Alcohols and neurotransmitter gated ion channels: past, present and future

@article{Lovinger1997AlcoholsAN,
  title={Alcohols and neurotransmitter gated ion channels: past, present and future},
  author={D. Lovinger},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={1997},
  volume={356},
  pages={267-282}
}
  • D. Lovinger
  • Published 1997
  • Chemistry, Medicine
  • Naunyn-Schmiedeberg's Archives of Pharmacology
The neurotransmitter-gated ion channels form a superfamily of neurotransmitter receptors specialized for recognizing transmitters and rapidly gating ion channels that are contained within the same holoprotein complex. A large body of research indicates that alcohols alter the function of this class of receptor at concentrations relevant to the intoxicating and anesthetic effects of the alcohols. In addition, studies have implicated several types of neurotransmitter-gated channels in… Expand
Acute Alcohol Action and Desensitization of Ligand-Gated Ion Channels
TLDR
Understanding interactions between ethanol and ionotropic receptor desensitization may help to explain different ethanol actions when ethanol is evaluated in vitro on cloned channel proteins, under physiological or pathological conditions or in distinct cell domains with modified ligand concentration and/or receptor conformation. Expand
Dual action of n-alcohols on neuronal nicotinic acetylcholine receptors.
TLDR
It is found that n-alcohols, depending on the carbon chain length, exert a dual action, potentiation and inhibition, on nnAChRs in primary cultured rat cortical neurons, suggesting that potentiating and inhibitory actions are exerted through two different binding sites. Expand
Glycine and gamma-aminobutyric acid(A) receptor function is enhanced by inhaled drugs of abuse.
TLDR
The data suggest that inhaled drugs of abuse affect ligand-gated ion channels, and that the molecular sites of action of these compounds may overlap with those of ethanol and the volatile anesthetics. Expand
Glycine and γ-aminobutyric acid(A) receptor function is enhanced by inhaled drugs of abuse
Inhalable solvents possess significant abuse liability and produce many of the neurobehavioral effects typically associated with central nervous system-depressant agents, including motorExpand
General anaesthetic actions on ligand-gated ion channels
TLDR
The last 10 years have witnessed an explosion of studies of anaesthetic modulation of recombinant ligand-gated ion channels, including recent studies which utilize chimeric and mutated receptors to identify regions of ligands-gating ion channels important for the actions of general anaesthetics. Expand
Regulation of NMDA receptors by ethanol.
  • M. Kumari, M. Ticku
  • Chemistry, Medicine
  • Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques
  • 2000
TLDR
Ethanol's effects on NMDA receptors, including alteration in receptor function and number, probably result from interplay of multiple mechanisms some of which are discussed here. Expand
Single-channel analyses of ethanol modulation of neuronal nicotinic acetylcholine receptors.
TLDR
Changes in single-channel parameters indicate that ethanol stabilizes the alpha4beta2 receptor-channel in the opening state, explaining how the maximum acetylcholine-induced whole-cell currents are further potentiated by ethanol. Expand
Ethanol inhibition of recombinant NR1/2A receptors: effects of heavy metal chelators and a zinc-insensitive NR2A mutant.
TLDR
The suggestion that low levels of zinc present in experimental solutions may affect the apparent ethanol sensitivity of NMDA receptors containing the NR2A subunit is supported. Expand
A Transmembrane Amino Acid in the GABAA Receptor β2 Subunit Critical for the Actions of Alcohols and Anesthetics
TLDR
It was found that potentiation by butanol, octanol, or isoflurane in the N265C mutant was nearly abolished after the application of OMTS, suggesting that an alcohol and volatile anesthetic binding site at position 265 of the β2 subunit was irreversibly occupied by octanethiol and consequently prevented butanol or is ofluranes from binding and producing their effects. Expand
Allosteric Modulation of GABAA Receptor Function by General Anesthetics and Alcohols
Since their introduction into clinical practice nearly 150 years ago, general anesthetics have become some of the most widely used and important therapeutic agents. Alcohol, specifically ethanol, isExpand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 120 REFERENCES
Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel.
TLDR
A complementary DNA clone containing the coding sequence of one of these rapidly responding channels, a 5HT3 subtype of the serotonin receptor, has been isolated by screening a neuroblastoma expression library for functional expression of serotonin-gated currents in Xenopus oocytes. Expand
Nicotinic acetylcholine receptors.
  • A. Karlin
  • Chemistry, Medicine
  • Methods in enzymology
  • 1977
TLDR
Nicotinic acetylcholine receptors (nAChRs) are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the postsynaptic side of the neuromuscular junction. Expand
Mutations in the channel domain alter desensitization of a neuronal nicotinic receptor
TLDR
Investigation of how structural elements could be involved in the desensitization of the acetylcholine-gated ion channel from the chick brain α-bungarotoxin sensitive homo-oligomeric α7 receptor using site-directed mutagenesis and expression in Xenopus oocytes finds that leucine-to-threonine mutant has an additional conducting state active at low acetylCholine concentrations. Expand
Rings of negatively charged amino acids determine the acetylcholine receptor channel conductance
TLDR
The single-channel conductance properties of these AChR mutants expressed in Xenopus laevis oocytes indicate that three clusters of negatively charged and glutamine residues neighbouring segment M2 of the α-, β-, γ- and δ-subunits, probably forming three anionic rings, are major determinants of the rate of ion transport. Expand
Rings of anionic amino acids as structural determinants of ion selectivity in the acetylcholine receptor channel
  • T. Konno, C. Busch, +6 authors B. Sakmann
  • Chemistry, Medicine
  • Proceedings of the Royal Society of London. Series B: Biological Sciences
  • 1991
TLDR
The experimental results suggest that the amino acid residues forming the intermediate ring come into close contact with permeating cations and possibly represent part of the physical correlate of the postulated selectivity filter in the AChR channel. Expand
Recent developments in alcoholism:neuronal ion channels.
  • E. Sanna, R. Harris
  • Chemistry, Medicine
  • Recent developments in alcoholism : an official publication of the American Medical Society on Alcoholism, the Research Society on Alcoholism, and the National Council on Alcoholism
  • 1993
TLDR
Effects of ethanol on ion channels were last reviewed in this series in 1987 and it is now clear that there are many subtypes of ligand- and voltage-gated ion channels and that the ethanol sensitivity of these channels is subtype dependent. Expand
Transmembrane topology of two kainate receptor subunits revealed by N-glycosylation.
  • Z. Wo, R. Oswald
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
  • 1994
TLDR
It is shown that a portion of these receptors previously thought to be a large intracellular loop is actually located extracellularly and an alternative model for the transmembrane topology of kainate receptors is proposed that could potentially serve as a framework for future detailed study of the structure of this important class of neurotransmitter receptors. Expand
P2x receptors bring new structure to ligand-gated ion channels
TLDR
Isolation of cDNAs that encode P2X receptors in the smooth muscle of vas deferens and in phaeochromocytoma cells indicates that the receptors are not related to other ligand-gated ion channels. Expand
Alcohol action on a neuronal membrane receptor: evidence for a direct interaction with the receptor protein.
TLDR
The results suggest that alcohols inhibit the function of this neurotransmitter receptor by interacting with a small hydrophobic pocket on the receptor protein. Expand
Cloned glutamate receptors.
The application of molecular cloning technology to the study of the glutamate receptor system has led to an explosion of knowledge about the structure, expression, and function of this most importantExpand
...
1
2
3
4
5
...