year of support centered on three distinct areas: mAChR ligand localization in pancreas and the effect of Ca{sup +2} on localization, continuation of assessment of quaternized and neutral mAChR ligands for possible use as PET myocardial imaging agents, and initiation of a study to determine the relationship of the ...

We have previously demonstrated that the highly conserved R209, that flanks the M1 transmembrane segment of nicotinic acetylcholine (ACh) receptors, is required for the transport of assembled homomeric neuronal ?7 nicotinic ACh receptors to the cell surface. In the present paper we show that basic residues at ...

The nicotinic acetylcholine receptor (nAChR) is the prototype member of the superfamily of pentameric ligand-gated ion channels. How the extracellular ligand-binding domain coordinates selective binding of ligand molecules to different subtypes of the receptor is unknown at the structural level. Here, we present the 2.2-� crystal ...

Micromolar concentrations of methylmercury and several organic mercury fungicides were found to block binding of [3H]acetylcholine (ACh) to the ACh-receptor of the electric organ of the electric ray, Torpedo ocellata. The same compounds had little or no effect on the catalytic activity of ACh-esterase of the same tissue. ...

The proposed program will demonstrate the ability of a detector based on measuring the conductance of nicotinic acetylcholine receptor (nAChR) ion channels to detect and quantify anatoxin-a contamination in drinking water systems.� The nAChR is extremely sensitive to the p...

Studies were completed on the time course of the effect of DFP on brain acetylcholinesterase ACH activity. While brain ACH activity is maximally depressed only 5 minutes after administration, most behavior effects require two or more hours before the maxi...

Protein phosphorylation is considered a key event in synaptic physiology. The acetylcholine receptor (AChR), a prototype of ligand-gated ion channels, plays a central role in postsynaptic signal transduction. To examine the functional consequences of AChR...

AbstractHuman SH-SY5Y neuroblastoma cells have been used to investigate mechanisms involved in CREB phosphorylation after activation of two endogenously expressed G_q/11-protein-coupled receptors, the M₃ muscarinic acetylcholine (mACh) and B₂ bradykinin receptors. ...

Evidence for an important link between sensitization of midbrain dopamine (DA) neuron reactivity and enhanced self-administration of amphetamine and cocaine has been reported. To the extent that exposure to nicotine also sensitizes nucleus accumbens DA reactivity, it is likely that it will also impact subsequent drug taking. It is thus necessary to gain an understanding of the ...

Historically, ACh has been implicated in learning and short-term memory functions. However, more recent studies have provided support for a role of cortical ACh in attentional effort, orienting and the detection of behavioral significant stimuli. The current review article summarizes studies in animals and humans which have investigated the role of ...

1. The action of acetylcholine (ACh) on the hyperpolarization-activated ('pacemaker') current if was studied in single myocytes from the sino-atrial (SA) node region of the rabbit heart, where low doses of ACh slow spontaneous activity by prolonging the diastolic depolarization phase. 2. Besides activating an outward component at voltages positive to the ...

Zinc is known to exert antidepressant-like actions and to make the effects of some antidepressants more efficient in animal models of depression. Both zinc and bupropion interact with nicotinic acetylcholine receptors (nAChRs) which are related with depression. Here we examined the effects of bupropion, in the absence and presence of zinc, on the ion ...

Contraction of normal esophageal circular muscle (ESO) in response to acetylcholine (ACh) is linked to M2 muscarinic receptors activating at least three intracellular phospholipases, i.e., phosphatidylcholine-specific phospholipase C (PC-PLC), phospholipase D (PLD), and the high molecular weight (85 kDa) cytosolic phospholipase A2 ...

The effect of ad libitum dietary exposure (as occurs in the field) to parathion for 14 d was investigated on the muscarinic acetylcholine receptor (mAChR) in brains and submaxillary glands of adults of a field species, the white-footed mouse Peromyscus leucopus. Immunoprecipitation using subtype selective antibodies revealed that the relative ratios of the ...

ET (endothelin)-1, a potent vasoconstrictor peptide released by the endothelium, plays an important role in vasomotor regulation and has been linked to diminished endothelial vasodilator capacity in several pathologies associated with human aging, including hypertension, Type 2 diabetes and coronary artery disease. However, it is currently unknown whether the decline in ...

Levels of mRNA for acetylcholine receptor (AChR) subunits are relatively low in innervated skeletal muscles. Following denervation they rise rapidly, leading to increased AChR synthesis. The mechanism by which motor nerves normally regulate these mRNA levels is not yet known. In order to determine the possible role of synaptic ...

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The most abundant subtype of cerebral nicotinic acetylcholine receptors (nAChR), ?4?2, plays a critical role in various brain functions and pathological states. Imaging agents suitable for visualization and quantification of ?4?2 nAChRs by positron emission tomography (PET) would present unique opportunities to define the function and ...

In this paper, research on the temporal and spatial distribution of cholinergic-related molecules in the lower auditory brainstem, with an emphasis on nicotinic acetylcholine receptors (nAChRs), is reviewed. The possible functions of acetylcholine (ACh) in driving selective auditory neurons before the onset of hearing, inducing ...

Mechanisms that regulate early events in the biogenesis of the ?7 nicotinic acetylcholine receptor (?7 AChR) are not well understood. Data presented here show that single amino acid mutations in the cytoplasmic loop of the ?7 AChR, between position 335 and 343, abolish or attenuate expression of mature pentameric ?7 ...

Interactions between cholinergic and glutamatergic neurotransmitter systems influence synaptic transmission and plasticity. While previous studies have examined cross-talk between acetylcholine (ACh) and NMDA or AMPA receptors, little is known about the effect of ACh on kainate receptors (KARs). We show that ...

Radish (Raphanus sativus L.) was grown on four layers of paper towel moistened with distilled water with and without acetylcholine (ACh) for five days in the dark after sowing. ACh at 1 nM promoted the growth (emergence and elongation) of lateral roots of radish plants, but had no effect on the stems and main roots. Moreover, ACh ...

Agrin activates MuSK, a receptor tyrosine kinase expressed in skeletal muscle, leading to tyrosine phosphorylation of the acetylcholine receptor (AChR) beta-subunit and clustering of AChRs. The importance of AChR beta-subunit tyrosine phosphorylation in clustering AChRs and ...

Mutations affecting acetylcholine receptors have been causally linked to the development of congenital myasthenic syndromes (CMS) in humans resulting from neuromuscular transmission defects. In an undergraduate Molecular Neurobiology course, the molecular basis of CMS was explored through study of a Caenorhabditis elegans model of the disease. The ...

Transmitter molecules bind to synaptic acetylcholine receptor channels (AChRs) to promote a global channel-opening conformational change. Although the detailed mechanism that links ligand binding and channel gating is uncertain, the energy changes caused by mutations appear to be more symmetrical between subunits in the transmembrane ...

We have developed a novel method for the preparation of 'recombinant proteoliposomes'. Membrane proteins were expressed on budded virus (BV) envelopes using baculovirus gene expression systems, and proteoliposomes were prepared by fusion of these viruses with liposomes. First, plasmid DNA containing the gene for the thyroid-stimulating hormone receptor (TSHR) or the ...

1. The distribution of acetylcholine receptors (AChR) at frog cutaneous pectoris neuromuscular junctions was studied quantitatively using [1125]alpha-bungarotoxin (alpha-BTX) labelling and EM autoradiography. 2. We found that, as in mouse end-plates, the AChR is localized uniformly along the thickened post-junctional membrane. In the ...

A comparison between several immobilization materials of AChE on surface of glassy carbon electrode(GCE) was presented. The immobilization methods employed crosslinking method with glutaraldehyde as a cross-linking agent and bovine serum albumin(BSA) as a protectant, AChE was immobilized on different membranes including nylon membrane, ...

This work describes the use of layered double hydroxides (LDHs) for the immobilisation of acetylcholinesterase (AChE) on insulator/semiconductor solid supports. Different LDHs have been synthesised by a co-precipitation method. Afterwards, biohybrid materials based on AChE-LDH mixtures have been produced using wild and recombinant enzymes. Spectroscopic ...

An acetylcholinesterase (AChE) gene, Ace.x, showing 93% identity of deduced amino acid sequence to Anopheles stephensi Ace has been cloned from a Culex pipiens strain homozygous for insensitive AChE (iAChE) mediated insecticide resistance. DNA sequence of genomic DNA clones identified exons 2-5. RFLP of six clones indicated four ...

Detection of autoantibodies associated with neurological disease typically involves immunoprecipitation of radioactively labeled native proteins. We explored whether single receptor subunits, fused to Renilla luciferase (Ruc), could detect patient autoantibodies in Luciferase Immunoprecipitation Systems. Myasthenia Gravis patient sera were tested for conformational ...

The nicotinic acetylcholine (ACh) receptor (nAChR) plays a crucial role in excitatory neurotransmission and is an important target for drugs and insecticides. Diverse nAChR subtypes with various subunit combinations confer differential selectivity for nicotinic drugs. We investigated the subtype selectivity of ...

The nicotinic ACh receptor obtained from the electric organ of Torpedo was used successfully to detect OP nerve agents but had low sensitivity for cyanide and sulfur mustard. Use of ACh receptor-regulated binding of the allosteric probe was more efficient than monitoring changes in fluorescent ...

Neonicotinoids are synthetic, nicotine-derived insecticides used for agricultural and household pest control. Though highly effective at activating insect nicotinic receptors, many neonicotinoids are also capable of directly activating and/or modulating the activation of vertebrate nicotinic receptors. In this study, we have investigated the actions of the ...

Acetylcholine (ACh) release is thought to be linked to choline (Ch) uptake and vesicular packaging in peripheral mammalian systems. Several compounds, having various inhibitory effects on isolated cholinergic systems, were tested for their ability to modulate the release of Ch and ACh from rat cortex slices. Release experiments were ...

As with other neurotransmitter receptors and ion channels, characterisation ofnicotinic acetylcholine receptors (nAChRs) has relied heavily on studies conducted with cloned receptors expressed in artificial expression systems. Although much has been achieved in recent years by such studies, considerable problems ...

Activation of nicotinic acetylcholine receptors (nAChRs) on neurons engages calcium-dependent signaling pathways regulating numerous events. Receptors containing ?7 subunits (?7-nAChRs) are prominent in this because of their abundance and high relative calcium permeability. We show here that EphB2 ...

The chronic effects of antidepressant treatment on striatal dopaminergic (DA) and muscarinic cholinergic (mACh) receptors of the rat brain have been examined comparatively in this study using /sup 3/H-spiroperidol (/sup 3/H-SPD) and /sup 3/H-quinuclidinyl benzilate (/sup 3/H-QNB) as the respective radioactive ligands. Imipramine and desipramine were used ...

Striatal dopamine (DA) and acetylcholine (ACh) regulate motivated behaviors and striatal plasticity. Interactions between these neurotransmitters may be important, through synchronous changes in parent neuron activities and reciprocal presynaptic regulation of release. How DA signalling is regulated by striatal muscarinic receptors ...

Striatal dopamine (DA) and acetylcholine (ACh) regulate motivated behaviors and striatal plasticity. Interactions between these neurotransmitters may be important, through synchronous changes in parent neuron activities and reciprocal presynaptic regulation of release. How DA signaling is regulated by striatal muscarinic receptors ...

Molecular biological studies and electrophysiological data have demonstrated that acetylcholine (ACh) is the principal cochlear and vestibular efferent neurotransmitter among mammalians. However, the functional roles of ACh in type II vestibular hair cells (VHCs II) among mammalians are still unclear, with the exception of the well-known alpha9-containing ...

NMDA receptor (NMDAR) activation requires concurrent membrane depolarization, and glutamatergic synapses lacking AMPA receptors (AMPARs) are often considered �silent� in the absence of another source of membrane depolarization. During the second postnatal week, NMDA currents can be enhanced in rat auditory cortex through activation of the ?7 nicotinic ...

BackgroundA crucial event in the development of the vertebrate neuromuscular junction (NMJ) is the postsynaptic enrichment of muscle acetylcholine (ACh) receptors (AChRs). This process involves two distinct steps: the local clustering of AChRs at synapses, which depends on the activation of the muscle-specific ...

The agonist binding affinity of nicotinic acetylcholine receptor (nAChR) from Torpedo californica electroplax, as inferred from ability of agonist to inhibit specific curaremimetic neurotoxin binding to nAChR, is sensitive to the duration of exposure to agonist. The concentration of carbachol necessary to prevent one-half of toxin ...

Nicotine dependence is linked to single nucleotide polymorphisms in the CHRNB4-CHRNA3-CHRNA5 gene cluster encoding the ?3?4?5 nicotinic acetylcholine receptor (nAChR). Here we show that the ?4 subunit is rate limiting for receptor activity, and that current increase by ?4 is maximally competed by one of the most ...

ACh release into the rodent prefrontal cortex is predictive of successful performance of cue detection tasks, yet the cellular mechanisms underlying cholinergic modulation of cortical function are not fully understood. Prolonged (�tonic�) muscarinic ACh receptor (mAChR) activation increases the excitability of ...

1. Acetylcholine (ACh) evoked secretion by the calcium ionophore, ionomycin, was studied at frog motor nerve endings. 2. Bath application of ionomycin stimulated an irreversible increase in the rate of spontaneous, quantal ACh release in the presence of extracellular Ca2+. In contrast, local application of ionomycin stimulated a rapid, reversible ...

1. Acetylcholine (ACh) evoked secretion by the calcium ionophore, ionomycin, was studied at frog motor nerve endings. 2. Bath application of ionomycin stimulated an irreversible increase in the rate of spontaneous, quantal ACh release in the presence of extracellular Ca2+. In contrast, local application of ionomycin stimulated a rapid, reversible ...

The animation depicts a speculative model of nicotinic acetylcholine receptor (AChR) gating at the frog neuromuscular junction. Following a nerve impulse, the neurotransmitter acetylcholine (ACh) is released from synaptic vesicles docked at the active zone of the presynaptic nerve terminal. ACh diffuses across the ...

Genetically modified acetylcholinesterase (AChE) from Drosophila melanogaster (dm) and from commercial sources, Electric eel (ee), Bovine erythrocites (be) and Human erythrocites (he), were investigated as biological receptors for the detection of methamidophos pesticide based on inhibition studies. Most engineered variant of AChE from ...

The alpha7 nicotinic acetylcholine receptor (nAChR) is an important target for treatment of cognitive deficits in schizophrenia and Alzheimer's disease. However, the receptor desensitizes rapidly in vitro, which has led to concern regarding its applicability as a clinically relevant drug target. Here we investigate the effects of ...

-inhibition'). Postsynaptic Excitation This was initially identified in experiments on sympathetic ganglia, as an atropine currents before (b1) and after adding 1 M neostigmine (b2) and then 1 M atropine (b3). [From Figs. 2 and 3 of presynaptic mAChRs with atropine enhances the overflow of ACh from the surface of the cat parietal cortex

receptor (nAChR) is a potential molecular target for general anesthetics. It is unclear, however, whether anesthetic action produces the same effect on the open and closed channels. Computations parallel to ourAChR to investigate the conformation-dependent anesthetic effects on channel structures and dynamics. Flexible ligand

in the Torpedo californica AChR has shown that substitution of specific residues can be critical to the channel substitutions at the C418 residue in the M4 transmembrane segment of the Torpedo californica AChR significantly at this presumably lipid-exposed position with- out loss of ion-channel function. As with the Torpedo ACh

A novel approach to broad-specificity medical countermeasure against chemical warfare nerve agent (CWNA) poisoning is by preventing excessive accumulation of ACh attributable to AChE inhibition of CWNA exposure. The effectiveness of various partial adenos...

BackgroundAlterations in muscarinic receptor expression and acetylcholinesterase (AchE) activity have been observed in tissues from Sudden Infant Death Syndrome (SIDS). Vagal overactivity has been proposed as a possible cause of SIDS as well as of vasovagal syncopes. The aim of the present study was to seek whether muscarinic receptor ...

XThe First International Symposium on Subtypes of Muscarinic Receptors held in 1983, promulgated the novel concept that there was more than one subtype of muscarinic receptors (mAchR). Now The Ninth Symposium is the first meeting to describe the phenotype...

Biphenyl-2-yl-carbamic acid 1-{9-[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydro-quinolin-5-yl)-ethylamino]-nonyl}-piperidin-4-yl ester (THRX-198321) is a single molecule composed of a muscarinic acetylcholine receptor (mAChR) antagonist moiety, represented by the fragment MA, linked by a C9 polymethylene chain to a ?(2)-adrenoceptor ...

A nanoparticle-based electrochemical immunosensor has been developed for the detection of phosphorylated acetylcholinesterase (AChE) adducts, which is a potential exposure biomarker for organophosphate pesticides (OP) and chemical warfare nerve agent exposures. Zirconia nanoparticles (ZrO2 NPs) were used as selective sorbents to capture the phosphorylated ...

Acetylcholine (ACh) is a known modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic ACh receptors (nAChRs). Yet, the subunit composition and specific location of nAChRs involved in DA-mediated locomotion remain to be established in vivo. Mice lacking ...

A nanoparticle-based electrochemical immunosensor has been developed for the detection of phosphorylated acetylcholinesterase (AChE), which is a potential exposure biomarker for organophosphate (OP) pesticides and chemical warfare nerve agent exposures. Zirconia nanoparticles (ZrO₂ NPs) were used as selective sorbents to capture the phosphorylated ...

of the levamisole sensitive nicotinic acetylcholine receptor (nAChR) were epitope-tagged at their extracellular C; Levamisole receptor; nAChR; ODR-2; -Bungarotoxin; Tandem affinity tag 1. Introduction A major component specific epitope-tags to the C-termini of levamisole receptor subunits, for ...

Muscarinic acetylcholine receptor (mAChR) activation of pancreatic ?-cells elevates intracellular Ca(2+) and potentiates glucose-stimulated insulin secretion. In addition, it activates a number of signaling molecules, including ERK1/2, whose activation has been shown to play an important role in regulating pancreatic ?-cell function and mass. The aim of ...

The flavonoid quercetin is a low molecular weight substance found in fruits and vegetables. Aside from its anti-oxidative effect, quercetin, like other flavonoids, has a wide range of neuropharmacological actions. The ?7 nicotinic acetylcholine receptor (?7 nAChR) has a Ca(2+)-binding site, is highly permeable to the Ca(2+) ion, and plays important roles ...

Cholinergic signalling in the sympathetic ganglia (SG) contributes to non-shivering thermogenesis by relaying the activation signal from the brain to SG neurons which activate many peripheral tissues to produce heat. Paradoxically, acetylcholinesterase (AChE) inhibitors, which should enhance cholinergic signalling, induce hypothermia. To understand the mechanism of how ...

... and that there appears to be a correlation between the I nhanced response to nicotine and increased [3H[ACh binding sites in cerebral cortex.!- 20. ...

... then clamped to zero using a short-circuit current amplifier (CEZ-9100, Nihon Kohden, Tokyo). The fluid resistance ... ...

... Induced by 56Fe Heavy-Particle Irradiation: Further ... been exposed to energetic particles (56Fe, 600 ... This loss of mAChR sensitivity was postulated ...

(?3)₂(?4)₃ is the most abundant type of neuronal nicotinic ACh receptor (nAChR) mediating cholinergic actions on the autonomic nervous system. Studies to refine or devise drugs selectively acting on (?3)₂(?4)₃ receptors ...

... and the interdigitated electrode1 5 nAChR biosensors have a signal-to-noise ratio ... is an important feature that would allow the biosensor to operate ...

MDMA is an illegal drug widely used by young people. The present study aimed to determine the involvement of different nicotinic acetylcholine receptor (nAChR) subtypes in the suppressive effect of MDMA in TNF-alpha production. Dihydrobetaerythroidine (antagonist of heteromeric nAChR), and hexamethonium (antagonist of peripheral ...

We identified a novel class of direct ion-channel blockers of ligand-gated ion channels called the gold nanoparticle�choline complex. Negatively charged gold nanoparticles (1.4 nm) block ion pores by binding to the sulfur group of the cysteine loop of nicotinic acetylcholine receptors (nAChRs), and currents evoked by acetylcholine ...

A series of carbamoyl bis-pyridinium monooximes linked with xylene linker were synthesized and their in-vitro reactivation potential was evaluated against acetylcholinesterase (AChE) inhibited by organophosphorus inhibitors (OP) such as sarin, DFP and VX and the data were compared with reactivation obtained with 2-PAM and obidoxime. Amongst the synthesized ...

Smokers are less likely to develop some inflammatory and allergic diseases. In Brown-Norway rats, nicotine inhibits several parameters of allergic asthma, including the production of Th2 cytokines and the cysteinyl leukotriene LTC(4). Cysteinyl leukotrienes are primarily produced by mast cells, and these cells play a central role in allergic asthma. Mast cells express a high-affinity ...

Apolipoprotein E (apoE) exerts prominent anti-inflammatory effects and undergoes recycling by target cells. We previously reported that the peptide Ac-hE18A-NH(2), composed of the receptor binding domain (LRKLRKRLLR) of apoE covalently linked to the Class A amphipathic peptide 18A, dramatically lowers plasma cholesterol and lipid ...

Apolipoprotein E (apoE) exerts prominent anti-inflammatory effects and undergoes recycling by target cells. We previously reported that the peptide, Ac-hE18A-NH₂, composed of the receptor binding domain (LRKLRKRLLR) of apoE covalently linked to the Class A amphipathic peptide 18A, dramatically lowers plasma ...

Nicotinic acetylcholine receptors (AChRs) are pentameric ligand-gated ion channels that mediate fast synaptic transmission at the neuromuscular junction (NMJ). After assembly in the endoplasmic reticulum (ER), AChRs must be transported to the plasma membrane through the secretory apparatus. Little is known about specific molecules that ...

The ?(7) acetylcholine receptor (AChR) mediates pre- and postsynaptic neurotransmission in the central nervous system and is a potential therapeutic target in neurodegenerative, neuropsychiatric and inflammatory disorders. We determined the crystal structure of the extracellular domain of a receptor chimera constructed from the human ...

Muscarinic acetylcholine receptors (mAchRs) are the predominant cholinergic receptors in the central and peripheral nervous systems of animals. They also have been found in various insect nervous systems. In this article, a full-length cDNA of a pupative mAchR (PmAchR) was obtained from the ...

Aggregation of nicotinic acetylcholine receptors (AChRs) in skeletal muscle is an essential step in the formation of the mammalian neuromuscular junction. While proteins that bind to myotube receptors such as agrin and laminin can stimulate AChR aggregation in cultured myotubes, removal of cell surface sialic acids ...