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 ...
PubMed Central
... This family includes Neu differentiation factor (NDF), heregulin (HRG), acetylcholine receptor inducing activity (ARIA), and the glial growth factors ...
DTIC Science & Technology
The regulation of muscarinic acetylcholine receptors by short-term exposure to agonists was investigated in intact mouse neuroblastoma (clone N1E-115) cells, using the hydrophilic ligand (tritium)N-methylscopolamine. It was found that preincubation of cel...
National Technical Information Service (NTIS)
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...
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...
Modern views on the structure of cholinesterase active sites and the mechanism of their interaction with organophosphorus inhibitors are considered. The attention is focused on the mechanism of the effect of cholinergic receptor blockers, acetylcholine antagonists, on the rate of interaction of acetylcholine esterase with ...
NASA Astrophysics Data System (ADS)
This study evaluates the biochemical and genetic aspects of the acetylcholine receptor proteins and cholinergic ligands in Drosophila melanogaster and Torpedo californica. Included are (1) a comparative study of nicotinic ligand-induced cation release from acetylcholine ...
Energy Citations Database
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 ...
. In particular, we describe separate lines with human a7 and human a4b2 nicotinic acetylcholine receptors, mouse Introduction Nicotinic acetylcholine receptors (nAChRs) are pentameric ligand-gated ion channels (LGICAChR is targeted for schizophrenia [2], Alzheimer's disease [3], and cognition ...
E-print Network
A homologous series of polyethylene glycol (PEG) monomethyl ethers were conjugated with three ligand series for nicotinic acetylcholine receptors. Conjugates of acetylaminocholine, the cyclic analog 1-acetyl-4,4-dimethylpiperazinium, and pyridyl ether A-84543 were prepared. Each series was found to retain significant affinity at ...
The nicotine receptor for the neurotransmitter acetylcholine is an allosteric protein composed of four different subunits assembled in a transmembrane pentamer ? 2? ? ? . The protein carries two acetylcholine sites at the level of the ? subunits and contains the ion channel. The complete sequence of the four subunits is known. The ...
... Title : Turnover of Acetylcholine Receptors: Mechanisms of Regulation. ... Acetylcholine receptors, RA5 Neuromuscular junctions, Motor nerves. ...
Nicotinic acetylcholine receptors are pentameric ligand-gated ion channels, which are involved in a wide range of neuronal functions. During the past decade, a large number of nicotinic acetylcholine receptor subunits have been cloned and showed a discreet yet overlapping distribution pattern. ...
Emerging evidence indicates that muscarinic receptors and ligands play key roles in regulating cellular proliferation and cancer progression. Both neuronal and nonneuronal acetylcholine production results in neurocrine, paracrine, and autocrine promotion of cell proliferation, apoptosis, migration, and other features critical for ...
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 ...
... Title : Primary Structure of Nicotinic Acetylcholine Receptor. ... One of the neurotransmitters used in the mammalian brain is acetylcholine. ...
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 ...
PubMed
... Accession Number : ADD754483. Title : ACETYLCHOLINE RECEPTOR CHANNEL IMAGED IN THE OPEN STATE. Descriptive ...
... Title : ACETYLCHOLINE RECEPTOR BINDING CHARACTERISTICS OF SNAKE AND CONE SNAIL VENOM POSTSYNAPTIC NEUROTOXINS ...
Recently, a family of stimulatory ligands for the EGF/erbB family of receptor tyrosine kinases has been described. This family includes Neu differentiation factor (NDF), heregulin (HRG), acetylcholine receptor inducing activity (ARIA), and the glial growt...
Methyllycaconitine (MLA) is a norditerpenoid alkaloid found in high abundance in toxic Delphinium (larkspur) species. It is a potent and selective antagonist of ?(7)-nicotinic acetylcholine receptors, but has not been well investigated for activity aside from receptor antagonism. The aim of this study was to investigate the effects of ...
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 intermolecular hydrogen ...
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...
A solid phase assay for ligands of curarimimetic toxin binding sites was developed. Its principle is the autoradiographic detection of the displacement of 125 I-alphabungarotoxin from Torpedo californica acetylcholine receptor. To permit analysis of large...
BackgroundNicotine is a psychoactive drug presenting a diverse array of biological activities, some positive, such as enhancement of cognitive performances, others negative, such as addiction liability. Ligands that discriminate between the different isotypes of nicotinic acetylcholine receptors (nAChRs) could present improved ...
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 ...
Quercetin mainly exists in the skin of colored fruits and vegetables as one of flavonoids. Recent studies show that quercetin, like other flavonoids, has diverse pharmacological actions. However, relatively little is known about quercetin effects in the regulations of ligand-gated ion channels. In the previous reports, we have shown that quercetin regulates subsets of ...
... Title : Activation, Inactivation, and Desensitization of Acetylcholine Receptor Channel Complex Detected by Binding of Perhydrohistrionicotoxin. ...
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 the most interesting compounds with ?1, ...
