gaba receptors


Summary: Cell-surface proteins that bind GAMMA-AMINOBUTYRIC ACID with high affinity and trigger changes that influence the behavior of cells. GABA-A receptors control chloride channels formed by the receptor complex itself. They are blocked by bicuculline and usually have modulatory sites sensitive to benzodiazepines and barbiturates. GABA-B receptors act through G-proteins on several effector systems, are insensitive to bicuculline, and have a high affinity for L-baclofen.

Top Publications

  1. Park J, Han J, Kim S, Park J, Go D, Sun B, et al. Spinal GABA receptors mediate the suppressive effect of electroacupuncture on cold allodynia in rats. Brain Res. 2010;1322:24-9 pubmed publisher
    ..These results suggest that spinal GABA(A) and GABA(B) receptors mediate the suppressive effect of low frequency EA on cold allodynia in the tail neuropathic rats. ..
  2. Yazaki Sugiyama Y, Kang S, Câteau H, Fukai T, Hensch T. Bidirectional plasticity in fast-spiking GABA circuits by visual experience. Nature. 2009;462:218-21 pubmed publisher
    ..Together these results suggest that the bidirectional recruitment of an initially binocular GABA circuit may contribute to experience-dependent plasticity in the developing visual cortex. ..
  3. Wegner F, Kraft R, Busse K, Hartig W, Schaarschmidt G, Schwarz S, et al. Functional and molecular analysis of GABA receptors in human midbrain-derived neural progenitor cells. J Neurochem. 2008;107:1056-69 pubmed publisher
    ..These data indicate that NPCs derived from human fetal midbrain tissue acquire essential GABA(A) receptor properties during neuronal maturation in vitro. ..
  4. Yoon S, Lee B, Kim H, Choi K, Yun J, Jang E, et al. Potential roles of GABA receptors in morphine self-administration in rats. Neurosci Lett. 2007;428:33-7 pubmed
    ..These data suggest that activation of both GABA(A) and GABA(B) receptors may be effective in suppressing the reinforcing effects of morphine. ..
  5. Yuan G, Gao W, Yang Y, Wu Y. Molecular cloning, genomic structure, and genetic mapping of two Rdl-orthologous genes of GABA receptors in the diamondback moth, Plutella xylostella. Arch Insect Biochem Physiol. 2010;74:81-90 pubmed publisher
    ..Two Rdl-orthologous genes of GABA receptors (PxGABARalpha1 and PxGABARalpha2) were cloned and sequenced from a susceptible strain (Roth) of Plutella ..
  6. Dupuis J, Bazelot M, Barbara G, Paute S, Gauthier M, Raymond Delpech V. Homomeric RDL and heteromeric RDL/LCCH3 GABA receptors in the honeybee antennal lobes: two candidates for inhibitory transmission in olfactory processing. J Neurophysiol. 2010;103:458-68 pubmed publisher
    ..calcium concentration potentiated GABA-elicited currents, suggesting a modulating effect of calcium on GABA receptors possibly through phosphorylation processes that remain to be determined...
  7. McCabe A, Easton C, Lischalk J, Moody W. Roles of glutamate and GABA receptors in setting the developmental timing of spontaneous synchronized activity in the developing mouse cortex. Dev Neurobiol. 2007;67:1574-88 pubmed
    ..GABA(A) inhibitors restore SSA in control slices, indicating that the emergence of GABA(A)-mediated inhibition is another major factor that helps terminate SSA. ..
  8. Masugi Tokita M, Shigemoto R. High-resolution quantitative visualization of glutamate and GABA receptors at central synapses. Curr Opin Neurobiol. 2007;17:387-93 pubmed
    ..The two-dimensional view and high sensitivity of SDS-FRL have revealed small, irregularly shaped AMPA receptor clusters within cerebellar synapses. ..
  9. Veenman L, Papadopoulos V, Gavish M. Channel-like functions of the 18-kDa translocator protein (TSPO): regulation of apoptosis and steroidogenesis as part of the host-defense response. Curr Pharm Des. 2007;13:2385-405 pubmed

More Information


  1. Murail S, Robert J, Coic Y, Neumann J, Ostuni M, Yao Z, et al. Secondary and tertiary structures of the transmembrane domains of the translocator protein TSPO determined by NMR. Stabilization of the TSPO tertiary fold upon ligand binding. Biochim Biophys Acta. 2008;1778:1375-81 pubmed publisher
    ..They reveal that the binding of a drug ligand that stimulates cholesterol translocation is able to stabilize the mTSPO tertiary structure. ..
  2. Otera H, Taira Y, Horie C, Suzuki Y, Suzuki H, Setoguchi K, et al. A novel insertion pathway of mitochondrial outer membrane proteins with multiple transmembrane segments. J Cell Biol. 2007;179:1355-63 pubmed
    ..These findings reveal a previously unidentified pathway of the membrane integration of MOM proteins with multiple TMSs. ..
  3. Ouyang C, Guo L, Lu Q, Xu X, Wang H. Enhanced activity of GABA receptors inhibits glutamate release induced by focal cerebral ischemia in rat striatum. Neurosci Lett. 2007;420:174-8 pubmed
    ..receptor, triggered by cerebral ischemia, can be down-regulated by exogenous GABA or by increased activity of GABA receptors, especially the presynaptic GABA(B) receptors, which might be one of the important mechanisms to protect ..
  4. Li P, Rudolph U, Huntsman M. Long-term sensory deprivation selectively rearranges functional inhibitory circuits in mouse barrel cortex. Proc Natl Acad Sci U S A. 2009;106:12156-61 pubmed publisher
  5. Martyniuk C, Aris Brosou S, Drouin G, Cahn J, Trudeau V. Early evolution of ionotropic GABA receptors and selective regimes acting on the mammalian-specific theta and epsilon subunits. PLoS ONE. 2007;2:e894 pubmed
    ..We discuss potential consequences for the evolution of mammals and of their CNS. ..
  6. Shoukrun R, Veenman L, Shandalov Y, Leschiner S, Spanier I, Karry R, et al. The 18-kDa translocator protein, formerly known as the peripheral-type benzodiazepine receptor, confers proapoptotic and antineoplastic effects in a human colorectal cancer cell line. Pharmacogenet Genomics. 2008;18:977-88 pubmed publisher
    ..In-vivo pharmacological treatment with the putative TSPO agonist FGIN-1-27 reduces tumor growth of the HT29 cell line. These data suggest that TSPO involvement in apoptosis provides a target for anticancer treatment. ..
  7. Zhang F, Li C, Wang R, Han D, Zhang Q, Zhou C, et al. Activation of GABA receptors attenuates neuronal apoptosis through inhibiting the tyrosine phosphorylation of NR2A by Src after cerebral ischemia and reperfusion. Neuroscience. 2007;150:938-49 pubmed
    ..immunoprecipitation and histology analysis to evaluate the neuroprotective effects by stimulating GABA receptors in rat four-vessel occlusion (4-VO) ischemic model, and to investigate the potential mechanism...
  8. Xing J, Li D, Li J. Role of GABA receptors in nitric oxide inhibition of dorsolateral periaqueductal gray neurons. Neuropharmacology. 2008;54:734-44 pubmed publisher
    ..The purpose of this report was to investigate the role of GABA receptors in NO modulation of neuronal activity through inhibitory and excitatory synaptic inputs within the ..
  9. Johnston G, Hanrahan J, Chebib M, Duke R, Mewett K. Modulation of ionotropic GABA receptors by natural products of plant origin. Adv Pharmacol. 2006;54:285-316 pubmed
  10. Kugler W, Veenman L, Shandalov Y, Leschiner S, Spanier I, Lakomek M, et al. Ligands of the mitochondrial 18 kDa translocator protein attenuate apoptosis of human glioblastoma cells exposed to erucylphosphohomocholine. Cell Oncol. 2008;30:435-50 pubmed
  11. Draguhn A, Axmacher N, Kolbaev S. Presynaptic ionotropic GABA receptors. Results Probl Cell Differ. 2008;44:69-85 pubmed the spinal cord, recent work has revealed an astonishing abundance and diversity of presynaptic ionotropic GABA receptors. While modern techniques allow for detailed studies at the cellular and molecular level in almost all regions ..
  12. Law R, Lightstone F. Modeling neuronal nicotinic and GABA receptors: important interface salt-links and protein dynamics. Biophys J. 2009;97:1586-94 pubmed publisher
    ..Homology models of the alpha4beta2 nicotinic acetylcholine (nACh) and beta2alpha1gamma2 GABA receptors were constructed based on the torpedo neuromuscular-like nicotinic receptor structure...
  13. Galvan A, Kuwajima M, Smith Y. Glutamate and GABA receptors and transporters in the basal ganglia: what does their subsynaptic localization reveal about their function?. Neuroscience. 2006;143:351-75 pubmed
  14. Maison S, Rosahl T, Homanics G, Liberman M. Functional role of GABAergic innervation of the cochlea: phenotypic analysis of mice lacking GABA(A) receptor subunits alpha 1, alpha 2, alpha 5, alpha 6, beta 2, beta 3, or delta. J Neurosci. 2006;26:10315-26 pubmed
    ..Results suggest that the GABAergic component of the olivocochlear system contributes to the long-term maintenance of hair cells and neurons in the inner ear. ..
  15. Kanold P, Shatz C. Subplate neurons regulate maturation of cortical inhibition and outcome of ocular dominance plasticity. Neuron. 2006;51:627-38 pubmed
    ..Thus, subplate neurons regulate molecular machinery required to establish an adult balance of excitation and inhibition in layer 4, and thereby influence the outcome of OD plasticity. ..
  16. Han D, Zhang Q, Yong Liu -, Li C, Zong Y, Yu C, et al. Co-activation of GABA receptors inhibits the JNK3 apoptotic pathway via the disassembly of the GluR6-PSD95-MLK3 signaling module in cerebral ischemic-reperfusion. FEBS Lett. 2008;582:1298-306 pubmed publisher
    ..Our results suggest that stimulation of the inhibitory GABA receptors can attenuate the excitatory JNK3 apoptotic signaling pathway via inhibiting the increased assembly of the ..
  17. Dubrovina N, Zinov ev D. Contribution of GABA receptors to extinction of memory traces in normal conditions and in a depression-like state. Neurosci Behav Physiol. 2008;38:775-9 pubmed publisher
    A relationship between the effects of activation and blockade of GABA receptors on extinction of a conditioned passive avoidance reaction on the one hand and the type of receptor and initial psychoemotional state on the other was found in ..
  18. Zeno S, Zaaroor M, Leschiner S, Veenman L, Gavish M. CoCl(2) induces apoptosis via the 18 kDa translocator protein in U118MG human glioblastoma cells. Biochemistry. 2009;48:4652-61 pubmed publisher
    ..In conclusion, our studies show that activation of TSPO by CoCl(2) application is required for ROS generation, leading to cardiolipin oxidation, and collapse of the Deltapsi(m), as induced by CoCl(2). ..
  19. Franks N. General anaesthesia: from molecular targets to neuronal pathways of sleep and arousal. Nat Rev Neurosci. 2008;9:370-86 pubmed publisher
    ..Recent work suggests that the thalamus and the neuronal networks that regulate its activity are the key to understanding how anaesthetics cause loss of consciousness. ..
  20. Veenman L, Shandalov Y, Gavish M. VDAC activation by the 18 kDa translocator protein (TSPO), implications for apoptosis. J Bioenerg Biomembr. 2008;40:199-205 pubmed publisher
    ..These data provide an understanding regarding the mechanisms whereby VDAC and TSPO may serve as targets to modulate apoptotic rates. This has implications for drug design to treat diseases such as neurodegeneration and cancer. ..
  21. Li C, Xu B, Wang W, Yu X, Zhu J, Yu H, et al. Coactivation of GABA receptors inhibits the JNK3 apoptotic pathway via disassembly of GluR6-PSD-95-MLK3 signaling module in KA-induced seizure. Epilepsia. 2010;51:391-403 pubmed publisher
    ..Taken together, we demonstrate that coactivation of the inhibitory GABA receptors can attenuate the excitatory JNK3 apoptotic signaling pathway via inhibiting the increased assembly of the ..
  22. Skilbeck K, Johnston G, Hinton T. Stress and GABA receptors. J Neurochem. 2010;112:1115-30 pubmed publisher
    ..The short- and long-term stress sensitivity of the GABAergic system implicates GABA(A) receptors in the non-genetic etiology of psychiatric illnesses such as depression and schizophrenia in which stress may be an important factor. ..
  23. Tsang S, Ng S, Xu Z, Xue H. The evolution of GABAA receptor-like genes. Mol Biol Evol. 2007;24:599-610 pubmed
  24. Harvey V, Duguid I, Krasel C, Stephens G. Evidence that GABA rho subunits contribute to functional ionotropic GABA receptors in mouse cerebellar Purkinje cells. J Physiol. 2006;577:127-39 pubmed
    ..cells (PCs) using agents reported to have increased affinity for rho subunit-containing GABA(C) over other GABA receptors. Exogenous application of the GABA(C)-preferring agonist cis-4-aminocrotonic acid (CACA) evoked whole-cell ..
  25. Harrison N, Lummis S. Molecular modeling of the GABA(C) receptor ligand-binding domain. J Mol Model. 2006;12:317-24 pubmed
    ..Figure: see text]. ..
  26. McCann C, Bracamontes J, Steinbach J, Sanes J. The cholinergic antagonist alpha-bungarotoxin also binds and blocks a subset of GABA receptors. Proc Natl Acad Sci U S A. 2006;103:5149-54 pubmed
    ..These results introduce a previously unrecognized tool for analysis of GABA(A)Rs but may complicate interpretation of some studies on neuronal nAChRs. ..
  27. Paul S. Alcohol-sensitive GABA receptors and alcohol antagonists. Proc Natl Acad Sci U S A. 2006;103:8307-8 pubmed
  28. Galvan A, Villalba R, West S, Maidment N, Ackerson L, Smith Y, et al. GABAergic modulation of the activity of globus pallidus neurons in primates: in vivo analysis of the functions of GABA receptors and GABA transporters. J Neurophysiol. 2005;94:990-1000 pubmed
    ..The effects of GABA on pallidal activity depend on the synaptic localization of GABA receptors and the distribution and activity of GABA transporters (GATs)...
  29. Vigh J, von Gersdorff H. Prolonged reciprocal signaling via NMDA and GABA receptors at a retinal ribbon synapse. J Neurosci. 2005;25:11412-23 pubmed
  30. Lummis S, L Beene D, Harrison N, Lester H, Dougherty D. A cation-pi binding interaction with a tyrosine in the binding site of the GABAC receptor. Chem Biol. 2005;12:993-7 pubmed
    ..Comparisons among four homologous receptors show variations in cation-pi binding energies that reflect the nature of the cationic center of the agonist. ..
  31. Buesa I, Ortiz V, Aguilera L, Torre F, Zimmermann M, Azkue J. Disinhibition of spinal responses to primary afferent input by antagonism at GABA receptors in urethane-anaesthetised rats is dependent on NMDA and metabotropic glutamate receptors. Neuropharmacology. 2006;50:585-94 pubmed
  32. Hosie A, Buckingham S, Hamon A, Sattelle D. Replacement of asparagine with arginine at the extracellular end of the second transmembrane (M2) region of insect GABA receptors increases sensitivity to penicillin G. Invert Neurosci. 2006;6:75-9 pubmed
    ..The A301S mutation that confers resistance to dieldrin did not significantly affect the antagonism by PCG. ..
  33. Papadopoulos V, Baraldi M, Guilarte T, Knudsen T, Lacapere J, Lindemann P, et al. Translocator protein (18kDa): new nomenclature for the peripheral-type benzodiazepine receptor based on its structure and molecular function. Trends Pharmacol Sci. 2006;27:402-9 pubmed
    ..Translocator protein (18kDa) is proposed as a new name, regardless of the subcellular localization of the protein. ..
  34. Yu Y, Cao L, Yang X. Modulation by brain natriuretic peptide of GABA receptors on rat retinal ON-type bipolar cells. J Neurosci. 2006;26:696-707 pubmed
    ..We therefore conclude that the increased calcium release from ryanodine-sensitive calcium stores by BNP may be responsible for the BNP-caused GABAA response suppression in ON-type BCs through stimulating calmodulin. ..
  35. Buckingham S, Biggin P, Sattelle B, Brown L, Sattelle D. Insect GABA receptors: splicing, editing, and targeting by antiparasitics and insecticides. Mol Pharmacol. 2005;68:942-51 pubmed
    Ionotropic GABA receptors are abundant in both vertebrate and invertebrate nervous systems, where they mediate rapid, mostly inhibitory synaptic transmission...
  36. Gwak Y, Tan H, Nam T, Paik K, Hulsebosch C, Leem J. Activation of spinal GABA receptors attenuates chronic central neuropathic pain after spinal cord injury. J Neurotrauma. 2006;23:1111-24 pubmed
  37. Alakuijala A, Alakuijala J, Pasternack M. Evidence for a functional role of GABA receptors in the rat mature hippocampus. Eur J Neurosci. 2006;23:514-20 pubmed
    ..The lack of GABA(C) receptor activation by less intensive stimulation under control conditions suggests that these receptors are extrasynaptic and activated via spillover of synaptically released GABA...
  38. Harrison N, Lummis S. Locating the carboxylate group of GABA in the homomeric rho GABA(A) receptor ligand-binding pocket. J Biol Chem. 2006;281:24455-61 pubmed
  39. Dent J. Evidence for a diverse Cys-loop ligand-gated ion channel superfamily in early bilateria. J Mol Evol. 2006;62:523-35 pubmed
    ..Many of these disappeared from the chordates. Subsequently, selected subunit genes expanded to form large subfamilies. ..
  40. Miyazato M, Sasatomi K, Hiragata S, Sugaya K, Chancellor M, de Groat W, et al. Suppression of detrusor-sphincter dysynergia by GABA-receptor activation in the lumbosacral spinal cord in spinal cord-injured rats. Am J Physiol Regul Integr Comp Physiol. 2008;295:R336-42 pubmed publisher
    ..Decreased activation of GABAA receptors due to hypofunction of GABAergic mechanisms in the spinal cord might be responsible, at least in part, for the development of DSD after SCT. ..
  41. Mancinelli R, Franchitto A, Gaudio E, Onori P, Glaser S, Francis H, et al. After damage of large bile ducts by gamma-aminobutyric acid, small ducts replenish the biliary tree by amplification of calcium-dependent signaling and de novo acquisition of large cholangiocyte phenotypes. Am J Pathol. 2010;176:1790-800 pubmed publisher
    ..We found that both small and large cholangiocytes expressed GABA receptors. GABA: (i) induced apoptosis of large cholangiocytes and reduced large IBDM; (ii) decreased secretin-..
  42. Benes F, Gisabella B. Rat modeling for GABA defects in schizophrenia. Adv Pharmacol. 2006;54:73-93 pubmed
  43. Datta S. Activation of pedunculopontine tegmental PKA prevents GABAB receptor activation-mediated rapid eye movement sleep suppression in the freely moving rat. J Neurophysiol. 2007;97:3841-50 pubmed
    ..These findings suggest that the PPT GABA(B) receptor activation-mediated REM sleep regulating mechanism involves inactivation of cAMP-PKA signaling in the freely moving rat. ..
  44. Grassi S, Frondaroli A, Scarduzio M, Dutia M, Dieni C, Pettorossi V. Effects of 17beta-estradiol on glutamate synaptic transmission and neuronal excitability in the rat medial vestibular nuclei. Neuroscience. 2010;165:1100-14 pubmed publisher
    ..These findings provide evidence for a novel potential mechanism to modulate the responsiveness of vestibular neurons to afferent inputs, and so regulate vestibular function in vivo. ..
  45. Kaja S, Hann V, Payne H, Thompson C. Aberrant cerebellar granule cell-specific GABAA receptor expression in the epileptic and ataxic mouse mutant, Tottering. Neuroscience. 2007;148:115-25 pubmed
  46. Li W, Jin X, Covey D, Steinbach J. Neuroactive steroids and human recombinant rho1 GABAC receptors. J Pharmacol Exp Ther. 2007;323:236-47 pubmed
    ..The data indicate that the binding sites mediating potentiation and inhibition differ from each other and that there are several (three or more) mechanisms for producing inhibition. ..
  47. Mehaffey W, Fernandez F, Maler L, Turner R. Regulation of burst dynamics improves differential encoding of stimulus frequency by spike train segregation. J Neurophysiol. 2007;98:939-51 pubmed
  48. Rupprecht R, Rammes G, Eser D, Baghai T, Schule C, Nothdurfter C, et al. Translocator protein (18 kD) as target for anxiolytics without benzodiazepine-like side effects. Science. 2009;325:490-3 pubmed publisher
    ..Thus, translocator protein (18 kD) ligands are promising candidates for fast-acting anxiolytic drugs with less severe side effects than benzodiazepines. ..
  49. Boyes J, Bolam J. Localization of GABA receptors in the basal ganglia. Prog Brain Res. 2007;160:229-43 pubmed
    ..the diverse roles of GABA in the basal ganglia it is necessary to define the precise localization of GABA receptors in relation to known neuron subtypes and known afferents...
  50. Urschel H, Hanselka L, Gromov I, White L, Baron M. Open-label study of a proprietary treatment program targeting type A gamma-aminobutyric acid receptor dysregulation in methamphetamine dependence. Mayo Clin Proc. 2007;82:1170-8 pubmed
    ..These findings suggest that the efficacy of the medications and of the entire program in treating methamphetamine dependence should be examined in controlled trials. ..
  51. Mejia C, García Alcocer G, Berumen L, Rosas Arellano A, Miledi R, Martinez Torres A. Expression of GABArho subunits during rat cerebellum development. Neurosci Lett. 2008;432:1-6 pubmed publisher
    ..The expression of GABA(C) receptors in the cerebellum adds a new dimension to the regulation of GABAergic neurotransmission and suggests further experiments to determine their functional consequences. ..
  52. Connaughton V, Nelson R, Bender A. Electrophysiological evidence of GABAA and GABAC receptors on zebrafish retinal bipolar cells. Vis Neurosci. 2008;25:139-53 pubmed publisher
    ..In summary, axon terminals contain bicuculline-sensitive GABAA receptors and both picrotoxin-sensitive and insensitive GABAC receptors. Dendritic processes express zinc- and picrotoxin-sensitive GABAC receptors. ..
  53. Kreft M, Zorec R. Anterior pituitary cells excited by GABA. J Physiol. 2008;586:3023-4 pubmed publisher