GABAA receptor subtypes as targets for neuropsychiatric drug development

Pharmacology and Therapeutics

Volumn 109, Issue 1-2, 2006, Pages 12-32

  Korpi, Esa R ^a   Sinkkonen, Saku T ^a  

^a UNIVERSITY OF HELSINKI   (Finland)

Author keywords

Alcoholism; Anxiety; Extrasynaptic receptors; GABAA receptor subtypes; Intrinsic activity; Subtype selectivity

Indexed keywords

3,6,7,9 TETRAHYDRO 2 (3 ISOXAZOLYL)IMIDAZO[4,5 D]PYRANO[4,3 B]PYRIDINE; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; 6 FLUORO 2,9 DIHYDRO 9 METHYL 2 PHENYL 4 (1 PYRROLIDINYLCARBONYL) 1H PYRIDO[3,4 B]INDOL 1 ONE; 7 CHLORO 5,6 DIHYDRO 3 (5 ISOPROPYL 1,2,4 OXADIAZOL 3 YL) 5 METHYL 4H IMIDAZO[1,5 A][1,4]BENZODIAZEPIN 6 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; ALCOHOL; ANESTHETIC AGENT; BENZODIAZEPINE; DIAZEPAM; ENFLURANE; ETOMIDATE; FLURAZEPAM; FUROSEMIDE; GABOXADOL; HALOTHANE; L 655708; LORECLEZOLE; MUSCIMOL; NEUROSTEROID; NGD 91 3; NIFLUMIC ACID; OCINAPLON; PAGOCLONE; PRASTERONE; PROPOFOL; RADEQUINIL; RWJ 51204; RY 023; RY 80; SALICYLIDENE SALICYLHYDRAZIDE; TIAGABINE; TRACAZOLATE; UNCLASSIFIED DRUG; UNINDEXED DRUG; ZALEPLON; ZOLPIDEM; ZOPICLONE;

AGITATION; ALCOHOLISM; AMNESIA; ANXIETY DISORDER; AUTISM; CLINICAL TRIAL; DRUG BINDING; DRUG EFFICACY; DRUG TARGETING; EPILEPSY; GENE CLUSTER; GENETIC LINKAGE; HAPPY PUPPET SYNDROME; HUMAN; HYPNOSIS; MENTAL DISEASE; MOOD DISORDER; NONHUMAN; OPIATE ADDICTION; PRIORITY JOURNAL; PROTEIN EXPRESSION; REVIEW; SCHIZOPHRENIA; SEDATION; SIDE EFFECT; WITHDRAWAL SYNDROME;

ANIMALS; HUMANS; MENTAL DISORDERS; PSYCHOTROPIC DRUGS; RECEPTORS, GABA-A;

EID: 28444445585     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.pharmthera.2005.05.009     Document Type: Review

References (230)

1. K. Abe, C. Takeyama, and K. Yoshimura Effects of S-8510, a novel benzodiazepine receptor partial inverse agonist, on basal forebrain lesioning-induced dysfunction in rats Eur J Pharmacol 347 2-3 1998 145 152
2. A receptor benzodiazepine binding site Curr Drug Target CNS Neurol Disord 2 4 2003 213 232
3. T. Backstrom, A. Andersson, L. Andree, V. Birzniece, M. Bixo, and I. Bjorn Pathogenesis in menstrual cycle-linked CNS disorders Ann N Y Acad Sci 1007 2003 42 53
4. A receptors in hippocampal neurons Mol Pharmacol 59 4 2001 814 824
5. A.N. Bateson Basic pharmacologic mechanisms involved in benzodiazepine tolerance and withdrawal Curr Pharm Des 8 1 2002 5 21
6. A receptor: an old target with new potential? Sleep Med 5 Suppl. 1 2004 S9 S15
7. D. Belelli, J.J. Lambert, J.A. Peters, K. Wafford, and P.J. Whiting The interaction of the general anesthetic etomidate with the γ-aminobutyric acid type A receptor is influenced by a single amino acid Proc Natl Acad Sci U S A 94 20 1997 11031 11036
8. A receptors Neuropharmacology 43 4 2002 651 661
9. F.M. Benes Evidence for altered trisynaptic circuitry in schizophrenic hippocampus Biol Psychiatry 46 5 1999 589 599
10. F.M. Benes, and S. Berretta GABAergic interneurons: implications for understanding schizophrenia and bipolar disorder Neuropsychopharmacology 25 1 2001 1 27
11. A receptors containing two different types of α subunits in murine brain using point-mutated α subunits J Biol Chem 279 42 2004 43654 43660
12. A receptor subtypes J Biol Chem 279 34 2004 35193 35200
13. E.P. Bonetti, W.P. Burkard, M. Gabl, W. Hunkeler, H.P. Lorez, and J.R. Martin Ro 15-4513: partial inverse agonism at the BZR and interaction with ethanol Pharmacol Biochem Behav 31 3 1988 733 749
14. A.E. Boyle, R. Segal, B.R. Smith, and Z. Amit Bidirectional effects of GABAergic agonists and antagonists on maintenance of voluntary ethanol intake in rats Pharmacol Biochem Behav 46 1 1993 179 182
15. C. Braestrup, M. Nielsen, P. Krogsgaard-Larsen, and E. Falch Partial agonists for brain GABA/benzodiazepine receptor complex Nature 280 5720 1979 331 333
16. Brambilla, P., Perez, J., Barale, F., Schettini, G., & Soares, J. C. (2003). GABAergic dysfunction in mood disorders. Mol Psychiatry 8(8), 721-737, 715.
17. A receptors suggest differential targeting of receptor subtypes J Neurosci 19 8 1999 2960 2973
18. A receptors Br J Pharmacol 136 7 2002 965 974
19. A receptor subtypes in hippocampal neurons in vitro J Comp Neurol 443 1 2002 43 55
20. A receptors Ann N Y Acad Sci 1007 2003 29 36
21. A receptor-operated chloride channels: II. Chronic effects of ethanol J Pharmacol Exp Ther 253 2 1990 713 719
22. S.E. Buffett-Jerrott, and S.H. Stewart Cognitive and sedative effects of benzodiazepine use Curr Pharm Des 8 1 2002 45 58
23. J.D. Buxbaum, J.M. Silverman, C.J. Smith, D.A. Greenberg, M. Kilifarski, and J. Reichert Association between a GABRB3 polymorphism and autism Mol Psychiatry 7 3 2002 311 316
24. V.B. Caraiscos, J.G. Newell, K.E. You-Ten, E.M. Elliott, T.W. Rosahl, and K.A. Wafford Selective enhancement of tonic GABAergic inhibition in murine hippocampal neurons by low concentrations of the volatile anesthetic isoflurane J Neurosci 24 39 2004 8454 8458
25. A receptor J Pharmacol Exp Ther 280 3 1997 1284 1295
26. P. Chadderton, T.W. Margrie, and M. Hausser Integration of quanta in cerebellar granule cells during sensory processing Nature 428 6985 2004 856 860
27. A α5 receptor inverse agonist which enhances cognition J Med Chem 46 11 2003 2227 2240
28. A α5 receptors with cognition enhancing properties J Med Chem 47 24 2004 5829 5832
29. R.S. Clarke Adverse effects of intravenously administered drugs used in anaesthetic practice Drugs 22 1 1981 26 41
30. B.J. Cole, M. Hillmann, D. Seidelmann, M. Klewer, and G.H. Jones Effects of benzodiazepine receptor partial inverse agonists in the elevated plus maze test of anxiety in the rat Psychopharmacology (Berl) 121 1 1995 118 126
31. A receptor J Neurosci 22 13 2002 5572 5580
32. E.H. Cook Jr., R.Y. Courchesne, N.J. Cox, C. Lord, D. Gonen, and S.J. Guter Linkage-disequilibrium mapping of autistic disorder, with 15q11-13 markers Am J Hum Genet 62 5 1998 1077 1083
33. S.J. Cooper β-Carbolines characterized as benzodiazepine receptor agonists and inverse agonists produce bi-directional changes in palatable food consumption Brain Res Bull 17 5 1986 627 637
34. A receptor γ2 subunit Neuropharmacology 47 1 2004 17 34
35. J. Covault, J. Gelernter, V. Hesselbrock, M. Nellissery, and H.R. Kranzler Allelic and haplotypic association of GABRA2 with alcohol dependence Am J Med Genet 129B 1 2004 104 109
36. A receptors J Med Chem 41 14 1998 2537 2552
37. A-receptor clustering results in enhanced anxiety and a bias for threat cues Nat Neurosci 2 9 1999 833 839
38. A receptor subtype to the pharmacological actions of benzodiazepine site inverse agonists Neuropharmacology 43 4 2002 679 684
39. A receptors Proc Natl Acad Sci U S A 99 13 2002 8980 8985
40. A receptors in mediating the effects of alcohol in the central nervous system J Psychiatry Neurosci 28 4 2003 263 274
41. A. De Bruyn, D. Souery, K. Mendelbaum, J. Mendlewicz, and C. Van Broeckhoven A linkage study between bipolar disorder and genes involved in dopaminergic and GABAergic neurotransmission Psychiatr Genet 6 2 1996 67 73
42. T.M. DeLorey, and R.W. Olsen GABA and epileptogenesis: comparing GABRB3 gene-deficient mice with Angelman syndrome in man Epilepsy Res 36 2-3 1999 123 132
43. D.M. Dick, H.J. Edenberg, X. Xuei, A. Goate, S. Kuperman, and M. Schuckit Association of GABRG3 with alcohol dependence Alcohol Clin Exp Res 28 1 2004 4 9
44. A receptor genes on chromosome 5 with alcoholism in the collaborative study on the genetics of alcoholism sample Am J Med Genet, Part B Neuropsychiatr Genet 132 1 2005 24 28
45. R. Dorow, R. Horowski, G. Paschelke, and M. Amin Severe anxiety induced by FG 7142, a β-carboline ligand for benzodiazepine receptors Lancet 2 8341 1983 98 99
46. T. Duka, V. Edelmann, B. Schutt, and R. Dorow β-Carbolines as tools in memory research: human data with the β-carboline ZK 93426 Psychopharmacol Ser 6 1988 246 260
47. A receptor reveals the importance of residue 101 in determining the allosteric effects of benzodiazepine site ligands Mol Pharmacol 56 4 1999 768 774
48. B. Ebert, K.A. Wafford, P.J. Whiting, P. Krogsgaard-Larsen, and J.A. Kemp Molecular pharmacology of γ-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different α, β, and γ receptor subunit combinations Mol Pharmacol 46 1994 957 963
49. B. Ebert, S.A. Thompson, K. Saounatsou, R. McKernan, P. Krogsgaard-Larsen, and K.A. Wafford Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human γ-aminobutyric acid type A receptors Mol Pharmacol 52 6 1997 1150 1156
50. A receptor, are associated with alcohol dependence and with brain oscillations Am J Hum Genet 74 4 2004 705 714
51. H. Eriksson, J. Haasio, and K. Korttila Comparison of eltanolone and thiopental in anaesthesia for termination of pregnancy Acta Anaesthesiol Scand 39 4 1995 479 484
52. A receptors: limits, insights, future developments Neuroscience 119 4 2003 933 943
53. J.G. Evans, G. Wilcock, and J. Birks Evidence-based pharmacotherapy of Alzheimer's disease Int J Neuropsychopharmacol 7 3 2004 351 369
54. J. Fastbom, Y. Forsell, and B. Winblad Benzodiazepines may have protective effects against Alzheimer disease Alzheimer Dis Assoc Disord 12 1 1998 14 17
55. A agonist THIP produces slow wave sleep and reduces spindling activity in NREM sleep in humans Psychopharmacology (Berl) 130 3 1997 285 291
56. A receptor β3 subunit gene and psychiatric morbidity in a post-traumatic stress disorder population Psychiatry Res 104 2 2001 109 117
57. U. Günther, J. Benson, D. Benke, J.M. Fritschy, G. Reyes, and F. Knoflach Benzodiazepine-insensitive mice generated by targeted disruption of the γ2 subunit gene of γ-aminobutyric acid type A receptors Proc Natl Acad Sci U S A 92 17 1995 7749 7753
58. M. Hamann, D.J. Rossi, and D. Attwell Tonic and spillover inhibition of granule cells control information flow through cerebellar cortex Neuron 33 4 2002 625 633
59. A receptors are mediated by the β subunit Neuropharmacology 45 3 2003 293 303
60. A receptor ε subunit mRNA in locus coeruleus neurons NeuroReport 12 13 2001 2981 2985
61. K. Hellevuo, and E.R. Korpi Failure of Ro 15-4513 to antagonize ethanol in rat lines selected for differential sensitivity to ethanol and in Wistar rats Pharmacol Biochem Behav 30 1 1988 183 188
62. K. Hellevuo, K. Kiianmaa, and E.R. Korpi Effect of GABAergic drugs on motor impairment from ethanol, barbital and lorazepam in rat lines selected for differential sensitivity to ethanol Pharmacol Biochem Behav 34 2 1989 399 404
63. A channel subtypes Mol Neurobiol 18 1 1998 35 86
64. A receptors in vitro NeuroReport 11 18 2000 4103 4106
65. A receptor α3-subunit gene Nucleic Acids Res 19 14 1991 4016
66. A.J. Hiltunen, and T.U. Jarbe Ro 15-4513 does not antagonize the discriminative stimulus- or rate-depressant effects of ethanol in rats Alcohol 5 3 1988 203 207
67. R. Hoehn-Saric Effects of THIP on chronic anxiety Psychopharmacology (Berl) 80 4 1983 338 341
68. G.E. Homanics, T.M. DeLorey, L.L. Firestone, J.J. Quinlan, A. Handforth, and N.L. Harrison Mice devoid of γ-aminobutyrate type A receptor b3 subunit have epilepsy, cleft palate, and hypersensitive behavior Proc Natl Acad Sci U S A 94 8 1997 4143 4148
69. G.E. Homanics, F.P. Elsen, S.W. Ying, A. Jenkins, C. Ferguson, and B. Sloat A gain-of-function mutation in the GABA receptor produces synaptic and behavioral abnormalities in the mouse Genes Brain Behav 4 1 2005 10 19
70. Y. Horiuchi, J. Nakayama, H. Ishiguro, T. Ohtsuki, S.D. Detera-Wadleigh, and T. Toyota Possible association between a haplotype of the GABA-A receptor a1 subunit gene (GABRA1) and mood disorders Biol Psychiatry 55 1 2004 40 45
71. A α6 Pro385Ser substitution and benzodiazepine sensitivity Am J Psychiatry 156 9 1999 1447 1449
72. A receptor J Neurosci 21 6 2001 RC136
73. B receptors in the hippocampus J Neurophysiol 90 4 2003 2690 2701
74. A receptor α6 subunit gene inactivation inhibits δ subunit expression J Neurosci 17 4 1997 1350 1362
75. H.L. June, and M.J. Lewis Ro15-4513 enhances and attenuates motor stimulant effects of ethanol in rats Alcohol 6 3 1989 245 248
76. H.L. June, G.H. Lummis, R.E. Colker, T.O. Moore, and M.J. Lewis Ro15-4513 attenuates the consumption of ethanol in deprived rats Alcohol Clin Exp Res 15 3 1991 406 411
77. H.L. June, J.M. Murphy, R.L. Hewitt, T.L. Greene, M. Lin, and J.J. Mellor-Burke Benzodiazepine receptor ligands with different intrinsic efficacies alter ethanol intake in alcohol-nonpreferring (NP) rats Neuropsychopharmacology 14 1 1996 55 66
78. H.L. June, S.L. Devaraju, M.W. Eggers, J.A. Williams, C.R. Cason, and T.L. Greene Benzodiazepine receptor antagonists modulate the actions of ethanol in alcohol-preferring and -nonpreferring rats Eur J Pharmacol 342 2-3 1998 139 151
79. A receptors containing α5 subunits in the CA1 and CA3 hippocampal fields regulate ethanol-motivated behaviors: an extended ethanol reward circuitry J Neurosci 21 6 2001 2166 2177
80. A1 receptors in the ventral pallidum Neuropsychopharmacology 28 12 2003 2124 2137
81. A receptor β3 subunit FASEB J 17 2 2003 250 252
82. H. Kallela, J. Haasio, and K. Korttila Comparison of eltanolone and propofol in anesthesia for termination of pregnancy Anesth Analg 79 3 1994 512 516
83. K. Kawasaki, M. Eigyo, M. Ikeda, T. Kihara, K. Koike, and A. Matsushita A novel benzodiazepine inverse agonist, S-8510, as a cognitive enhancer Prog Neuropsychopharmacol Biol Psychiatry 20 8 1996 1413 1425
84. J.F. Kerrigan, W.D. Shields, T.Y. Nelson, D.L. Bluestone, W.E. Dodson, and B.F. Bourgeois Ganaxolone for treating intractable infantile spasms: a multicenter, open-label, add-on trial Epilepsy Res 42 2-3 2000 133 139
85. M. Kjaer, and H. Nielsen The analgesic effect of the GABA-agonist THIP in patients with chronic pain of malignant origin. A phase-1-2 study Br J Clin Pharmacol 16 5 1983 477 485
86. M. Kneussel, and H. Betz Receptors, gephyrin and gephyrin-associated proteins: novel insights into the assembly of inhibitory postsynaptic membrane specializations J Physiol 525 Pt 1 2000 1 9
87. E.R. Korpi, T. Kuner, P.H. Seeburg, and H. Lüddens Selective antagonist for the cerebellar granule cell-specific γ-aminobutyric acid type A receptor Mol Pharmacol 47 2 1995 283 289
88. A receptors Prog Neurobiol 67 2 2002 113 159
89. A receptor δ subunit-deficient mice: recruitment of γ2 subunits Neuroscience 109 4 2002 733 743
90. S. Korsgaard, D.E. Casey, J. Gerlach, O. Hetmar, B. Kaldan, and L.B. Mikkelsen The effect of tetrahydroisoxazolopyridinol (THIP) in tardive dyskinesia: a new γ-aminobutyric acid agonist Arch Gen Psychiatry 39 9 1982 1017 1021
91. A agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic Biochem Pharmacol 68 8 2004 1573 1580
92. J. Kuhmonen, J. Lukkarinen, O. Grohn, J. Jolkkonen, and J. Sivenius Diazepam does not reduce infarct size in rats subjected to transient occlusion of the middle cerebral artery when normothermia is maintained J Pharm Pharmacol 54 11 2002 1565 1569
93. A receptors in the CNS: where and why? Prog Biophys Mol Biol 87 1 2005 33 46
94. E. Kulonen Ethanol and GABA Med Biol 61 3 1983 147 167
95. A receptors: genomic and nongenomic mechanisms Pharmacol Ther 101 3 2004 211 226
96. A receptors Prog Neurobiol 71 1 2003 67 80
97. A agonist THIP increases non-REM sleep and enhances non-REM sleep-specific delta activity in the rat during the dark period Sleep 20 12 1997 1099 1104
98. A receptors in the regulation of sleep: initial sleep responses to peripherally administered modulators and agonists Sleep 22 1 1999 33 42
99. A agonist THIP (gaboxadol) increases non-REM sleep and enhances delta activity in the rat NeuroReport 7 13 1996 2241 2245
100. A) agonist 4,5,6, 7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol persistently increases sleep maintenance and intensity during chronic administration to rats J Pharmacol Exp Ther 293 3 2000 1084 1090
101. A agonist gaboxadol on nocturnal sleep and hormone secretion in healthy elderly subjects Am J Physiol: Endocrinol Metab 281 1 2001 E130 E137
102. P.A. Lapchak, and D.M. Araujo Preclinical development of neurosteroids as neuroprotective agents for the treatment of neurodegenerative diseases Int Rev Neurobiol 46 2001 379 397
103. J. Lappalainen, E. Krupitsky, M. Remizov, S. Pchelina, A. Taraskina, and E. Zvartau Association between alcoholism and γ-aminobutyric acid α2 receptor subtype in a Russian population Alcohol Clin Exp Res 29 4 2005 493 498
104. K. Laxer, D. Blum, B.W. Abou-Khalil, M.J. Morrell, D.A. Lee, and J.L. Data Assessment of ganaxolone's anticonvulsant activity using a randomized, double-blind, presurgical trial design. Ganaxolone Presurgical Study Group Epilepsia 41 9 2000 1187 1194
105. A receptors on CA1 hippocampal neurons is consistent with subunit changes in a model of alcohol withdrawal and dependence J Pharmacol Exp Ther 310 3 2004 1234 1245
106. T. Lindeburg, S. Folsgard, H. Sillesen, E. Jacobsen, and H. Kehlet Analgesic, respiratory and endocrine responses in normal man to THIP, a GABA-agonist Acta Anaesthesiol Scand 27 1 1983 10 12
107. A channels activated by THIP are modulated by diazepam in CA1 pyramidal neurons in the rat brain hippocampal slice Mol Cell Neurosci 24 1 2003 250 257
108. R.G. Lister, and J.W. Karanian Ro 15-4513 induces seizures in DBA/2 mice undergoing alcohol withdrawal Alcohol 4 1987 409 411
109. A receptors J Med Chem 39 9 1996 1928 1934
110. A receptor β2 gene with schizophrenia Mol Psychiatry 9 6 2004 603 608
111. Aγ2 gene cluster and alcohol dependence in a Scottish population Mol Psychiatry 4 6 1999 539 544
112. K. Low, F. Crestani, R. Keist, D. Benke, I. Brunig, and J.A. Benson Molecular and neuronal substrate for the selective attenuation of anxiety Science 290 5489 2000 131 134
113. A receptor subunit mRNAs in the rat locus coeruleus Brain Res Mol Brain Res 24 1-4 1994 219 226
114. A/ benzodiazepine receptor heterogeneity: neurophysiological implications Neuropharmacology 34 1995 245 254
115. A receptor trafficking, channel activity, and functional plasticity of inhibitory synapses Pharmacol Ther 102 3 2004 195 221
116. S.M. Madsen, T. Lindeburg, S. Folsgard, E. Jacobsen, and H. Sillesen Pharmacokinetics of the γ-aminobutyric acid agonist THIP (Gaboxadol) following intramuscular administration to man, with observations in dog Acta Pharm Toxicol (Copenh) 53 5 1983 353 357
117. A receptor. Mechanism of action and physiological significance Prog Neurobiol 38 4 1992 379 395
118. C.E. Mancuso, M.G. Tanzi, and M. Gabay Paradoxical reactions to benzodiazepines: literature review and treatment options Pharmacotherapy 24 9 2004 1177 1185
119. A receptors Mol Pharmacol 67 3 2005 775 788
120. I. Massat, D. Souery, J. Del-Favero, L. Oruc, M.M. Noethen, and D. Blackwood Excess of allele1 for α3 subunit GABA receptor gene (GABRA3) in bipolar patients: a multicentric association study Mol Psychiatry 7 2 2002 201 207
121. A agonist gaboxadol improves the quality of post-nap sleep Psychopharmacology (Berl) 157 3 2001 299 304
122. S. Mathias, J. Zihl, A. Steiger, and M. Lancel Effect of repeated gaboxadol administration on night sleep and next-day performance in healthy elderly subjects Neuropsychopharmacology 30 4 2005 833 841
123. A receptor subtype selective cognition enhancers Curr Drug Target CNS Neurol Disord 2 4 2003 233 239
124. A receptor subunit cluster and association to autism Am J Med Genet 131B 1 2004 51 59
125. A-receptor containing α5 subunit antagonizes ethanol's neurobehavioral effects in Long-Evans rats Psychopharmacology (Berl) 172 4 2004 455 462
126. A receptor subtypes really occur in the brain? Trends Neurosci 19 4 1996 139 143
127. A receptor α1 subtype Nat Neurosci 3 6 2000 587 592
128. A receptor gene clusters are derived from an ancestral cluster Genomics 26 3 1995 580 586
129. A receptor subunit genes in autistic disorder J Neurogenet 15 3-4 2001 245 259
130. E. Mignot, S. Taheri, and S. Nishino Sleeping with the hypothalamus: emerging therapeutic targets for sleep disorders Nat Neurosci 5 2002 1071 1075
131. R.M. Mihalek, P.K. Banerjee, E.R. Korpi, J.J. Quinlan, L.L. Firestone, and Z.P. Mi Attenuated sensitivity to neuroactive steroids in γ-aminobutyrate type A receptor δ subunit knockout mice Proc Natl Acad Sci U S A 96 22 1999 12905 12910
132. A and glycine receptors Nature 389 6649 1997 385 389
133. F. Minier, and E. Sigel Positioning of the α-subunit isoforms confers a functional signature to γ-aminobutyric acid type A receptors Proc Natl Acad Sci U S A 101 20 2004 7769 7774
134. A receptors responsible for tonic and phasic conductances Neurochem Res 26 8-9 2001 907 913
135. A-receptor subtypes: a new pharmacology Curr Opin Pharmacol 1 1 2001 22 25
136. E.P. Monaghan, L.A. Navalta, L. Shum, D.W. Ashbrook, and D.A. Lee Initial human experience with ganaxolone, a neuroactive steroid with antiepileptic activity Epilepsia 38 9 1997 1026 1031
137. A receptor ε-subunit in cholinergic and aminergic neurones and evidence for co-distribution with the θ-subunit in rat brain Neuroscience 111 3 2002 657 669
138. S.J. Moss, and T.G. Smart Constructing inhibitory synapses Nat Rev Neurosci 2 4 2001 240 250
139. A receptors J Neurosci 19 7 1999 2474 2488
140. A receptors which contain the α5 subunit, in the elevated plus-maze test Prog Neuropsychopharmacol Biol Psychiatry 26 7-8 2002 1389 1392
141. K. Nishikawa, and N.L. Harrison The actions of sevoflurane and desflurane on the γ-aminobutyric acid receptor type A: effects of TM2 mutations in the α and β subunits Anesthesiology 99 3 2003 678 684
142. A receptors: contrasting effects of α1(S270) and β2(N265) point mutations Neuropharmacology 42 3 2002 337 345
143. A receptor β3 subunit genes and alcoholism Psychiatry Res 81 2 1998 133 147
144. Z. Nusser, and I. Mody Selective modulation of tonic and phasic inhibitions in dentate gyrus granule cells J Neurophysiol 87 5 2002 2624 2628
145. A receptors to synaptic and extrasynaptic membranes of cerebellar granule cells J Neurosci 18 5 1998 1693 1703
146. A receptors Biochem Pharmacol 68 8 2004 1675 1684
147. L.S. Overstreet, and G.L. Westbrook Paradoxical reduction of synaptic inhibition by vigabatrin J Neurophysiol 86 2 2001 596 603
148. A receptor α5 subunit gene locus (GABRA5) and bipolar affective disorder Am J Med Genet 81 1 1998 73 80
149. A receptor α1 and α3 subunits genes and alcoholism Alcohol Clin Exp Res 21 3 1997 430 433
150. A. Parsian, and Z.H. Zhang Human chromosomes 11p15 and 4p12 and alcohol dependence: possible association with the GABRB1 gene Am J Med Genet 88 5 1999 533 538
151. A receptor changes in δ subunit-deficient mice: altered expression of α4 and γ2 subunits in the forebrain J Comp Neurol 446 2 2002 179 197
152. A receptors in central synapses J Neurosci 19 2 1999 578 588
153. H.R. Petersen, I. Jensen, and M. Dam THIP: a single-blind controlled trial in patients with epilepsy Acta Neurol Scand 67 2 1983 114 117
154. A. Pierucci-Lagha, J. Covault, R. Feinn, M. Nellissery, C. Hernandez-Avila, and C. Oncken GABRA2 alleles moderate the subjective effects of alcohol, which are attenuated by finasteride Neuropsychopharmacology 30 6 2005 1193 1203
155. A receptors: immunocytochemical distribution of 13 subunits in the adult rat brain Neuroscience 101 4 2000 815 850
156. D.M. Porcello, M.M. Huntsman, R.M. Mihalek, G.E. Homanics, and J.R. Huguenard Intact synaptic GABAergic inhibition and altered neurosteroid modulation of thalamic relay neurons in mice lacking delta subunit J Neurophysiol 89 3 2003 1378 1386
157. A receptor subunit for benzodiazepine pharmacology Nature 338 6216 1989 582 585
158. A receptor: agonist/antagonist efficacy of 4-PIOL Eur J Pharmacol 409 3 2000 233 242
159. M. Radel, R.L. Vallejo, N. Iwata, R. Aragon, J.C. Long, and M. Virkkunen Haplotype-based localization of an alcohol dependence gene to the 5q34 γ-aminobutyric acid type A gene cluster Arch Gen Psychiatry 62 1 2005 47 55
160. S. Rassnick, E. D'Amico, E. Riley, and G.F. Koob GABA antagonist and benzodiazepine partial inverse agonist reduce motivated responding for ethanol Alcohol Clin Exp Res 17 1993 124 130
161. D.S. Reddy, and M.A. Rogawski Enhanced anticonvulsant activity of ganaxolone after neurosteroid withdrawal in a rat model of catamenial epilepsy J Pharmacol Exp Ther 294 3 2000 909 915
162. T. Reich, H.J. Edenberg, A. Goate, J.T. Williams, J.P. Rice, and P. Van Eerdewegh Genome-wide search for genes affecting the risk for alcohol dependence Am J Med Genet 81 3 1998 207 215
163. A receptor isoforms J Neurosci 23 24 2003 8608 8617
164. J.P. Rice, A. Goate, J.T. Williams, L. Bierut, D. Dorr, and W. Wu Initial genome scan of the NIMH genetics initiative bipolar pedigrees: chromosomes 1, 6, 8, 10, and 12 Am J Med Genet 74 3 1997 247 253
165. - co-transporter KCC2 renders GABA hyperpolarizing during neuronal maturation Nature 397 6716 1999 251 255
166. M.A. Rogawski, and D.S. Reddy Neurosteroids and infantile spasms: the deoxycorticosterone hypothesis Int Rev Neurobiol 49 2002 199 219
167. Aα6 receptor subunit gene (GABRA6) is associated with abdominal obesity and cortisol secretion Int J Obes Relat Metab Disord 26 7 2002 938 941
168. A receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates Proc Natl Acad Sci U S A 102 3 2005 915 920
169. A receptor function and dissection of the pharmacology of benzodiazepines and general anesthetics through mouse genetics Annu Rev Pharmacol Toxicol 44 2004 475 498
170. A receptor subtypes Nature 401 6755 1999 796 800
171. A receptor subtypes: dissecting their pharmacological functions Trends Pharmacol Sci 22 4 2001 188 194
172. A receptor diversity in the human genome Gene 227 2 1999 213 222
173. R. Saitz, M.F. Mayo-Smith, M.S. Roberts, H.A. Redmond, D.R. Bernard, and D.R. Calkins Individualized treatment for alcohol withdrawal. A randomized double-blind controlled trial JAMA 272 7 1994 519 523
174. A receptor subunits: role of the δ subunit J Neurosci 14 11 Pt 2 1994 7077 7086
175. A receptor shows a ligand-gated receptor super-family Nature 328 6127 1987 221 227
176. M.A. Schuckit, C. Mazzanti, T.L. Smith, U. Ahmed, M. Radel, and N. Iwata Selective genotyping for the role of 5-HT2A, 5-HT2C, and GABA α6 receptors and the serotonin transporter in the level of response to alcohol: a pilot study Biol Psychiatry 45 5 1999 647 651
177. M. Schumacher, S. Weill-Engerer, P. Liere, F. Robert, R.J. Franklin, and L.M. Garcia-Segura Steroid hormones and neurosteroids in normal and pathological aging of the nervous system Prog Neurobiol 71 1 2003 3 29
178. R.D. Schwartz-Bloom, K.A. Miller, D.A. Evenson, B.J. Crain, and J.V. Nadler Benzodiazepines protect hippocampal neurons from degeneration after transient cerebral ischemia: an ultrastructural study Neuroscience 98 3 2000 471 484
179. J.W. Sear, and C. Prys-Roberts Alphadione and minaxolone pharmacokinetics Ann Anesthesiol Fr 22 2 1981 142 148
180. E.M. Sellers, C.A. Naranjo, M. Harrison, P. Devenyi, C. Roach, and K. Sykora Diazepam loading: simplified treatment of alcohol withdrawal Clin Pharmacol Ther 34 1983 822 826
181. A α6 receptor variants are associated with neuroticism Biol Psychiatry 55 3 2004 244 249
182. A receptors in rat hypothalamic neurons expressing the ε-subunit J Neurosci 25 1 2005 88 95
183. Y. Shao, M.L. Cuccaro, E.R. Hauser, K.L. Raiford, M.M. Menold, and C.M. Wolpert Fine mapping of autistic disorder to chromosome 15q11-q13 by use of phenotypic subtypes Am J Hum Genet 72 3 2003 539 548
184. K.L. Shelton, and K.A. Grant Effects of naltrexone and Ro 15-4513 on a multiple schedule of ethanol and Tang self-administration Alcohol Clin Exp Res 25 11 2001 1576 1585
185. A receptor subtypes Pharmacol Rev 47 2 1995 181 234
186. A receptors Trends Pharmacol Sci 18 11 1997 425 429
187. A receptor ε and θ subunits display unusual structural variation between species and are enriched in the rat locus ceruleus J Neurosci 20 10 2000 3588 3595
188. A receptor function by niflumic acid, a nonsteroidal anti-inflammatory drug Mol Pharmacol 64 3 2003 753 763
189. Aergic inhibition in a mouse model Eur J Neurosci 20 8 2004 2168 2178
190. D. Sinnett, J. Wagstaff, K. Glatt, E. Woolf, E.J. Kirkness, and M. Lalande High-resolution mapping of the γ-aminobutyric acid receptor subunit β3 and α5 gene cluster on chromosome 15q11-q13, and localization of breakpoints in two Angelman syndrome patients Am J Hum Genet 52 6 1993 1216 1229
191. A receptor gene regulation in the brain and anxiety behavior Steroids 67 6 2002 519 528
192. A receptor α4 subunit in association with increased anxiety J Neurosci 18 14 1998 5275 5284
193. K. Soares, J. Rathbone, and J. Deeks γ-Aminobutyric acid agonists for neuroleptic-induced tardive dyskinesia Cochrane Database Syst Rev 4 2004 (CD000203)
194. A receptors and alcohol dependence and the effects of genetic imprinting Am J Med Genet, Part B Neuropsychiatr Genet 117 1 2003 39 45
195. J.M. Sonner, J.F. Antognini, R.C. Dutton, P. Flood, A.T. Gray, and R.A. Harris Inhaled anesthetics and immobility: mechanisms, mysteries, and minimum alveolar anesthetic concentration Anesth Analg 97 3 2003 718 740
196. J.M. Sonner, M. Cascio, Y. Xing, M.S. Fanselow, J. Kralic, and A.L. Morrow α1 subunit-containing g-aminobutyrate type A receptors in forebrain contribute to the effect of inhaled anesthetics on conditioned fear Mol Pharmacol 68 1 2005 61 68
197. A receptor δ subunit J Neurophysiol 90 2 2003 903 910
198. A receptors: building the bridge between subunit mRNAs, their promoters, and cognate transcription factors Pharmacol Ther 101 3 2004 259 281
199. A receptors Proc Natl Acad Sci U S A 100 24 2003 14439 14444
200. A α5 receptor inverse agonists as cognition enhancers J Med Chem 47 9 2004 2176 2179
201. A receptors Mol Pharmacol 58 6 2000 1434 1440
202. Aα5 benzodiazepine binding site J Med Chem 47 14 2004 3642 3657
203. A. Strohle, E. Romeo, F. di Michele, A. Pasini, B. Hermann, and G. Gajewsky Induced panic attacks shift γ-aminobutyric acid type A receptor modulatory neuroactive steroid composition in patients with panic disorder: preliminary results Arch Gen Psychiatry 60 2 2003 161 168
204. R.D. Strous, R. Maayan, R. Lapidus, R. Stryjer, M. Lustig, and M. Kotler Dehydroepiandrosterone augmentation in the management of negative, depressive, and anxiety symptoms in schizophrenia Arch Gen Psychiatry 60 2 2003 133 141
205. A receptors are a target for alcohol Nat Neurosci 5 8 2002 721 722
206. P.D. Suzdak, J.R. Glowa, J.N. Crawley, R.D. Schwartz, P. Skolnick, and S.M. Paul A selective imidazobenzodiazepine antagonist of ethanol in the rat Science 234 1986 1243 1247
207. J. Tang, J. Qi, P.F. White, B. Wang, and R.H. Wender Eltanolone as an alternative to propofol for ambulatory anesthesia Anesth Analg 85 4 1997 801 807
208. A receptors are the molecular substrates mediating precipitation of narcosis but not of sedation by the combined use of diazepam and alcohol in vivo Eur J Neurosci 18 9 2003 2599 2604
209. G.K. Thaker, C.A. Tamminga, L.D. Alphs, J. Lafferman, T.N. Ferraro, and T.A. Hare Brain γ-aminobutyric acid abnormality in tardive dyskinesia. Reduction in cerebrospinal fluid GABA levels and therapeutic response to GABA agonist treatment Arch Gen Psychiatry 44 6 1987 522 529
210. A receptors Mol Pharmacol 61 4 2002 861 869
211. A receptors Br J Pharmacol 142 1 2004 97 106
212. M. Uhart, M.E. McCaul, L.M. Oswald, L. Choi, and G.S. Wand GABRA6 gene polymorphism and an attenuated stress response Mol Psychiatry 9 11 2004 998 1006
213. A receptor β2-α6-α1-γ2 subunit gene cluster Mol Cell Neurosci 16 1 2000 34 41
214. N. Valentin, and O.K. Bank-Mikkelsen Respiratory effect of THIP, a GABA-agonistic analgesic, during halothane anaesthesia Acta Anaesthesiol Scand 27 5 1983 366 368
215. A receptors J Pharmacol Exp Ther 295 1 2000 337 345
216. A receptor in mice make inhibition exciting Pharmacol Ther 103 2 2004 109 120
217. A receptor agonist gaboxadol: lack of ethanol potentiation and benzodiazepine cross-tolerance Eur J Pharmacol 482 1-3 2003 215 222
218. D.A. Wagner, and C. Czajkowski Structure and dynamics of the GABA binding pocket: a narrowing cleft that constricts during activation J Neurosci 21 1 2001 67 74
219. M. Wallner, H.J. Hanchar, and R.W. Olsen Ethanol enhances α4β3δ and α6β3δ γ-aminobutyric acid type A receptors at low concentrations known to affect humans Proc Natl Acad Sci U S A 100 25 2003 15218 15223
220. K. Wegelius, A. Honkanen, and E.R. Korpi Benzodiazepine receptor ligands modulate ethanol drinking in alcohol-preferring rats Eur J Pharmacol 263 1994 141 147
221. A receptors and their activation by GABA spillover in the mouse dentate gyrus J Neurosci 23 33 2003 10650 10661
222. H.A. Westra, and S.H. Stewart Cognitive behavioural therapy and pharmacotherapy: complementary or contradictory approaches to the treatment of anxiety? Clin Psychol Rev 18 3 1998 307 340
223. A receptors is essential for benzodiazepine agonist binding J Biol Chem 267 3 1992 1426 1429
224. A receptor channels: from subunits to functional entities Curr Opin Neurobiol 2 1992 263 269
225. A receptor subunit mRNAs in the rat brain: I. Telencephalon, diencephalon, mesencephalon J Neurosci 12 1992 1040 1062
226. A receptor α6 subunit in hippocampal pyramidal neurons produces extrasynaptic receptors and an increased tonic inhibition Neuropharmacology 43 4 2002 530 549
227. O.M. Wolkowitz, J.H. Kramer, V.I. Reus, M.M. Costa, K. Yaffe, and P. Walton DHEA treatment of Alzheimer's disease: a randomized, double-blind, placebo-controlled study Neurology 60 7 2003 1071 1076
228. Y. Wu, W. Wang, and G.B. Richerson Vigabatrin induces tonic inhibition via GABA transporter reversal without increasing vesicular GABA release J Neurophysiol 89 4 2003 2021 2034
229. K. Yamada, A. Watanabe, Y. Iwayama-Shigeno, and T. Yoshikawa Evidence of association between γ-aminobutyric acid type A receptor genes located on 5q34 and female patients with mood disorders Neurosci Lett 349 1 2003 9 12
230. P. Zwanzger, D. Eser, F. Padberg, T.C. Baghai, C. Schule, and R. Rupprecht Neuroactive steroids are not affected by panic induction with 50 microg cholecystokinin-tetrapeptide (CCK-4) in healthy volunteers J Psychiatr Res 38 2 2004 215 217