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Modulators of the Inhibitory Glycine Receptor

ACS Chemical Neuroscience, 2020
The inhibitory glycine receptor is a member of the Cys-loop superfamily of ligand-gated ion channels. It is the principal mediator of rapid synaptic inhibition in the spinal cord and brainstem and plays an important role in the modulation of higher brain functions including vision, hearing, and pain signaling. Glycine receptor function is controlled by
Ulrike Breitinger, Hans-Georg Breitinger
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The inhibitory neuronal glycine receptor

BioEssays, 1994
AbstractGlycine is a major inhibitory neurotransmitter in the spinal cord and in the brain stem, where it acts by activating a chloride conductance. The postsynaptic glycine receptor has been purified and contains two transmembrane subunits of 48 kDa (α) and 58 kDa (β), and a peripheral membrane protein of 93 kDa.
C, Béchade, C, Sur, A, Triller
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Functional reconstitution of the glycine receptor

Biochemistry, 1989
The functional reconstitution of the chloride channel coupled glycine receptor is described. Glycine receptors were purified from the cholate extract of rat spinal cord membranes by affinity chromatography and incorporated into phospholipid vesicles by the addition of phosphatidylcholine and removal of detergent by gel filtration.
M, García-Calvo   +5 more
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Biology of the Postsynaptic Glycine Receptor

1997
Glycine is one of the major inhibitory neurotransmitters, and upon binding to its receptor it activates chloride conductances. Receptors are accumulated immediately opposite release sites, at the postsynaptic differentiations, where they form functional microdomains.
C, Vannier, A, Triller
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The Glycine Receptor

1985
In the vertebrate CNS, many different compounds including acetylcholine, catecholamines, peptides, and amino acids have been identified as bona fide or candidate neurotransmitter substances. Amongst these the amino acids glycine and GABA have been particularly well characterized.
H. Betz   +4 more
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In vitro interaction of the glycine receptor with the leptin receptor

Physiology & Behavior, 2002
The coordination and regulation of electrical signals across excitable cells is a complex, dynamic phenomenon requiring, in part, the interaction of ion channels with cellular constituents. The intracellular loops or domains of many ion channel subunits have been shown to specifically bind other cellular components that act in receptor targeting ...
John F, Leite   +3 more
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Effects of GABA Receptor Antagonists on Retinal Glycine Receptors and on Homomeric Glycine Receptor Alpha Subunits

Journal of Neurophysiology, 2005
Glycinergic and GABAergic inhibition are juxtaposed at one retinal synaptic layer yet likely perform different functions. These functions have usually been evaluated using receptor antagonists. In examining retinal glycine receptors, we were surprised to find that commonly used concentrations of GABA antagonists blocked significant fractions of the ...
Peiyuan, Wang, Malcolm M, Slaughter
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Glycine Receptor Drug Discovery

2017
Postsynaptic glycine receptor (GlyR) chloride channels mediate inhibitory neurotransmission in the spinal cord and brain stem, although presynaptic and extrasynaptic GlyRs are expressed more widely throughout the brain. In humans, GlyRs are assembled as homo- or heteromeric pentamers of α1-3 and β subunits. GlyR malfunctions have been linked to a range
Lynch, Joseph W.   +3 more
openaire   +4 more sources

Glycine receptors

British Journal of Pharmacology, 2006
S P H Alexander, A Mathie, J A Peters
  +4 more sources

Insulin Increases the Potency of Glycine at Ionotropic Glycine Receptors

Molecular Pharmacology, 2007
The mechanisms by which insulin modulates neuronal plasticity and pain processes remain poorly understood. Here we report that insulin rapidly increases the function of glycine receptors in murine spinal neurons and recombinant human glycine receptors expressed in human embryonic kidney cells.
Valerie B, Caraiscos   +5 more
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