Binds to the nicotinic acetylcholine receptors bungarotoxins. Medical search. Frequent questions

Similarly, κ-bungarotoxin acts to block postsynaptic nAchRs, but its effect is primarily on neuronal receptors rather than muscular nicotinic receptors. (wikipedia.org)
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)
bungarotoxin can be a highly particular toxin that binds to peripheral nicotinic acetylcholine receptors (nAChRs) and it performed a key function in the isolation and characterization of mammalian nAChRs [19]. (liveconscience.com)
Just like various other long-chain neurotoxins, in addition, it binds to neuronal 7 nAChRs [20]. (liveconscience.com)
bungarotoxins particularly bind to neuronal nAChRs (32, 42 and 34) [20]. (liveconscience.com)
Rasmussen encephalitis (RE) sera were screened for antibodies to human alpha7 nicotinic acetylcholine receptors (nAChRs) using electrophysiology, calcium imaging, and ligand binding assays. (ox.ac.uk)
Sera from two of nine patients with RE blocked ACh-induced currents through alpha7 nAChRs and the ACh-induced rise in intracellular free calcium ([Ca2+]i) and inhibited (125)I-alpha-bungarotoxin binding in cells expressing alpha7 nAChRs. (ox.ac.uk)
3H]-Methyllycaconitine ([3H]-MLA) is a new radioligand with selectivity for alpha7-type neuronal nicotinic acetylcholine receptors (nAChRs). (ox.ac.uk)
This invention particularly relates to compounds that are ligands for alpha 7 nicotinic acetylcholine receptors (α7 nAChRs). (justia.com)
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)
The agonist ligand nicotine shows an up to 30-fold higher affinity to nACHRs than acetylcholine (ACh). (biomedcentral.com)

loop_ _audit_author.name _audit_author.pdbx_ordinal 'Harel, M.' 1 'Kasher, R.' 2 'Sussman, J.L.' 3 # _citation.id primary _citation.title ;The Binding Site of Acetylcholine Receptor as Visualized in the X-Ray Structure of a Complex between Alpha-Bungarotoxin and a Mimotope Peptide. (rcsb.org)
TMB-8 is much less potent (IC50 approximately 30-200 microM) as an inhibitor of high-affinity 3H-labeled acetylcholine or 125I-labeled alpha-bungarotoxin binding to human muscle nAChR, ganglionic alpha 3 beta 4-nAChR, or ganglionic alpha 7-nAChR subtypes. (aspetjournals.org)
its pharmacology and distribution in crudely dissected brain regions closely paralleled that of the well-established alpha7-ligand [125I]-alpha-bungarotoxin. (ox.ac.uk)
However, a small population of [3H]-MLA binding sites was apparently insensitive to alpha-bungarotoxin. (ox.ac.uk)
Here we have extended the study to mouse brain, using autoradiography to examine the distribution of [3H]-MLA and [125I]-alpha-bungarotoxin binding sites. (ox.ac.uk)
Specific binding, defined by unlabelled MLA (Ki = 0.69 nM), was completely inhibited by (-)-nicotine (Ki = 1.62 microM), whereas alpha-bungarotoxin inhibited only 85% of specific binding (Ki = 3.5 nM). (ox.ac.uk)
The distributions of [125I]-alpha-bungarotoxin and [3H]-MLA binding sites were compared by autoradiography, and binding was quantitated in 72 brain regions. (ox.ac.uk)
Serial sections labelled with [3H]-MLA in the absence or presence of unlabelled MLA or alpha-bungarotoxin provided no evidence for any alpha-bungarotoxin-resistant binding. (ox.ac.uk)
The results are discussed in terms of binding sites that are inaccessible to alpha-bungarotoxin in membrane preparations. (ox.ac.uk)
This study demonstrates the utility of [3H]-MLA for characterization of alpha7-type nicotinic receptors in mammalian brain, and suggests that it labels a population identical to that defined by [125I]-alpha-bungarotoxin. (ox.ac.uk)

Effects of thujone, a major ingredient of absinthe, wormwood oil and some herbal medicines, were tested on the function of α7 subunit of the human nicotinic acetylcholine (α7 nACh) receptor expressed in Xenopus oocytes using the two-electrode voltage-clamp technique. (chapman.edu)
By integrating all-atom molecular dynamics simulations, bioinformatics, two-electrode voltage clamp electrophysiology and 125 I-α-bungarotoxin assays of chimeric nAChR subunits, we identify residues across the extracellular, transmembrane and extended M4 helix of the δ subunit that make structural signatures that contribute to intransigent assembly rules. (ox.ac.uk)
The exact subunit stoichiometry is not known and it is possible that more than one functional α3β4 receptor assembles in vivo with varying subunit stoichiometries. (wikipedia.org)
It binds to the D subunit of ATP synthase and NADH dehydrogenase . (mdwiki.org)

The effect of bisabolol on the function of nicotinic acetylcholine receptor (nAChR) in Xenopus oocytes and interneurons of rat hippocampal slices was evaluated. (terpene.info)
Xenopus oocytes have been extensively used to study biogenesis, functional architecture, and modulation of plasma membrane expression of mRNAs encoding membrane receptors or ion channels. (researchbib.com)
1986). A Xenopus oocyte can also assemble the subunits of a receptor and insert them into its surface membrane (Parker et al. (researchbib.com)
1987) reported for the first time that Xenopus oocytes successfully express glutamate receptors from lobster (Palinurus japonicus ) abdominal muscle. (researchbib.com)
1990) published that amino acid receptors expressed in Xenopus oocyte after " microinjection of mRNA from the leg of locust Schistocerca gregaria. (researchbib.com)

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)

In the presence of a cholinesterase inhibitor to prevent hydrolysis and atropine to block muscarinic cholinergic receptors, [ 3 H]acetylcholine bound rapidly, reversibly, and with high affinity to rat brain membranes (K(D) = 12.3 ± 0.8 nM, B(max) = 4.6 ± 0.1 pmoles/g of tissue). (northwestern.edu)
The monomeric form binds with high affinity to muscular and neuronal alpha-7/CHRNA7 nicotinic acetylcholine receptors (nAChR). (snakevenomdb.org)

On the basis of its ability to bind to nicotinic cholinergic receptors in electric tissue and at the neuromuscular junction, α-bungarotoxin has been widely used to identify central nicotinic receptors. (northwestern.edu)
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. (snakevenomdb.org)
nAChR is found at the edges of junctional folds at the neuromuscular junction on the postsynaptic side, and is activated by acetylcholine release across the synapse. (wikidoc.org)
Drugs such as the neuromuscular blocking agents bind reversibly to the nicotinic receptors in the neuromuscular junction and are used routinely in anaesthesia. (wikidoc.org)

Molecular biology has shown that the nicotinic and muscarinic receptors belong to distinct protein superfamilies . (wikidoc.org)

1981) demonstrated the presence of binding sites for a-bungarotoxin when oocytes were injected with mRNA from the electric organ of Torpedo marmorata. (researchbib.com)

The "calcium antagonist" TMB-8 [3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester] is a potent, non-competitive, functional antagonist at diverse nicotinic acetylcholine receptor subtypes. (aspetjournals.org)
However, this study shows that TMB-8 acts as a noncompetitive, functional antagonist at diverse nicotinic acetylcholine receptor (nAChR) subtypes with potencies that exceed those for other reported effects of TMB-8, including inhibition of intracellular Ca2+ mobilization. (aspetjournals.org)
[17] It inhibits receptor activity in the NMDA glutamate receptor subtypes. (mdwiki.org)

Like other transmembrane receptors , acetylcholine receptors are classified according to their "pharmacology", or according to their relative affinities and sensitivities to different molecules. (wikidoc.org)

Collectively, our results indicate that thujone inhibits the function of the α7-nACh receptor and impairs cellular and behavioral correlates of cholinergic modulation of learning and memory. (chapman.edu)
However, the suitability of this ligand as a probe for nicotinic cholinergic receptors in the central nervous system has been questioned. (northwestern.edu)
The use of [ 3 H]acetylcholine of high specific activity to measure cholinergic binding sites in rat is reported here. (northwestern.edu)
The muscarine cholinergic receptor activates a G protein when bound to ex.c. ach. (wikidoc.org)
The cholinergic postsynaptic membrane is an acetyl-choline receptor-rich membrane mediating fast chemical communication at the nerve-muscle synapse. (iucr.org)

Bungarotoxins function by modulating acetylcholine neurotransmission in both muscles and neurons. (wikipedia.org)
α-Bungarotoxin irreversibly blocks the binding of acetylcholine (ACh) to postsynaptic nicotinic acetylcholine receptors (nAchR) on both muscle and neurons. (wikipedia.org)
Isoflurane acts as a positive allosteric modulator of the GABA A receptor in electrophysiology studies of neurons and recombinant receptors. (mdwiki.org)

Thujone inhibits the function of α7-nicotinic acetylcholine receptors " by Ahmed Sultan, Keun-Hang Susan Yang et al. (chapman.edu)
It was found that bisabolol reversibly and concentration dependently inhibits acetylcholine-induced receptor mediated currents. (terpene.info)
Inhibits neuromuscular transmission by blocking acetylcholine release from the nerve termini. (snakevenomdb.org)
The α-2 adrenergic receptor (A2AR) inhibits insulin or glucagons release. (proteopedia.org)

While all α-neurotoxins of the three-finger family will act on muscle nAchR, these differences in structure determine selectivity of the toxin for its receptor as well as affinity and dissociation. (wikipedia.org)
Cytisine and (-)-nicotine had the highest affinity (K(I) = 1-6 nM) for the [ 3 H]acetylcholine binding site. (northwestern.edu)
Cytisine and (-)-nicotine had the highest affinity (K(I) = 1-6 nM) for the [3H]acetylcholine binding site. (northwestern.edu)
Using automated patch-clamp recordings, we demonstrate that fluorescent synthetic α-bungarotoxin has the expected nanomolar affinity for the nicotinic receptor. (univ-grenoble-alpes.fr)

Like most large toxins, chemical synthesis of α-bungarotoxin is challenging, explaining why all previous reports use purified or recombinant α-bungarotoxin. (univ-grenoble-alpes.fr)

An acetylcholine receptor (abbreviated AChR ) is an integral membrane protein that responds to the binding of the neurotransmitter acetylcholine . (wikidoc.org)

Nicotinic receptors are the primary mediator of the effects of nicotine . (wikidoc.org)
Unlike acetylcholine and carbachol, nicotine uniquely induced drastic rearrangement of egg cortical microfilaments in a dose-dependent way. (mdpi.com)
Is the post-COVID-19 syndrome a severe impairment of acetylcholine-orchestrated neuromodulation that responds to nicotine administration? (biomedcentral.com)

Alpha7-acetylcholine receptor antibodies in two patients with Rasmussen encephalitis. (ox.ac.uk)
In myasthenia gravis , the receptor is targeted by antibodies , leading to muscle weakness. (wikidoc.org)

Bungarotoxins are a group of closely related neurotoxic proteins of the three-finger toxin superfamily found in the venom of kraits including Bungarus multicinctus (the many-banded krait). (wikipedia.org)
Many biologically essential proteins, especially - bungarotoxins, - bungarotoxins and - bungarotoxins, have already been well characterized through the venom of em Bungarus /em types. (liveconscience.com)
Prior functional measurements show that metabotropic glutamate receptors influence voltage-gated calcium channels and proteins that are involved in synaptic vesicle priming. (uni-wuerzburg.de)
M1, M3, M5 receptors are coupled with G q proteins, while M2 and M4 receptors are coupled with G i/o proteins. (proteopedia.org)
Since the last overview of sPLA 2 -binding proteins (sPLA 2 -BPs) 10 years ago, several important discoveries have occurred in this area. (ijbs.com)

TMB-8 is also a potent inhibitor (IC50 approximately 500 nM) of a functional, central nervous system nAChR subtype that mediates nicotinic agonist-stimulated [3H]dopamine release from rat brain synaptosomes. (aspetjournals.org)
Furthermore, functional differences observed in α 2 δ 2 β receptors can be rationalized by changes in dynamical behavior that manifest themselves at the agonist binding site. (ox.ac.uk)
The binding of an agonist to them causes a sympathetic response. (proteopedia.org)

1987) reported the successful expression of serotonin, dopamine, GABA and glycine receptors. (researchbib.com)
Isoflurane likely binds to GABA , glutamate and glycine receptors, but has different effects on each receptor. (mdwiki.org)

The distribution of the metabotropic glutamate receptor mGlu4 is investigated in physiological brain slices enabling the analysis of the receptor in its natural environment. (uni-wuerzburg.de)
muscarinic acetylcholine receptors ( mAChR , also known as " metabotropic " acetylcholine receptors) are particularly responsive to muscarine . (wikidoc.org)
Dopamine receptors are a class of metabotropic G protein-coupled receptors that are important in the central nervous system. (proteopedia.org)

Bungarotoxins are toxins found in the venom of snakes and kraits. (wikipedia.org)
They discovered that this venom consisted of a mixture of individual toxins that act at different sites and receptors to modulate neurotransmission. (wikipedia.org)
The four characterized toxins are: α-Bungarotoxin β-Bungarotoxin (not a three-finger toxin) γ-Bungarotoxin (Q9YGJ0) k-Bungarotoxin Research involving bungarotoxins has been significant in improving our understanding of neurotransmission. (wikipedia.org)
Nicotinic acetylcholine receptors can be blocked by curare and toxins present in the venoms of snakes and shellfishes , like α-bungarotoxin . (wikidoc.org)

The receptor is a transmembrane pentameric glycoprotein. (proteopedia.org)
As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric [(α3) m (β4) n where m + n = 5]. (wikipedia.org)

Because the neurobiological substrate of cariprazine has remained elusive, we took advantage of PharmacoSTORM to provide in vivo evidence that cariprazine predominantly binds to D 3 dopamine receptors on Islands of Calleja granule cell axons but avoids dopaminergic terminals. (nature.com)

Abstract Muscle nicotinic acetylcholine receptors are a class of heteropentameric ligand-gated cation channels with constituent subunits adopting a fixed stoichiometric arrangement. (ox.ac.uk)
Next, we determined the efficacy of the fluorescent-tagged α-bungarotoxin to block acetylcholine (ACh)-mediated currents in response to muscle nicotinic receptor activation in TE671 cells. (univ-grenoble-alpes.fr)
We thus demonstrate that synthetic fluorescent-tagged α-bungarotoxin preserves excellent properties for binding onto muscle nicotinic receptors. (univ-grenoble-alpes.fr)

An autoradiographic study of the distribution of binding sites for the novel alpha7-selective nicotinic radioligand [3H]-methyllycaconitine in the mouse brain. (ox.ac.uk)

It works as a postsynaptic neurotoxin binding to the receptor as an extracellular ligand by interacting with OH group leaving the acetylcholine channel open which releases ions used in creating an action potential. (proteopedia.org)

Secreted phospholipases A 2 (sPLA 2 s) participate in a very broad spectrum of biological processes through their enzymatic activity and as ligands for membrane and soluble receptors. (ijbs.com)
Cholesterol interactions with the receptor are apparently essential for stabilizing and maintaining its physiological architecture, since the transmembrane structure contracts, involving displacements of the helices at the outer membrane surface by ∼2 Å (1-3 Å), when this lipid is extracted. (iucr.org)
Structure of the ACh receptor in Torpedo postsynaptic membrane. (iucr.org)

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)

It is shown that cholesterol segregates preferentially around the receptors in both leaflets of the lipid bilayer, interacting robustly with specific transmembrane sites and creating a network of bridging microdomains. (iucr.org)

Visualizing synaptic plasticity in vivo by large-scale imaging of endogenous AMPA receptors. (neurotree.org)

Moreover, specific binding of [125I] -bungarotoxin was not altered by thujone. (chapman.edu)

Nicotinic receptor modulation. (inra.fr)

Chemical synthesis of α-bungarotoxin requires hydrazide-based coupling of three peptide fragments in successive steps. (univ-grenoble-alpes.fr)
The blocking effect of fluorescent α-bungarotoxin could be displaced by incubation with a 20-mer peptide mimicking the α-bungarotoxin binding site. (univ-grenoble-alpes.fr)

This subclassification describes additional structural aspects of the toxin as well as the receptors they act on. (wikipedia.org)

Phalloidin, bungarotoxins, tetrodotoxin and their fluorescent and biotin conjugates, including Biotium's bright and photostable CF dyes. (bosunlife.com)

The diffusion of Na + and K + across the receptor causes depolarization, the end-plate potential, that opens voltage-gated sodium channels , which allows for firing of the action potential and potentially muscular contraction. (wikidoc.org)

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)

α-bungarotoxin is a large, 74 amino acid toxin containing five disulphide bridges, initially identified in the venom of Bungarus multicinctus snake. (univ-grenoble-alpes.fr)

A lack of correlation between the regional distribution of sites labeled by [ 3 H]acetylcholine and those labeled by 125 I-labeled α-bungarotoxin suggests that these two binding sites are not located on the same molecule. (northwestern.edu)
There must be 5 molecules of cobra toxin (red) to block the receptor (blue) as each molecule binds with an individual alpha chain on the acetylcholine receptor. (proteopedia.org)

In actuality, venom contains several distinct bungarotoxins, each varying in which receptors they act on and how powerful they are. (wikipedia.org)

Muscarinic acetylcholine receptors can be blocked by the drugs atropine and scopolamine . (wikidoc.org)

Conversely, β- and γ-bungarotoxins act presynaptically to cause excessive acetylcholine release and subsequent depletion, resulting in paralysis. (wikipedia.org)
Causes paralysis by preventing acetylcholine binding to the nAChR. (snakevenomdb.org)

In contrast, the mAChRs are not ion channels, but belong instead to the superfamily of G-protein-coupled receptors that activate other ionic channels via a second messenger cascade. (wikidoc.org)

Ligands which inhibit the α3β4 receptor have been shown to modulate drug-seeking behavior, [6] making α3β4 a promising target for the development of novel antiaddictive agents. (wikipedia.org)

Binding of acetylcholine to the N termini of each of the two alpha subunits results in the 15° rotation of all M2 helices. (wikidoc.org)

Small molecules readily penetrate tissue preparations and bind their targets with known stoichiometry. (nature.com)
Although all acetylcholine receptors, by definition, respond to acetylcholine, they respond to other molecules as well. (wikidoc.org)

Alternatively, - bungarotoxins - the main lethal elements bind to voltage-sensitive potassium stations in the presynaptic site [21,22]. (liveconscience.com)

These symptoms are the result of bungarotoxin presence in the venom. (wikipedia.org)

Corresponding dSTORM data indeed suggests that a subset of the mGlu4 receptor is correlated with the voltage-gated calcium channel Cav2.1 on distances around 60 nm. (uni-wuerzburg.de)

Nicotinic receptors are assembled as combinations of α (2-6) and and β (2-4) subunits. (alomone.com)

[1] The cytoplasm side of the nAChR receptor has rings of high negative charge that determine the specific cation specificity of the receptor and remove the hydration shell often formed by ions in aqueous solution. (wikidoc.org)

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)

In competition studies, nicotinic agonists were more than 1000 times more potent than ganglionic and neuromuscular blocking drugs in displacing [ 3 H]acetylcholine binding. (northwestern.edu)

c ) The 5.8 Å density map and superimposed 2.7 Å structure of the Torpedo receptor (PDB entry 6uwz ) obtained from detergent-solubilized protein complexed with α -bungarotoxin. (iucr.org)

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