GABAA receptors: Subtypes provide diversity of function and pharmacology

Neuropharmacology

Volumn 56, Issue 1, 2009, Pages 141-148

  Olsen, Richard W ^a   Sieghart, Werner ^b  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b Medical University of Vienna   (Austria)

Author keywords

Allosteric modulators; Chloride channels; GABA; Heteropentamers; Inhibitory neurotransmission

Indexed keywords

3 METHYL 6 (3 TRIFLUOROMETHYLPHENYL) 1,2,4 TRIAZOLO[4,3 B]PYRIDAZINE; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 6 FLUORO 2,9 DIHYDRO 9 METHYL 2 PHENYL 4 (1 PYRROLIDINYLCARBONYL) 1H PYRIDO[3,4 B]INDOL 1 ONE; 7 TERT BUTYL 3 (2,5 DIFLUOROPHENYL) 6 (2 METHYL 2H 1,2,4 TRIAZOL 3 YLMETHOXY) 1,2,4 TRIAZOLO[4,3 B]PYRIDAZINE; 8 AZIDO 5,6 DIHYDRO 5 METHYL 6 OXO 4H IMIDAZO[1,5 A][1,4]BENZODIAZEPINE 3 CARBOXYLIC ACID ETHYL ESTER; ABECARNIL; BENZODIAZEPINE DERIVATIVE; CHLORIDE CHANNEL; CLONAZEPAM; DIAZEPAM; ETOMIDATE; FLUMAZENIL; INDIPLON; ISOFLURANE; NICOTINIC RECEPTOR; PROPOFOL; RECEPTOR SUBTYPE; ZALEPLON; ZOLPIDEM;

ALLOSTERISM; CELLULAR DISTRIBUTION; CHANNEL GATING; DRUG RECEPTOR BINDING; GABAERGIC SYSTEM; HUMAN; NEUROMODULATION; NEUROTRANSMISSION; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN LOCALIZATION; REVIEW;

ANIMALS; CHLORIDE CHANNELS; GABA AGENTS; ION CHANNEL GATING; NEURAL INHIBITION; RECEPTORS, GABA-A;

EID: 58049133111     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2008.07.045     Document Type: Review

References (106)

1. A receptors as a target for the development of novel anxiolytics. Expert Opin. Investig. Drugs 14 (2005) 599-616
2. A receptors. Br. J. Pharmacol. 144 (2005) 357-366
3. A receptors, is a nonsedating anxiolytic in rodents and primates. J. Pharmacol. Exp. Ther. 316 (2006) 410-422
4. A receptor. Mol. Pharmacol. 65 (2004) 68-76
5. Bali, M., Jansen, M., Akabas, M.H. 2007. Spatial relationship between the GABAA receptor β2 M3 region and the α1 subunit preM1 region. SfN abstracts, #441.8.
6. A receptors: classification on the basis of subunit structure and receptor function. Pharmacol. Rev. 50 (1998) 291-313
7. Basile A.S., Lippa A.S., and Skolnick P. Anxioselective anxiolytics: can less be more?. Eur. J. Pharmacol. 500 (2004) 441-451
8. A receptors. Insight into the absolute arrangement. J. Biol. Chem. 277 (2002) 46020-46025
9. Belelli D., Lambert J.J., Peters J.A., Wafford K., and Whiting P.J. The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid. Proc. Natl. Acad. Sci. U.S.A. 94 (1997) 11031-11036
10. Bencsits E., Ebert V., Tretter V., and Sieghart W. A significant part of native gamma -aminobutyric acidA receptors containing alpha 4 subunits do not contain gamma or delta subunits. J. Biol. Chem. 274 (1999) 19613-19616
11. A receptors containing two different types of alpha subunits in murine brain using point-mutated alpha subunits. J. Biol. Chem. 279 (2004) 43654-43660
12. A-receptor subtypes in the spinal cord: an immunohistochemical study. J. Neurosci. 16 (1996) 283-297
13. Boue-Grabot E., Roudbaraki M., Bascles L., Tramu G., Bloch B., and Garret M. Expression of GABA receptor rho subunits in rat brain. J. Neurochem. 70 (1998) 899-907
14. Brejc K., van Dijk W.J., Klaassen R.V., Schuurmans M., van der Oost J., Smit A.B., and Sixma T.K. Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. Nature 411 (2001) 269-276
15. A receptors suggest differential targeting of receptor subtypes. J. Neurosci. 19 (1999) 2960-2973
16. Brown N., Kerby J., Bonnert T.P., Whiting P.J., and Wafford K.A. Pharmacological characterization of a novel cell line expressing human alpha(4)beta(3)delta GABA(A) receptors. Br. J. Pharmacol. 136 (2002) 965-974
17. Burgard E.C., Tietz E.I., Neelands T.R., and Macdonald R.L. Properties of recombinant gamma-aminobutyric acid A receptor isoforms containing the alpha 5 subunit subtype. Mol. Pharmacol. 50 (1996) 119-127
18. Caraiscos V.B., Elliott E.M., You-Ten K.E., Cheng V.Y., Belelli D., Newell J.G., Jackson M.F., Lambert J.J., Rosahl T.W., Wafford K.A., MacDonald J.F., and Orser B.A. Tonic inhibition in mouse hippocampal CA1 pyramidal neurons is mediated by alpha5 subunit-containing gamma-aminobutyric acid type A receptors. Proc. Natl. Acad. Sci. U.S.A. 101 (2004) 3662-3667
19. A beta-subunit homomeric receptors. Neuroreport 7 (1996) 943-947
20. A alpha5 receptors with cognition enhancing properties. J. Med. Chem. 47 (2004) 5829-5832
21. A receptor alpha 4 subunits mediate extrasynaptic inhibition in thalamus and dentate gyrus and the action of gaboxadol. Proc. Natl. Acad. Sci. U.S.A. 103 (2006) 15230-15235
22. Collingridge G.L., Olsen R.W., Peters J., and Spedding M. A nomenclature for ligand-gated ion channels. Neuropharmacology 56 (2009) 2-5
23. A receptor. J. Neurosci. 22 (2002) 5572-5580
24. Corringer P.J., Le Novere N., and Changeux J.P. Nicotinic receptors at the amino acid level. Annu. Rev. Pharmacol. Toxicol. 40 (2000) 431-458
25. Crestani F., Keist R., Fritschy J.-M., Benke D., Vogt K., Prut L., Bluthmann H., Mohler H., and Rudolph U. Trace fear conditioning involves hippocampal alpha5 GABA(A) receptors. Proc. Natl. Acad. Sci. U.S.A. 99 (2002) 8980-8985
26. A receptor structure relieved by AChBP. Trends Biochem. Sci. 27 (2002) 280-287
27. Dellisanti C.D., Yao Y., Stroud J.C., Wang Z.Z., and Chen L. Crystal structure of the extracellular domain of nAChR alpha1 bound to alpha-bungarotoxin at 1.94 A resolution. Nat. Neurosci. 10 (2007) 953-962
28. A receptors in mediating the anxiolytic effects of benzodiazepines. J. Neurosci. 25 (2005) 10682-10688
29. C receptor rho subunits in the mammalian retina. J. Neurosci. 16 (1996) 4479-4490
30. A receptors: limits, insights, future developments. Neuroscience 119 (2003) 933-943
31. A receptor extracellular and transmembrane domains: important insights in pharmacology and function. Mol Pharmacol. 68 (2005) 1291-1300
32. Farrant M., and Nusser Z. Variations on an inhibitory theme: phasic and tonic activation of GABA(A) receptors. Nat. Rev. Neurosci. 6 (2005) 215-229
33. Fritschy J.M., Benke D., Mertens S., Oertel W.H., Bachi T., and Mohler H. Five subtypes of type A gamma-aminobutyric acid receptors identified in neurons by double and triple immunofluorescence staining with subunit-specific antibodies. Proc. Natl. Acad. Sci. U.S.A. 89 (1992) 6726-6730
34. A receptors containing the alpha 1 subunit to neurochemically distinct subpopulations of rat hippocampal interneurons. Eur. J. Neurosci. 6 (1994) 837-853
35. A receptor subtypes: differential association of the alpha 1 and alpha 3 subunits with serotonergic and GABAergic neurons. Neuroscience 54 (1993) 881-892
36. A-receptor subtypes in cholinergic and parvalbumin-positive neurons of the rat and marmoset medial septum-diagonal band complex. Neuroscience 65 (1995) 101-117
37. Glykys J., Peng Z., Chandra D., Homanics G.E., Houser C.R., and Mody I. A new naturally occurring GABA(A) receptor subunit partnership with high sensitivity to ethanol. Nat. Neurosci. 10 (2007) 40-48
38. A receptor agonist with subtype-selective efficacy, as a potential treatment for generalized anxiety disorder and muscle spasms. CNS Drug Rev. 9 (2003) 3-20
39. Gunther U., Benson J., Benke D., Fritschy J.M., Reyes G., Knoflach F., Crestani F., Aguzzi A., Arigoni M., Lang Y., Bluethmann H., Mohler H., and Luscher B. Benzodiazepine-insensitive mice generated by targeted disruption of the gamma 2 subunit gene of gamma-aminobutyric acid type A receptors. Proc. Natl. Acad. Sci. U.S.A. 92 (1995) 7749-7753
40. A receptors. Proc. Natl. Acad. Sci. U.S.A. 103 (2006) 8546-8551
41. A beta subunit isoforms in synaptic and extrasynaptic receptor populations of mouse dentate gyrus granule cells. J. Physiol. 586 (2008) 989-1004
42. A channel subtypes. Mol. Neurobiol. 18 (1998) 35-86
43. Hilf R.J., and Dutzler R. X-ray structure of a prokaryotic pentameric ligand-gated ion channel. Nature 452 (2008) 375-379
44. A receptors through two discrete transmembrane sites. Nature 444 (2006) 486-489
45. A and acetylcholine receptor M3 segments. J. Neurosci. 26 (2006) 4492-4499
46. A receptors containing alpha6 subunits. J. Neurosci. 18 (1998) 2449-2457
47. Jia F., Yue M., Chandra D., Keramidas A., Goldstein P.A., Homanics G.E., and Harrison N.L. Taurine is a potent activator of extrasynaptic GABA(A) receptors in the thalamus. J. Neurosci. 28 (2008) 106-115
48. Jurd R., Arras M., Lambert S., Drexler B., Siegwart R., Crestani F., Zaugg M., Vogt K.E., Ledermann B., Antkowiak B., and Rudolph U. General anesthetic actions in vivo strongly attenuated by a point mutation in the GABA(A) receptor beta3 subunit. Faseb. J. 17 (2003) 250-252
49. Korpi E.R., Mihalek R.M., Sinkkonen S.T., Hauer B., Hevers W., Homanics G.E., Sieghart W., and Luddens H. Altered receptor subtypes in the forebrain of GABA(A) receptor delta subunit-deficient mice: recruitment of gamma 2 subunits. Neuroscience 109 (2002) 733-743
50. Koulen P., Brandstatter J.H., Enz R., Bormann J., and Wassle H. Synaptic clustering of GABA(C) receptor rho-subunits in the rat retina. Eur. J. Neurosci. 10 (1998) 115-127
51. Areceptor anesthetic binding sites identified at subunit interfaces by photolabeling. J. Neurosci. 26 (2006) 11599-11605
52. Li M., and DeBlas A. Coexistence of two beta subunit isoforms in the same gamma-aminobutyric acid type A receptor. J. Biol. Chem. 272 (1997) 16564-16569
53. A receptors. J. Neurosci. 26 (2006) 1749-1758
54. Low K., Crestani F., Keist R., Benke D., Brunig I., Benson J.A., Fritschy J.M., Rulicke T., Bluethmann H., Mohler H., and Rudolph U. Molecular and neuronal substrate for the selective attenuation of anxiety. Science 290 (2000) 131-134
55. A receptor channels. Annu. Rev. Neurosci. 17 (1994) 569-602
56. A receptors. J. Physiol. 515 Pt 3 (1999) 711-727
57. McKernan R.M., Rosahl T.W., Reynolds D.S., Sur C., Wafford K.A., Atack J.R., Farrar S., Myers J., Cook G., Ferris P., Garrett L., Bristow L., Marshall G., Macaulay A., Brown N., Howell O., Moore K.W., Carling R.W., Street L.J., Castro J.L., Ragan C.I., Dawson G.R., and Whiting P.J. Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype. Nat. Neurosci. 3 (2000) 587-592
58. Mihic S.J., Ye Q., Wick M.J., Koltchine V.V., Krasowski M.D., Finn S.E., Mascia M.P., Valenzuela C.F., Hanson K.K., Greenblatt E.P., Harris R.A., and Harrison N.L. Sites of alcohol and volatile anaesthetic action on GABA(A) and glycine receptors. Nature 389 (1997) 385-389
59. C receptor subunits in native central neurons. J. Neurosci. 24 (2004) 7241-7250
60. A receptor diversity and pharmacology. Cell Tissue Res. 326 (2006) 505-516
61. Mody I., and Pearce R.A. Diversity of inhibitory neurotransmission through GABA(A) receptors. Trends Neurosci. 27 (2004) 569-575
62. Moragues N., Ciofi P., Lafon P., Odessa M.F., Tramu G., and Garret M. cDNA cloning and expression of a gamma-aminobutyric acid A receptor epsilon-subunit in rat brain. Eur. J. Neurosci. 12 (2000) 4318-4330
63. Moragues N., Ciofi P., Tramu G., and Garret M. Localisation of GABA(A) receptor epsilon-subunit in cholinergic and aminergic neurones and evidence for co-distribution with the theta-subunit in rat brain. Neuroscience 111 (2002) 657-669
64. A receptors on rat hippocampal pyramidal neurons. J. Physiol. 577 (2006) 841-856
65. Nusser Z., and Mody I. Selective modulation of tonic and phasic inhibitions in dentate gyrus granule cells. J. Neurophysiol. 87 (2002) 2624-2628
66. A receptor in relation to specific GABAergic synapses in the dentate gyrus. Eur. J. Neurosci. 7 (1995) 630-646
67. A receptors to synaptic and extrasynaptic membranes of cerebellar granule cells. J. Neurosci. 18 (1998) 1693-1703
68. A receptor subtypes in the cerebellum of alpha1-subunit-deficient mice. J. Neurochem. 96 (2006) 136-147
69. A receptors: insights from mutant and knockout mice. In: Martin D.L., and Olsen R.W. (Eds). GABA in the Nervous System: The View at 50 Years (2000), Lippincott, Williams & Wilkins, Philadelphia 81-96
70. A receptors: classification on the basis of subunit composition, pharmacology, and function. Pharmacol Rev, in press. doi:10.1124/pr.108.000505.
71. A gamma2S, glycine alpha1 and glycine alpha2 receptor subunits in vitro. Eur. J. Neurosci. 12 (2000) 3137-3145
72. A receptor subunits in the rat CNS. J. Comp. Neurol. 326 (1992) 193-216
73. Pirker S., Schwarzer C., Wieselthaler A., Sieghart W., and Sperk G. GABA(A) receptors: immunocytochemical distribution of 13 subunits in the adult rat brain. Neuroscience 101 (2000) 815-850
74. A receptor subtypes in the cerebellum of mouse and rat. J. Neurochem. 87 (2003) 1444-1455
75. Reynolds D.S., Rosahl T.W., Cirone J., O'Meara G.F., Haythornthwaite A., Newman R.J., Myers J., Sur C., Howell O., Rutter A.R., Atack J., Macaulay A.J., Hadingham K.L., Hutson P.H., Belelli D., Lambert J.J., Dawson G.R., McKernan R., Whiting P.J., and Wafford K.A. Sedation and anesthesia mediated by distinct GABA(A) receptor isoforms. J. Neurosci. 23 (2003) 8608-8617
76. Rossi D.J., Hamann M., and Attwell D. Multiple modes of GABAergic inhibition of rat cerebellar granule cells. J. Physiol. 548 (2003) 97-110
77. Rudolph U., and Antkowiak B. Molecular and neuronal substrates for general anaesthetics. Nat. Rev. Neurosci. 5 (2004) 709-720
78. Rudolph U., Crestani F., Benke D., Brunig I., Benson J.A., Fritschy J.M., Martin J.R., Bluethmann H., and Mohler H. Benzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypes. Nature 401 (1999) 796-800
79. A receptor function and dissection of the pharmacology of benzodiazepines and general anesthetics through mouse genetics. Annu. Rev. Pharmacol. Toxicol. 44 (2004) 475-498
80. A receptors. Br. J. Pharmacol. 142 (2004) 97-106
81. A receptor subunits: role of the delta subunit. J. Neurosci. 14 (1994) 7077-7086
82. A receptors: modulating gain and maintaining the tone. Trends Neurosci. 27 (2004) 262-269
83. A-benzodiazepine receptors. Trends Pharmacol. Sci. 10 (1989) 407-411
84. A receptor subtypes. Pharmacol. Rev. 47 (1995) 181-234
85. A receptor subtypes. Curr. Top. Med. Chem. 2 (2002) 795-816
86. A receptors. Trends Pharmacol. Sci. 18 (1997) 425-429
87. Simon J., Wakimoto H., Fujita N., Lalande M., and Barnard E.A. Analysis of the set of GABA(A) receptor genes in the human genome. J. Biol. Chem. 279 (2004) 41422-41435
88. Sine S.M., and Engel A.G. Recent advances in Cys-loop receptor structure and function. Nature 440 (2006) 448-455
89. A receptors. Trends Pharmacol. Sci. 16 (1995) 162-168
90. Sohal V.S., Keist R., Rudolph U., and Huguenard J.R. Dynamic GABA(A) receptor subtype-specific modulation of the synchrony and duration of thalamic oscillations. J. Neurosci. 23 (2003) 3649-3657
91. A receptor is concentrated in synaptic junctions containing the alpha 1 and beta 2/3 subunits in hippocampus, cerebellum and globus pallidus. Neuropharmacology 35 (1996) 1425-1444
92. A receptors. Proc. Natl. Acad. Sci. U.S.A. 100 (2003) 14439-14444
93. Sternfeld F., Carling R.W., Jelley R.A., Ladduwahetty T., Merchant K.J., Moore K.W., Reeve A.J., Street L.J., O'Connor D., Sohal B., Atack J.R., Cook S., Seabrook G., Wafford K., Tattersall F.D., Collinson N., Dawson G.R., Castro J.L., and MacLeod A.M. Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers. J. Med. Chem. 47 (2004) 2176-2179
94. Sur C., Quirk K., Dewar D., Atack J., and McKernan R. Rat and human hippocampal alpha5 subunit-containing gamma-aminobutyric AcidA receptors have alpha5 beta3 gamma2 pharmacological characteristics. Mol. Pharmacol. 54 (1998) 928-933
95. A receptor subtype. J. Neurosci. 17 (1997) 2728-2737
96. Tretter V., Hauer B., Nusser Z., Mihalek R.M., Hoger H., Homanics G.E., Somogyi P., and Sieghart W. Targeted disruption of the GABA(A) receptor delta subunit gene leads to an up-regulation of gamma 2 subunit-containing receptors in cerebellar granule cells. J. Biol. Chem. 276 (2001) 10532-10538
97. Unwin N. Structure and action of the nicotinic acetylcholine receptor explored by electron microscopy. FEBS Lett. 555 (2003) 91-95
98. Unwin N. Refined structure of the nicotinic acetylcholine receptor at 4A resolution. J. Mol. Biol. 346 (2005) 967-989
99. Wallner M., Hanchar H.J., and Olsen R.W. Ethanol enhances alpha 4 beta 3 delta and alpha 6 beta 3 delta gamma-aminobutyric acid type A receptors at low concentrations known to affect humans. Proc. Natl. Acad. Sci. U.S.A. 100 (2003) 15218-15223
100. Wegelius K., Pasternack M., Hiltunen J.O., Rivera C., Kaila K., Saarma M., and Reeben M. Distribution of GABA receptor rho subunit transcripts in the rat brain. Eur. J. Neurosci. 10 (1998) 350-357
101. Whiting P.J. GABA-A receptors: a viable target for novel anxiolytics?. Curr. Opin. Pharmacol. 6 (2006) 24-29
102. A receptors based on subunit composition. In: Martin D.L., and Olsen R.W. (Eds). GABA in the Nervous System: the View at Fifty Years (2000), Lippincott Williams & Wilkins, Philadelphia 113-126
103. A receptor subunit mRNAs in the rat brain. I. Telencephalon, diencephalon, mesencephalon. J. Neurosci. 12 (1992) 1040-1062
104. Wohlfarth K.M., Bianchi M.T., and Macdonald R.L. Enhanced neurosteroid potentiation of ternary GABA(A) receptors containing the delta subunit. J. Neurosci. 22 (2002) 1541-1549
105. Yamakura T., Bertaccini E., Trudell J.R., and Harris R.A. Anesthetics and ion channels: molecular models and sites of action. Annu. Rev. Pharmacol. Toxicol. 41 (2001) 23-51
106. A receptors to a dopamine hyperfunction. Proc. Natl. Acad. Sci. U.S.A. 102 (2005) 17154-17159