... Title : ACETYLCHOLINE RECEPTOR BINDING CHARACTERISTICS OF SNAKE AND CONE SNAIL VENOM POSTSYNAPTIC NEUROTOXINS ...

... Title : Acetylcholine Receptor Binding Characteristics of Snake and Cone Snail Venom Postsynaptic Neurotoxins: Further Studies with a Non ...

... Title : Activation, Inactivation, and Desensitization of Acetylcholine Receptor Channel Complex Detected by Binding of Perhydrohistrionicotoxin. ...

... Accession Number : ADA113141. Title : Structural Models of the Nicotinic Acetylcholine Receptor and Its Toxin-Binding Sites. ...

... Accession Number : ADA299841. Title : Sensitivity Increase in Nicotinic Acetylcholine Receptor Binding in Fiber Optic Wave Guide. ...

... ACETYLCHOLINE RECEP'TORVN~tNNG-CHARkACTERISTICS OF SNAKE AND CONE SNAIL VENOM POSTSYNAPTIC NEUROTOXINS ...

... Title : Structural Characterization of the Putative Cholinergic Binding Region alpha(179-201) of the Nicotinic Acetylcholine Receptor. ...

... Accession Number : ADA228229. Title : Spatial Relationships between Drug Binding Sites on the Surface of the Acetylcholine Receptor. ...

... Accession Number : ADA222751. Title : Spatial Relationships between Drug Binding Sites on the Surface of the Acetylcholine Receptor. ...

... Title : Spatial Relationships between Drug Binding Sites on the Surface of the Acetylcholine Receptor: Preparation and Interaction of Fluorescent ...

... A solid phase radioassay was develDped to measure the binding of neuro- toxins to receptors using binding of 1'lI-labeled a-bungarotoxin (BTX) to ...

Ligand binding studies with nicotinic acetylcholine receptor on the fiber optic biosensor indicate K (sub i) values for antagonists were similar to those obtained in membrane binding assays. The agonists appear much less potent. This may be due to the ina...

This research was designed to 1) develop binding-inhibition assays that could be used to screen compounds that might be effective in inhibiting neurotoxin binding to the acetylcholine receptor (AChR), 2) carry out studies to identify the anionic site on p...

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...

Binding of 125 I a-bungarotoxin to acetylcholine receptors of a ganglionic homogenate of the marine mollusc Aplysia is blocked by the anticholinesterases eserine and neostigmine. Eserine and neostigmine also block toxin binding to a solubilized receptor p...

Antibody against acetylcholine receptor induces an increase in the rate of degradation of acetylcholine receptors on a mouse cell line (BC3H-1) and cultured rat skeletal muscle. The increased rate of degradation results in a lowered density of acetylcholine receptors on ...

Tritiated acetylcholine was used to measure binding sites with characteristics of nicotinic cholinergic receptors in rat brain. Regulation of the binding sites in vivo was examined by administering two drugs that stimulate nicotinic receptors directly or indirectly. After 10 days of exposure to ...

Fluorescence based screening assays are provided that allow for the for identification of agents that selectively bind to a ligand-gated ion channel (LGIC) such as a nicotinic acetylcholine receptor (nAChR). Also provided are methods for identifying agent...

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 nicotinic acetylcholine receptor is a prototype ligand-gated ion channel that mediates signal transduction in the neuromuscular junctions and other cholinergic synapses. The molecular basis for the energetics of ligand binding and unbinding is critical to our understanding of the pharmacology of this class of ...

The authors analyze the role of dopamine and muscarinic acetylcholine receptor blocking components in the antistereotypic action of neuroleptics with different chemical structure. To determine dopamine-blocking activity in vitro, binding of /sup 3/H-spiperone with membranes of the rat striatum was measured. To study the blocking action ...

The Neuromuscular Disease Center at Washington University provides this comprehensive Web site for information on acetylcholine and acetylcholine receptors. Visitors will find detailed Web pages covering acetylcholine metabolism, acetylcholine receptors (including ...

Nicotinic acetylcholine receptors mediate fast synaptic transmission by fluxing ions across the membrane in response to neurotransmitter binding. We show here that during affinity purification of the nicotinic acetylcholine receptor from Torpedo, phosphatidic acid, but not other anionic or ...

Nicotinic acetylcholine receptors mediate fast synaptic transmission by fluxing ions across the membrane in response to neurotransmitter binding. We show here that during affinity purification of the nicotinic acetylcholine receptor from Torpedo, phosphatidic acid, but not other anionic or ...

The level of binding of a labeled acetylcholine muscarinic antagonist (quinuclidinyl benzilate) to different cerebral membranes has been measured. Of the regions examined, circadian rhythmicity of binding could only be detected significantly in the hippocampus and the hypothalamus and not in the cerebral cortex, striatum, or ...

This report describes the preparation and/or characterization of several fluorescent probes of the muscle-type nicotinic acetylcholine receptor for Torpedo californica. These probes include the following: (1) four fluorescein isothiocyante Naja naja siame...

Studies of the binding of labelled ?-bungarotoxin to mouse skeletal muscle endplates have allowed the quantification of acetylcholine receptor sites at the post-synaptic membrane.

Purified ? -toxin from Naja nigricollis snake venom labeled by [3H]acetylation binds specifically to the acetylcholine receptors of mouse neuroblastoma cells. Toxin binding was inhibited by inhibitors for nicotinic and muscarinic acetylcholine receptors. Clones of ...

... Title : Turnover of Acetylcholine Receptors: Mechanisms of Regulation. ... Acetylcholine receptors, RA5 Neuromuscular junctions, Motor nerves. ...

Our previous studies on cationic and uncharged substrates and reversible aliphatic and aromatic inhibitors led to the conclusions (1) that the subsite at which the trimethylammonio group of acetylcholine (AcCh) binds to acetylcholinesterase (AcChE) is not...

Our study of acetylcholinesterase (AcChE) is based on the view that the Beta-trimethylammonio substituent of acetylcholine binds at an uncharged subsite, better termed 'trimethyl' than 'anionic,' and would be more specifically explored by uncharged reagen...

Alpha-bungarotoxin is known to bind with nicotinic acetylcholine receptors of skeletal muscle. Binding of iodine 125-labeled alpha bungarotoxin to the murine thymus, muscle, and liver was estimated. The toxin was bound to the muscle. The thymus was also capable of binding a considerable amount ...

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

... impact of conventional pesticide use. Imidacloprid, a chloronicotinyl compound synthesized from the heterocyclic nitromethylenes, binds to nicotinergic acetylcholine receptors in the ... ...

... acetylcholine for muscarinic receptors in the nervous system and at peripheral organs. Because the ... Bind. Hydrol. IM LD50 WR No. Bottle No. ...

... National Heart and Lung Institute, National Institutes of Health, Bethesda, Maryland D DC ... The authors wish to express their 1.-inks ...

... Personal Author(s) : Shain, WG ; Greene, LA ; Carpenter, DO ; Sytkowski, AJ ; Vogel, Z. Handle / proxy Url : Report Date : FEB 1974. ...

Antibodies in the sera of patients with myasthenia gravis are believed to play an important role in the pathogenesis of the disorder. They have recently been shown to accelerate the degradation of acetylcholine receptors in cultured mammalian skeletal muscle and at intact neuromuscular junctions. To elucidate the mechanism of the antibody-accelerated ...

Because of the complex nature of the nicotinic acetylcholine receptor, it has not been possible to develop a reliable model of the cholinergic binding site. For example, the receptor has a molecular weight over 250,000 daltrons, five homologous subunits, ...

Acetylcholine receptor, a component of the specialized muscle membrane, appears during the differentiation of embryonic myogenic cells in tissue culture. Demonstration of incorporation of the radioactive precursor L-[35S]methionine into purified receptor polypeptides is presented as evidence for its synthesis de novo. The identity of ...

... Title : Primary Structure of Nicotinic Acetylcholine Receptor. ... One of the neurotransmitters used in the mammalian brain is acetylcholine. ...

The influence of chemical modification on the parameters of the binding of cholinergic ligands by the nicotinic acetylcholine receptor of squid optical ganglia was investigated. The presence of two subpopulations of recognition sites, differing in the composition of the groups contained in them, was detected. It was established with ...

Partial contents include: Light-activated channels in limulus ventral photoreceptors; Paramagnetic hydrophobic ions as probes for electrically active conformational transitions in Ion channels; Acetylcholine receptor. Dynamic properties; Acetylcholine-activated channel current-voltage relations in symmetrical Na(+) solutions; A ...

... Accession Number : ADD754483. Title : ACETYLCHOLINE RECEPTOR CHANNEL IMAGED IN THE OPEN STATE. Descriptive ...

A synthetic dodecapeptide corresponding to residues 185-196 of the Torpedo acetylcholine receptor alpha subunit, which contains the adjacent cysteine residues at positions 192 and 193, was recently shown by us to contain the essential elements for alpha-bungarotoxin binding. In the present study, we have used Sepharose-linked peptides ...

The binding of postsynaptic neurotoxins from snake and marine cone snail (Conus sp.) venoms to nicotinic acetylcholine receptor (AchR) was investigated with an ELISA-based, non-radioactive assay.

Black lipid membranes were formed with oxidized cholesterol in the presence of either the acetylcholine receptor, purified from the electric organ of the electric ray Torpedo californica or its tryptic digest. In both cases, conductance of cations increased and was dependent on the concentration of the receptor protein. Conductance of ...

Peptides corresponding to portions of curaremimetic neurotoxin loop 2 and to a structurally similar segment of rabies virus glycoprotein were synthetically modified in order to gain information on structure-function relationships of neurotoxin loop 2 interactions with the acetylcholine receptor. Binding of synthetic peptides to the ...

Anionic lipids influence the ability of the nicotinic acetylcholine receptor to gate open in response to neurotransmitter binding, but the underlying mechanisms are poorly understood. We show here that anionic lipids with relatively small headgroups, and thus the greatest ability to influence lipid packing/bilayer physical properties, ...

Identifiable Aplysia neurons have one or more of three different ionic responses to acetylcholine, due to Na, Cl, and K conductance increases, respectively. The nature of the acetylcholine receptor mediating these three responses was studied using alpha-b...

by the American College of Cardiology The parasympathetic nervous system acts through the vagus nerve to regulate stimulation leads to a release of acetylcholine from the vagus nerve. Acetylcholine binds muscarinic receptors). DISCUSSION Acetylcholine is released from the vagus nerve of the ...

, 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) structure of the Torpedo ...

A radioiodinated ligand that binds to muscarinic acetylcholine receptors was shown to distribute in the brain by a receptor-mediated process. With single-photon-emission imaging techniques, radioactivity was detected in the cerebrum but not in the cerebellum, whereas with a flow-limited radiotracer, radioactivity ...

Nicotinic acetylcholine receptors are ligand-gated ion conducting transmembrane channels from the Cys-loop receptor super-family. The ?4?2 subtype is the predominant heteromeric subtype of nicotinic receptors found in the brain. Allosteric modulators for ?4?2 receptors interact at a site other ...

Histrionicotoxin from the Colombian frog Dendrobates histrionicus and its perhydro derivative reversibly block the acetylcholine-sensitive ion conductance system in frog neuromuscular preparations. The perhydro derivative and [3H]perhydrohistrionicotoxin, like histrionicotoxin, caused a significant decrease in the peak amplitude of the end-plate current and shortened its rise ...

Histrionicotoxin from the Colombian frog Dendrobates histrionicus and its perhydro derivative reversibly block the acetylcholine-sensitive ion conductance system in frog neuromuscular preparations. The perhydro derivative and [3H]perhydrohistrionicotoxin, like histrionicotoxin, caused a significant decrease in the peak amplitude of the end-plate current and shortened its rise ...

Intact rat brain cells were dissociated and used to study the regulation of muscarinic acetylcholine receptors upon exposure to muscarinic receptor agonists. Incubation of cells with carbamylcholine resulted in a time-dependent decrease in subsequent (/sup 3/H)N-methylscopolamine specific binding, an effect which ...

The authors review three examples of how fluorescence spectroscopic techniques have been employed to elucidate structural features of the nicotinic acetylcholine receptor from the electric organ of Torpedo californica. The instrumentation and most relevant fluorescence methods utilized for these studies are briefly discussed. The examples reviewed are as ...

The major brain nicotinic acetylcholine receptor is assembled from two subunits termed ? 4 and n? 1. When expressed in Xenopus oocytes, these subunits reconstitute a functional acetylcholine receptor that is inhibited by progesterone levels similar to those found in serum. In this report, we show that the steroid ...

Evidence for a population of acetylcholine (ACh) receptors in the human retina is presented. The authors have used the irreversible ligand TH-propylbenzilylcholine mustard (TH-PrBCM) to label muscarinic receptors. TH- or SVI-alpha-bungarotoxin (alpha-BTx) was used to label putative nicotinic receptors. Muscarinic ...

The perhydro derivative of histrionicotoxin reversibly blocks the excitatory ionic transduction system in the synaptic and sarcolemmal membranes of mammalian skeletal muscle cells. The efficacy of perhydrohistrionicotoxin as an antagonist at the post-synaptic membrane is increased by the transient presence of acetylcholine in the endplate of innervated muscles and at ...

and Isacoff (1), for example, used this approach to determine that NMDA receptors containing NR1 and NR3B of engagement for NMDA receptor subunits. Proc. Natl. Acad. Sci. USA. 105:14163� 14168. 3. Ji, W., P. Xu, ., L trafficking by using a-bungarotoxin-binding-site-tagged receptors. Proc. Natl. Acad. Sci. USA. ...

High-affinity binding of (/sup 3/H)acetylcholine to muscarinic cholinergic sites in rat CNS and peripheral tissues was measured in the presence of cytisin, which occupies nicotinic cholinergic receptors. The muscarinic sites were characterized with regard to binding kinetics, pharmacology, anatomical distribution, ...

The continuous alpha-neurotoxin-binding regions on the extracellular part (residues 1-210) of the alpha-chain of Torpedo californica acetylcholine receptor were localized by reaction of 125I-labelled alpha-bungarotoxin with synthetic overlapping peptides spanning this entire part of the chain. The specificity of the ...

Phencyclidine is a highly specific noncompetitive inhibitor of the nicotinic acetylcholine receptor. In a novel approach to study this site, a spin-labeled analogue of phencyclidine, 4-phenyl-4-(1-piperidinyl)-2,2,6,6-tetramethylpiperidinoxyl (PPT) was synthesized. The binding of PPT inhibits 86Rb flux (IC50 = 6.6 microM), and ...

nicotinic acetylcholine receptor (nAChR) Target Category: Receptor binding Method of detection: PET Source in the central nervous system, where their activation by acetylcholine and nicotine always causes a rapid's disease, Alzheimer's disease, and Parkinson's disease. nAChRs also play a ...

The introduction of the isoxazole ring as bioisosteric replacement of the acetyl group of anatoxin-a led to a new series of derivatives binding to nicotinic acetylcholine receptors. Bulkier substitutions than methyl at the 3 position of isoxazole were shown to be detrimental for the activity. The binding potency of ...

Acetylcholine receptor enriched membranes from Torpedo ocellata, Torpedo marmorata and Torpedo californica were studied using [3H] azido-phencyclidine (AZ-PCP). [3H]-PCP binding to receptors from all three species revealed marked similarities. Photoaffinity labeling by [3H]-AZ-PCP resulted in the tagging of mainly ...

The acetylcholine receptor from denervated rat skeletal muscle was purified by affinity chromatography and, after reduction, was treated with the affinity alkylating agent 4-(N-maleimido)benzyltri[3H]methylammonium iodide. The receptor specifically incorporated approximately I mol of alkylating agent per mol of 125I-labeled ? ...

The acetylcholine receptor from Torpedo californica was labeled by reaction with the fluorescent probe 4-[N-(iodoacetoxy)ethyl-N-methyl]amino-7-nitrobenz-2-oxa-1,3-diazole without apparent effect on its in vitro ligand binding and functional properties. Addition of acetylcholine or carbamoylcholine to the ...

The GA-binding protein (GABP) transcription factor has been shown in vitro to regulate the expression of the neuromuscular proteins utrophin, acetylcholine esterase, and acetylcholine receptor subunits ? and ? through the N-box promoter motif (5?-CCGGAA-3?), but its in vivo function remains unknown. A single point ...

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 C but lacking ...