glycine receptors

Summary

Summary: Cell surface receptors that bind GLYCINE with high affinity and trigger intracellular changes which influence the behavior of cells. Glycine receptors in the CENTRAL NERVOUS SYSTEM have an intrinsic chloride channel and are usually inhibitory.

Top Publications

  1. Grasshoff C, Antkowiak B. Effects of isoflurane and enflurane on GABAA and glycine receptors contribute equally to depressant actions on spinal ventral horn neurones in rats. Br J Anaesth. 2006;97:687-94 pubmed
    ..As GABAA and glycine receptors are potential candidates we investigated the impact of both receptor systems in mediating the depressant ..
  2. Yevenes G, Moraga Cid G, Avila A, Guzman L, Figueroa M, Peoples R, et al. Molecular requirements for ethanol differential allosteric modulation of glycine receptors based on selective Gbetagamma modulation. J Biol Chem. 2010;285:30203-13 pubmed publisher
    It is now believed that the allosteric modulation produced by ethanol in glycine receptors (GlyRs) depends on alcohol binding to discrete sites within the protein structure...
  3. Ye J. Regulation of excitation by glycine receptors. Results Probl Cell Differ. 2008;44:123-43 pubmed
    ..This chapter is an overview of selective studies on the newly discovered roles of GlyRs in regulating neuronal excitation, and inhibition, particularly in the upper brain areas. ..
  4. Perkins D, Trudell J, Crawford D, Alkana R, Davies D. Targets for ethanol action and antagonism in loop 2 of the extracellular domain of glycine receptors. J Neurochem. 2008;106:1337-49 pubmed publisher
    ..of a traditional pharmacological antagonist to probe the molecular sites and mechanisms of ethanol action in glycine receptors (GlyRs)...
  5. Kondratskaya E, Betz H, Krishtal O, Laube B. The beta subunit increases the ginkgolide B sensitivity of inhibitory glycine receptors. Neuropharmacology. 2005;49:945-51 pubmed
    ..of ginkgolide B (GB), a component of the extract from the leaves of the Ginkgo biloba tree, on recombinant glycine receptors (GlyRs) expressed in Xenopus oocytes by using voltage-clamp recording. GB (0...
  6. Ye J, Sokol K, Bhavsar U. Glycine receptors contribute to hypnosis induced by ethanol. Alcohol Clin Exp Res. 2009;33:1069-74 pubmed publisher
    ..Given that hypnosis is caused by neuronal depression in upper brain areas, we therefore conclude that brain GlyRs contribute at least in part to the hypnosis induced by ethanol. ..
  7. Molander A, Löf E, Stomberg R, Ericson M, Söderpalm B. Involvement of accumbal glycine receptors in the regulation of voluntary ethanol intake in the rat. Alcohol Clin Exp Res. 2005;29:38-45 pubmed
    ..activation and how they relate to EtOH reinforcement remain to be elucidated, but recent data indicate that glycine receptors (GlyRs) in the nAc may be involved...
  8. Jensen A, Bergmann M, Sander T, Balle T. Ginkgolide X is a potent antagonist of anionic Cys-loop receptors with a unique selectivity profile at glycine receptors. J Biol Chem. 2010;285:10141-53 pubmed publisher
    ..Thus, we propose that the distinct functionalities of ginkgolide X compared with the other ginkgolides could arise from different flexibility and thus different binding modes to the ion channel of the anionic Cys-loop receptor. ..
  9. Awatramani G, Turecek R, Trussell L. Staggered development of GABAergic and glycinergic transmission in the MNTB. J Neurophysiol. 2005;93:819-28 pubmed
    ..The apparent switch in GABA/glycine transmission was predominantly due to enhanced glycinergic function. ..

More Information

Publications62

  1. Beato M, Sivilotti L. Single-channel properties of glycine receptors of juvenile rat spinal motoneurones in vitro. J Physiol. 2007;580:497-506 pubmed
    ..Our results suggest that glycine receptors on ventral horn neurones in the juvenile rat are heteromers and have fast gating, similar to that of ..
  2. Haeseler G, Ahrens J, Krampfl K, Bufler J, Dengler R, Hecker H, et al. Structural features of phenol derivatives determining potency for activation of chloride currents via alpha(1) homomeric and alpha(1)beta heteromeric glycine receptors. Br J Pharmacol. 2005;145:916-25 pubmed
    ..The aim of our study was to identify structural features that determine their modulatory effects at glycine receptors. We investigated the effects of four methylated phenol derivatives and two halogenated analogues on chloride ..
  3. Chen Y, Dai T, Zeng Y. Strychnine-sensitive glycine receptors mediate the analgesic but not hypnotic effects of emulsified volatile anesthetics. Pharmacology. 2007;80:151-7 pubmed
    The present study was designed to investigate the role of strychnine-sensitive glycine receptors in hypnosis and analgesia induced by emulsified volatile anesthetics...
  4. Lozovaya N, Yatsenko N, Beketov A, Tsintsadze T, Burnashev N. Glycine receptors in CNS neurons as a target for nonretrograde action of cannabinoids. J Neurosci. 2005;25:7499-506 pubmed
    ..These results suggest that the direct inhibition of GlyRs by endocannabinoids can modulate the hippocampal network activity. ..
  5. Lynch J. Molecular structure and function of the glycine receptor chloride channel. Physiol Rev. 2004;84:1051-95 pubmed
  6. Muller E, Triller A, Legendre P. Glycine receptors and GABA receptor alpha 1 and gamma 2 subunits during the development of mouse hypoglossal nucleus. Eur J Neurosci. 2004;20:3286-300 pubmed
    In the hypoglossal nucleus, GABA and glycine mediate inhibition at separate or mixed synapses containing glycine receptors (GlyRs) and/or GABA(A) receptors (GABA(A)Rs)...
  7. Fuentealba J, Guzman L, Manríquez Navarro P, Perez C, Silva M, Becerra J, et al. Inhibitory effects of tutin on glycine receptors in spinal neurons. Eur J Pharmacol. 2007;559:61-4 pubmed
    ..obtained from Coriaria ruscifolia subspecie ruscifolia, a native poisonous Chilean plant, on spinal glycine receptors using patch clamp recordings...
  8. Qi R, Zhang J, Lu D, Wang H, Wang H, Li C. Glycine receptors contribute to cytoprotection of glycine in myocardial cells. Chin Med J (Engl). 2007;120:915-21 pubmed
    ..Glycine could directly activate GlyR on the cardiomyocytes and prevent calcium influx into the cardiomyocytes. ..
  9. Lynch J, Callister R. Glycine receptors: a new therapeutic target in pain pathways. Curr Opin Investig Drugs. 2006;7:48-53 pubmed
    ..Future therapies aimed at specifically increasing current flux through alpha3-containing GlyRs may prove effective in providing analgesia. ..
  10. Tang Z, Lu Y, Chen L. Developmental stability of taurine's activation on glycine receptors in cultured neurons of rat auditory cortex. Neurosci Lett. 2008;430:54-9 pubmed
    ..During natural development, taurine's receptor target undergoes a shift from glycine receptors to GABA(A) receptors in cortical neurons...
  11. Kilb W, Hanganu I, Okabe A, Sava B, Shimizu Okabe C, Fukuda A, et al. Glycine receptors mediate excitation of subplate neurons in neonatal rat cerebral cortex. J Neurophysiol. 2008;100:698-707 pubmed publisher
    ..Because glycine receptors play an important role during early corticogenesis, we analyzed the functional consequences of glycine ..
  12. Ye J, Wang F, Krnjevic K, Wang W, Xiong Z, Zhang J. Presynaptic glycine receptors on GABAergic terminals facilitate discharge of dopaminergic neurons in ventral tegmental area. J Neurosci. 2004;24:8961-74 pubmed
    ..In many cells, glycine had no effect on remaining miniature IPSCs, suggesting a preterminal site of glycine receptors (GlyRs)...
  13. Lorenzo L, Barbe A, Portalier P, Fritschy J, Bras H. Differential expression of GABAA and glycine receptors in ALS-resistant vs. ALS-vulnerable motoneurons: possible implications for selective vulnerability of motoneurons. Eur J Neurosci. 2006;23:3161-70 pubmed
    ..ALS-susceptible motor nuclei. However, although motoneurons express high levels of glycine receptors (GlyR) and GABA(A) receptors (GABA(A)R), no such studies have been carried out yet for inhibitory synaptic ..
  14. Beato M. The time course of transmitter at glycinergic synapses onto motoneurons. J Neurosci. 2008;28:7412-25 pubmed publisher
    ..cord slices by recording synaptic currents in the presence of a low-affinity competitive antagonist at glycine receptors [2-(3-carboxypropyl)-3-amino-6-(4-methoxyphenyl)pyridazinium (SR-95531)]...
  15. Foadi N, Leuwer M, Demir R, Dengler R, Buchholz V, de la Roche J, et al. Lack of positive allosteric modulation of mutated alpha(1)S267I glycine receptors by cannabinoids. Naunyn Schmiedebergs Arch Pharmacol. 2010;381:477-82 pubmed publisher
    ..There are hints that non-cannabinoid receptor mechanisms of these cannabinoids might be mediated via glycine receptors. In this study, we investigated the impact of the amino acid residue serine at position 267 on the glycine-..
  16. Chen Y, Dai T, Zeng Y. Strychnine-sensitive glycine receptors mediate analgesia induced by emulsified inhalation anaesthetics in thermal nociception but not in chemical nociception. Basic Clin Pharmacol Toxicol. 2007;100:165-9 pubmed
    The present study was designed to investigate the role of strychnine-sensitive glycine receptors in analgesia induced by emulsified inhalation anaesthetics...
  17. Plested A, Groot Kormelink P, Colquhoun D, Sivilotti L. Single-channel study of the spasmodic mutation alpha1A52S in recombinant rat glycine receptors. J Physiol. 2007;581:51-73 pubmed
    Inherited defects in glycine receptors lead to hyperekplexia, or startle disease. A mutant mouse, spasmodic, that has a startle phenotype, has a point mutation (A52S) in the glycine receptor alpha1 subunit...
  18. Caraiscos V, Bonin R, Newell J, Czerwinska E, MacDonald J, Orser B. Insulin increases the potency of glycine at ionotropic glycine receptors. Mol Pharmacol. 2007;71:1277-87 pubmed
    ..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...
  19. Nakae A, Tanaka T, Miyake K, Hase M, Mashimo T. Comparing methods of detection and quantitation of RNA editing of rat glycine receptor alpha3. Int J Biol Sci. 2008;4:397-405 pubmed
    ..The demonstrated methodologies should be very useful when extended to the evaluation of other types of RNA editing and single base mutations. ..
  20. Beato M, Burzomato V, Sivilotti L. The kinetics of inhibition of rat recombinant heteromeric alpha1beta glycine receptors by the low-affinity antagonist SR-95531. J Physiol. 2007;580:171-9 pubmed
    The GABA(A) antagonist SR-95531 (gabazine) is known to block glycine receptors, albeit with low affinity...
  21. Ehrensperger M, Hanus C, Vannier C, Triller A, Dahan M. Multiple association states between glycine receptors and gephyrin identified by SPT analysis. Biophys J. 2007;92:3706-18 pubmed
    The scaffolding protein gephyrin is known to anchor glycine receptors (GlyR) at synapses and to participate in the dynamic equilibrium between synaptic and extrasynaptic GlyR in the neuronal membrane...
  22. Heinze L, Harvey R, Haverkamp S, Wässle H. Diversity of glycine receptors in the mouse retina: localization of the alpha4 subunit. J Comp Neurol. 2007;500:693-707 pubmed
    ..Thus, there is no apparent compensation of the loss of alpha1 or alpha3 subunits by an upregulation of alpha4 subunit gene expression; however, the alpha2 subunit is moderately upregulated. ..
  23. Jiang P, Yang C, Wang Y, Xu T. Mechanisms of modulation of pregnanolone on glycinergic response in cultured spinal dorsal horn neurons of rat. Neuroscience. 2006;141:2041-50 pubmed
    The glycine receptors and neurosteroids in spinal cord are both implicated in nociceptive signal processing...
  24. Xu H, Zhou K, Huang Y, Chen L, Xu T. Taurine activates strychnine-sensitive glycine receptors in neurons of the rat inferior colliculus. Brain Res. 2004;1021:232-40 pubmed
    ..These findings indicate that Tau activates glycine receptors in neurons of the rat IC and thus may have a functional role in regulating or modulating the ..
  25. Liu Y, Hu C, Tang Y, Chen J, Dong M, Song T, et al. Clozapine inhibits strychnine-sensitive glycine receptors in rat hippocampal neurons. Brain Res. 2009;1278:27-33 pubmed publisher
    ..However, the mechanism of seizure associated with Clo therapy is not completely clear. Strychnine-sensitive glycine receptors (GlyRs) play an important role in regulating the excitability in the hippocampus...
  26. Zeilhofer H. The glycinergic control of spinal pain processing. Cell Mol Life Sci. 2005;62:2027-35 pubmed
    ..E receptors of the EP2 subtype and leads to a protein kinase A-dependent phosphorylation and inhibition of glycine receptors containing the alpha3 subunit (GlyRalpha3)...
  27. Lu T, Rubio M, Trussell L. Glycinergic transmission shaped by the corelease of GABA in a mammalian auditory synapse. Neuron. 2008;57:524-35 pubmed publisher
    ..By applying glycine to native or recombinant glycine receptors, we show that response decay times are accelerated by addition of GABA, a weak partial agonist of glycine ..
  28. Vitanova L. Immunocytochemical study of glycine receptors in the retina of the frog Xenopus laevis. Anat Embryol (Berl). 2006;211:237-45 pubmed
    The expression of glycine receptors in the retina of clawed frog, Xenopus laevis was studied immunocytochemically...
  29. Majumdar S, Heinze L, Haverkamp S, Ivanova E, Wässle H. Glycine receptors of A-type ganglion cells of the mouse retina. Vis Neurosci. 2007;24:471-87 pubmed
    ..The results show that A-type ganglion cells receive preferentially kinetically fast glycinergic inputs, mediated by GlyRs composed of alpha1 and beta subunits. ..
  30. Lorenzo L, Barbe A, Bras H. Mapping and quantitative analysis of gephyrin cytoplasmic trafficking pathways in motoneurons, using an optimized Transmission Electron Microscopy Color Imaging (TEMCI) procedure. J Neurocytol. 2004;33:241-9 pubmed
    ..Gephyrin is a scaffolding protein, which plays a crucial role in the clustering of the GABA(A) and glycine receptors to the cytoskeleton...
  31. Zhang L, Gong N, Fei D, Xu L, Xu T. Glycine uptake regulates hippocampal network activity via glycine receptor-mediated tonic inhibition. Neuropsychopharmacology. 2008;33:701-11 pubmed
    Functional glycine receptors (GlyRs) are enriched in the hippocampus, but their role in hippocampal function remains unclear...
  32. Waldvogel H, Baer K, Allen K, Rees M, Faull R. Glycine receptors in the striatum, globus pallidus, and substantia nigra of the human brain: an immunohistochemical study. J Comp Neurol. 2007;502:1012-29 pubmed
    b>Glycine receptors (GlyRs) are heteropentameric chloride ion channels that facilitate fast-response, inhibitory neurotransmission in the mammalian spinal cord and brain...
  33. Grudzinska J, Schemm R, Haeger S, Nicke A, Schmalzing G, Betz H, et al. The beta subunit determines the ligand binding properties of synaptic glycine receptors. Neuron. 2005;45:727-39 pubmed
    Inhibitory glycine receptors (GlyRs) regulate motor coordination and sensory signal processing in spinal cord and other brain regions. GlyRs are pentameric proteins composed of membrane-spanning alpha and beta subunits...
  34. Maksay G, Bíró T, Laube B, Nemes P. Hyperekplexia mutation R271L of alpha1 glycine receptors potentiates allosteric interactions of nortropeines, propofol and glycine with [3H]strychnine binding. Neurochem Int. 2008;52:235-40 pubmed
    Human alpha1 and hyperekplexia mutant alpha1(R271L) glycine receptors (GlyRs) were transiently expressed in human embryonic kidney 293 cells for [3H]strychnine binding. Binding parameters were determined using a ternary allosteric model...
  35. Singer J. GABA is an endogenous ligand for synaptic glycine receptors. Neuron. 2008;57:475-7 pubmed publisher
    ..Lu, Rubio, and Trussell, however, demonstrate in this issue of Neuron the first instance of cotransmission in which two neurotransmitters act on the same postsynaptic receptor. ..
  36. Wang G, Jiang Z, Fan X, Zhang L, Li X, Ke K. Neuroprotective effect of taurine against focal cerebral ischemia in rats possibly mediated by activation of both GABAA and glycine receptors. Neuropharmacology. 2007;52:1199-209 pubmed
    ..Such effect is possibly mediated by the activation of both GABA(A) receptors and strychnine-sensitive glycine receptors. Moreover, inhibition of caspase-3 expression is involved in this neuroprotective effect...
  37. Aguayo L, van Zundert B, Tapia J, Carrasco M, Alvarez F. Changes on the properties of glycine receptors during neuronal development. Brain Res Brain Res Rev. 2004;47:33-45 pubmed
    b>Glycine receptors (GlyRs) play a major role in the excitability of spinal cord and brain stem neurons...
  38. Madry C, Betz H, Geiger J, Laube B. Supralinear potentiation of NR1/NR3A excitatory glycine receptors by Zn2+ and NR1 antagonist. Proc Natl Acad Sci U S A. 2008;105:12563-8 pubmed publisher
    Coassembly of the glycine-binding NMDA receptor subunits NR1 and NR3A results in excitatory glycine receptors of low efficacy...
  39. Cheng W, Yin Q, Cheng M, Chen H, Wang S, Feng T, et al. Intracerebroventricular or intrathecal injection of glycine produces analgesia in thermal nociception and chemical nociception via glycine receptors. Eur J Pharmacol. 2009;614:44-9 pubmed publisher
    The present study was designed to investigate the role of glycine receptors in analgesia induced by injection of glycine in vivo...
  40. Nguyen H, Li K, daGraca R, Delphin E, Xiong M, Ye J. Behavior and cellular evidence for propofol-induced hypnosis involving brain glycine receptors. Anesthesiology. 2009;110:326-32 pubmed publisher
    ..Furthermore, glycine receptors exist throughout the central nervous system, including areas of the brain thought to be involved in sleep...
  41. Meier J, Henneberger C, Melnick I, Racca C, Harvey R, Heinemann U, et al. RNA editing produces glycine receptor alpha3(P185L), resulting in high agonist potency. Nat Neurosci. 2005;8:736-44 pubmed
    The function of supramedullary glycine receptors (GlyRs) is still unclear. Using Wistar rat collicular slices, we demonstrate GlyR-mediated inhibition of spike discharge elicited by low glycine (10 microM)...
  42. Yang Z, Aubrey K, Alroy I, Harvey R, Vandenberg R, Lynch J. Subunit-specific modulation of glycine receptors by cannabinoids and N-arachidonyl-glycine. Biochem Pharmacol. 2008;76:1014-23 pubmed publisher
    b>Glycine receptors (GlyRs) mediate inhibitory neurotransmission in spinal cord motor and pain sensory neurons...
  43. Ge L, Lee S, Liu J, Yang X. Glycine receptors are functionally expressed on bullfrog retinal cone photoreceptors. Neuroscience. 2007;146:427-34 pubmed
    Using immunocytochemical and whole cell recording techniques, we examined expression of glycine receptors on bullfrog retinal cone photoreceptors...
  44. Perkins D, Trudell J, Crawford D, Alkana R, Davies D. Molecular targets and mechanisms for ethanol action in glycine receptors. Pharmacol Ther. 2010;127:53-65 pubmed publisher
    b>Glycine receptors (GlyRs) are recognized as the primary mediators of neuronal inhibition in the spinal cord, brain stem and higher brain regions known to be sensitive to ethanol...
  45. Bluem R, Schmidt E, Corvey C, Karas M, Schlicksupp A, Kirsch J, et al. Components of the translational machinery are associated with juvenile glycine receptors and are redistributed to the cytoskeleton upon aging and synaptic activity. J Biol Chem. 2007;282:37783-93 pubmed
    ..be increased at earlier stages of in vitro differentiation by inhibition of either the ERK1/2 pathway or glycine receptors and simultaneous N-methyl-D-aspartate receptor activation...
  46. Crawford D, Trudell J, Bertaccini E, Li K, Davies D, Alkana R. Evidence that ethanol acts on a target in Loop 2 of the extracellular domain of alpha1 glycine receptors. J Neurochem. 2007;102:2097-2109 pubmed publisher
    Considerable evidence indicates that ethanol acts on specific residues in the transmembrane domains of glycine receptors (GlyRs)...
  47. Gill S, Veruki M, Hartveit E. Functional properties of spontaneous IPSCs and glycine receptors in rod amacrine (AII) cells in the rat retina. J Physiol. 2006;575:739-59 pubmed
    ..We have used rat retinal slices to investigate the functional properties of inhibitory glycine receptors on AII cells by recording spontaneous IPSCs (spIPSCs) in whole cells and glycine-evoked responses in outside-..
  48. Molander A, Söderpalm B. Glycine receptors regulate dopamine release in the rat nucleus accumbens. Alcohol Clin Exp Res. 2005;29:17-26 pubmed
    ..Recently strychnine-sensitive glycine receptors (GlyR) have attracted some interest in this matter...
  49. Madry C, Mesic I, Bartholomäus I, Nicke A, Betz H, Laube B. Principal role of NR3 subunits in NR1/NR3 excitatory glycine receptor function. Biochem Biophys Res Commun. 2007;354:102-8 pubmed
    ..In contrast, receptors assembled from NR1 and NR3 subunits function as calcium-impermeable excitatory glycine receptors that respond to agonist application only with low efficacy...
  50. Cavara N, Orth A, Hollmann M. Effects of NR1 splicing on NR1/NR3B-type excitatory glycine receptors. BMC Neurosci. 2009;10:32 pubmed publisher
    ..members of the NMDAR family, the NR3 subunits, have been reported to assemble with NR1 to form excitatory glycine receptors in heterologous expression systems...
  51. Deleuze C, Runquist M, Orcel H, Rabie A, Dayanithi G, Alonso G, et al. Structural difference between heteromeric somatic and homomeric axonal glycine receptors in the hypothalamo-neurohypophysial system. Neuroscience. 2005;135:475-83 pubmed
    b>Glycine receptors are ionotropic receptors formed by either the homomeric assembly of ligand-binding alpha subunits or the heteromeric combination of an alpha subunit and the auxiliary beta subunit...
  52. Wang D, Mangin J, Moonen G, Rigo J, Legendre P. Mechanisms for picrotoxin block of alpha2 homomeric glycine receptors. J Biol Chem. 2006;281:3841-55 pubmed
    ..the convulsant alkaloid picrotoxin (PTX) can inhibit neuronal gamma-aminobutyric acid (GABA) and homomeric glycine receptors (GlyR)...
  53. Betz H, Laube B. Glycine receptors: recent insights into their structural organization and functional diversity. J Neurochem. 2006;97:1600-10 pubmed
    Strychnine-sensitive glycine receptors (GlyRs) are known to mediate synaptic inhibition in spinal cord, brainstem and other regions of the CNS...