Cited by 745Neuroscience and Neuropharmacology ResearchNicotinic Acetylcholine Receptors StudyEpilepsy research and treatment

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Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes

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Rudolph, Uwe, Knoflach, Frédéric·2011·Nature Reviews Drug Discovery

DOI 10.1038/nrd3502PMC PMC3375401

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Abstract

GABAA (γ-aminobutyric acid, type A) receptors are a family of ligand-gated ion channels that are essential for the regulation of central nervous system function. Benzodiazepines — which non-selectively target GABAA receptors containing the α1, α2, α3 or α5 subunits — have been in clinical use for decades and are still among the most widely prescribed drugs for the treatment of insomnia and anxiety disorders. However, their use is limited by side effects and the risk of drug dependence. In the past decade, the identification of separable key functions of GABAA receptor subtypes suggests that receptor subtype-selective compounds could overcome the limitations of classical benzodiazepines; furthermore, they might be valuable for novel indications such as chronic pain, depression, schizophrenia, cognitive enhancement and stroke.

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International Union of Pharmacology: Approaches to the Nomenclature of Voltage-Gated Ion Channels
Catterall, W. A., Chandy, K. G., Clapham, D. E., Gutman, G. A., Hofmann, F., Harmar, A. J., Abernethy, D. R., & Spedding, M. (2003) · Pharmacological Reviews · doi:10.1124/pr.55.4.5 · Cited by 7,126
Cortical inhibitory neurons and schizophrenia
Lewis, D. A., Hashimoto, T., & Volk, D. W. (2005) · Nature Reviews Neuroscience · doi:10.1038/nrn1648 · Cited by 2,297 · cited 1×
“In post-mortem brain from patients with schizophrenia, there is an upregulation of the α2 subunit in the axon initial segments of these pyramidal neuron”
Background
Benzodiazepine Receptor: Demonstration in the Central Nervous System
Möhler, H., & Okada, T. (1977) · Science · doi:10.1126/science.918669 · Cited by 1,709 · cited 1×
“Benzodiazepines have been shown to bind to specific sites in the central nervous syste”
Background
New approaches to antidepressant drug discovery: beyond monoamines
Berton, O., & Nestler, E. J. (2006) · Nature Reviews Neuroscience · doi:10.1038/nrn1846 · Cited by 1,589 · cited 1×
“Although there is tremendous interest in developing antidepressant agents that utilize different mechanisms of action, the development of such agents has not yet been successfu”
Background
Benzodiazepine receptors in rat brain
Squires, R. F., & Bræstrup, C. (1977) · Nature · doi:10.1038/266732a0 · Cited by 1,453
GABAA receptors: immunocytochemical distribution of 13 subunits in the adult rat brain
Pirker, S., Schwarzer, C., Wieselthaler, A., Sieghart, W., & Sperk, G. (2000) · Neuroscience · doi:10.1016/s0306-4522(00)00442-5 · Cited by 1,344
GABA A ‐receptor heterogeneity in the adult rat brain: Differential regional and cellular distribution of seven major subunits
Fritschy, J., & Mohler, H. (1995) · Journal of Comparative Neurology · doi:10.1002/cne.903590111 · Cited by 1,244
Benzodiazepine actions mediated by specific γ-aminobutyric acidA receptor subtypes
Rudolph, U., Crestani, F., Benke, D., Brünig, I., Benson, J. A., Fritschy, J.-M., Martin, J. R., Bluethmann, H., & Möhler, H. (1999) · Nature · doi:10.1038/44579 · Cited by 1,172
Self-citation
International Union of Pharmacology. LXX. Subtypes of γ-Aminobutyric AcidA Receptors: Classification on the Basis of Subunit Composition, Pharmacology, and Function. Update
Olsen, R. W., & Sieghart, W. (2008) · Pharmacological Reviews · doi:10.1124/pr.108.00505 · Cited by 1,064
Regulation of firing of dopaminergic neurons and control of goal-directed behaviors
Grace, A. A., Floresco, S. B., Goto, Y., & Lodge, D. J. (2007) · Trends in Neurosciences · doi:10.1016/j.tins.2007.03.003 · Cited by 1,034 · cited 1×
“, activates tonic firing of dopaminergic neurons in the midbrain; this circuit involves glutamatergic neurons in the hippocampus, GABAergic neurons in the nucleus accumbens and GABAergic neurons in the ventral pallidu”
Background
Circuit-based framework for understanding neurotransmitter and risk gene interactions in schizophrenia
Lisman, J. E., Coyle, J. T., Green, R. W., Javitt, D. C., Benes, F. M., Heckers, S., & Grace, A. A. (2008) · Trends in Neurosciences · doi:10.1016/j.tins.2008.02.005 · Cited by 1,010 · cited 1×
“, activates tonic firing of dopaminergic neurons in the midbrain; this circuit involves glutamatergic neurons in the hippocampus, GABAergic neurons in the nucleus accumbens and GABAergic neurons in the ventral pallidu”
Background
GABAA receptors: Subtypes provide diversity of function and pharmacology
Olsen, R. W., & Sieghart, W. (2008) · Neuropharmacology · doi:10.1016/j.neuropharm.2008.07.045 · Cited by 986
Molecular and neuronal substrate for the selective attenuation of anxiety
Löw, K., Crestani, F., Keist, R., Benke, D., Brünig, I., Benson, J. A., Fritschy, J.-M., Rülicke, T., Bluethmann, H., Möhler, H., et al. (2000) · Science · doi:10.1126/science.290.5489.131 · Cited by 946 · cited 1×
“Histidine-to-arginine point mutations at a conserved residue in the α1, α2, α3 or α5 subunit abolish binding of diazepam, whereas the action of the physiological neurotransmitter GABA is preserve”
BackgroundSelf-citation
Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABAA receptor α1 subtype
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., et al. (2000) · Nature Neuroscience · doi:10.1038/75761 · Cited by 944
The GABAergic deficit hypothesis of major depressive disorder
Luscher, B., Shen, Q., & Sahir, N. (2011) · Molecular Psychiatry · doi:10.1038/mp.2010.120 · Cited by 934
Reducing excessive GABA-mediated tonic inhibition promotes functional recovery after stroke
Clarkson, A. N., Huang, B. S., MacIsaac, S. E., Mody, I., & Carmichael, S. T. (2010) · Nature · doi:10.1038/nature09511 · Cited by 869
Molecular and neuronal substrates for general anaesthetics
Rudolph, U., & Antkowiak, B. (2004) · Nature reviews. Neuroscience · doi:10.1038/nrn1496 · Cited by 771
Self-citation
A new benzodiazepine pharmacology
Möhler, H., Fritschy, J. M., & Rudolph, U. (2002) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.300.1.2 · Cited by 716
Self-citation
Variations in GABRA2, Encoding the α2 Subunit of the GABAA Receptor, Are Associated with Alcohol Dependence and with Brain Oscillations
Edenberg, H. J., Dick, D. M., Xuei, X., Tian, H., Almasy, L., Bauer, L. O., Crowe, R. R., Goate, A., Hesselbrock, V., Jones, K., et al. (2004) · The American Journal of Human Genetics · doi:10.1086/383283 · Cited by 655
The ‘ABC’ of GABA receptors
Bormann, J. (2000) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(99)01413-3 · Cited by 629
Enhanced Learning and Memory and Altered GABAergic Synaptic Transmission in Mice Lacking the α5 Subunit of the GABA A Receptor
Collinson, N., Kuenzi, F. M., Jarolimek, W., Maubach, K. A., Cothliff, R., Sur, C., Smith, A., Otu, F. M., Howell, O., Atack, J. R., et al. (2002) · The Journal of Neuroscience · doi:10.1523/jneurosci.22-13-05572.2002 · Cited by 628
SEVERE ANXIETY INDUCED BY FG 7142, A β-CARBOLINE LIGAND FOR BENZODIAZEPINE RECEPTORS
Dorow, R., Horowski, R., Paschelke, G., Amin, M., & Bræstrup, C. (1983) · The Lancet · doi:10.1016/s0140-6736(83)90076-4 · Cited by 580 · cited 1×
“Importantly, none of these α5-containing receptor selective drugs displays the convulsant and anxiogenic activities of the non-selective GABA A receptor inverse agonists FG-7142, DMCM (methyl-6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate) or β-CCM (methyl β-carboline-3-carboxylate), which are not used therapeuticall”
Background
General anesthetic actions in vivo strongly attenuated by a point mutation in the GABA A receptor β3 subunit
Jurd, R., Arrasa, M., Lambert, S., Drexler, B., Siegwart, R., Crestani, F., Zaugg, M., Vogt, K. E., Ledermann, B., Antkowiak, B., et al. (2003) · The FASEB Journal · doi:10.1096/fj.02-0611fje · Cited by 558
Self-citation
Decreased GABAA-receptor clustering results in enhanced anxiety and a bias for threat cues
Crestani, F., Lorez, M., Baer, K., Essrich, C., Benke, D., Laurent, J. P., Belzung, C., Fritschy, J.-M., Lüscher, B., & Mohler, H. (1999) · Nature Neuroscience · doi:10.1038/12207 · Cited by 550 · cited 1×
“In addition, heterozygous γ2 ( Gabrg2 ) knockout mice display an anxiety-like phenotype in tests of unconditioned anxiet”
Background
Interaction of Convulsive Ligands with Benzodiazepine Receptors
Bræstrup, C., Schmiechen, R., Neef, G., et al. (1982) · Science · doi:10.1126/science.6281892 · Cited by 547 · cited 1×
“Benzodiazepines have been shown to bind to specific sites in the central nervous syste”
Background
Trace fear conditioning involves hippocampal α 5 GABA A receptors
Crestani, F., Keist, R., Fritschy, J.-M., Benke, D., Vogt, K., Prut, L., Blüthmann, H., Möhler, H., & Rudolph, U. (2002) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.142288699 · Cited by 528 · cited 1×
“Histidine-to-arginine point mutations at a conserved residue in the α1, α2, α3 or α5 subunit abolish binding of diazepam, whereas the action of the physiological neurotransmitter GABA is preserve”
BackgroundSelf-citation
γ‐Aminobutyric AcidA Receptor α5‐Subunit Creates Novel Type II Benzodiazepine Receptor Pharmacology
Pritchett, D. B., & Seeburg, P. H. (1990) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.1990.tb01237.x · Cited by 503 · cited 1×
“Zolpidem, which is an imidazopyridine, has a high affinity for α1-containing GABA A receptors, a 20-fold lower affinity for α2-containing GABA A receptors and α3-containing GABA A receptors, and no affinity for α5-containing GABA A receptor”
Background
GABAA receptor subtypes: dissecting their pharmacological functions
Rudolph, U., Crestani, F., & Möhler, H. (2001) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(00)01646-1 · Cited by 472
Self-citation
Specific GABA A Circuits for Visual Cortical Plasticity
Fagiolini, M., Fritschy, J.-M., Löw, K., Möhler, H., Rudolph, U., & Hensch, T. K. (2004) · Science · doi:10.1126/science.1091032 · Cited by 471
Self-citation
Stuck in a rut: rethinking depression and its treatment
Holtzheimer, P. E., & Mayberg, H. S. (2010) · Trends in Neurosciences · doi:10.1016/j.tins.2010.10.004 · Cited by 456 · cited 1×
“Currently available antidepressant medications act on the serotonergic and/or noradrenergic systems, but the response rate (defined as >50% decrease in depression severity from baseline) is only approximately 60”
Background
Reversal of pathological pain through specific spinal GABAA receptor subtypes
Knabl, J., Witschi, R., Hösl, K., Reinold, H., Zeilhofer, U. B., Ahmadi, S., Brockhaus, J., Sergejeva, M., Hess, A., Brune, K., et al. (2008) · Nature · doi:10.1038/nature06493 · Cited by 438 · cited 1×
“When diazepam is administered intrathecally in α2(H101R) and α3(H126R) mice, its antihyperalgesic action is significantly reduced in models of inflammatory pain and of neuropathic pain, demonstrating that spinal α2- and α3-containing GABA A receptors are mediating the antihyperalgesic actions of intrathecal diazepa”
BackgroundSelf-citation
Neural bases for addictive properties of benzodiazepines
Tan, K. R., Brown, M., Labouèbe, G., Yvon, C., Creton, C., Fritschy, J.-M., Rudolph, U., & Lüscher, C. (2010) · Nature · doi:10.1038/nature08758 · Cited by 397 · cited 1×
“, and their addictive properties have been linked to α1-containing GABA A receptor”
BackgroundSelf-citation
Hooked on benzodiazepines: GABAA receptor subtypes and addiction
Tan, K. R., Rudolph, U., & Lüscher, C. (2011) · Trends in Neurosciences · doi:10.1016/j.tins.2011.01.004 · Cited by 363
Self-citation
Co-localization of GABAA receptors and benzodiazepine receptors in the brain shown by monoclonal antibodies
Schoch, P., Richards, J. G., Häring, P., et al. (1985) · Nature · doi:10.1038/314168a0 · Cited by 316
GABA A receptor α4 subunits mediate extrasynaptic inhibition in thalamus and dentate gyrus and the action of gaboxadol
Chandra, D., Jia, F., Liang, J., Peng, Z., Suryanarayanan, A., Werner, D. F., Spigelman, I., Houser, C. R., Olsen, R. W., Harrison, N. L., et al. (2006) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0604304103 · Cited by 315 · cited 1×
“In mice, it induces sedation largely via α4-containing GABA A receptor”
Background
Cognitive and sedative effects of benzodiazepine use
Buffett-Jerrott, S., & Stewart, S. (2002) · Current Pharmaceutical Design · doi:10.2174/1381612023396654 · Cited by 312 · cited 1×
“Several studies in animals and humans have suggested that classical benzodiazepines can impair learning and memor”
Background
Mechanism of action of the hypnotic zolpidem in vivo
Crestani, F., Martin, J. R., Möhler, H., & Rudolph, U. (2000) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0703717 · Cited by 307 · cited 1×
“Indeed, in α1(H101R) mice the motor sedative action of zolpidem was abolished, which demonstrates that the sedative action of zolpidem is mediated by α1-containing GABA A receptor”
BackgroundSelf-citation
Subunit-Selective Modulation of GABA Type A Receptor Neurotransmission and Cognition in Schizophrenia
Lewis, D. A., Cho, R. Y., Carter, C. S., Eklund, K. E., Förster, S., Kelly, M. A., & Montrose, D. M. (2008) · American Journal of Psychiatry · doi:10.1176/appi.ajp.2008.08030395 · Cited by 291 · cited 1×
“Some cognitive functions were improved with TPA023 treatmen”
Background
The Role of GABA in the Mediation and Perception of Pain
Enna, S. J., & McCarson, K. E. (2006) · Advances in pharmacology · doi:10.1016/s1054-3589(06)54001-3 · Cited by 288 · cited 1×
“Benzodiazepines are generally not considered to be analgesic agents as they lack clear efficacy when given systemically in human”
Background
Allelic and haplotypic association of GABRA2 with alcohol dependence
Covault, J., Gelernter, J., Hesselbrock, V., Nellissery, M., & Kranzler, H. R. (2004) · American Journal of Medical Genetics Part B Neuropsychiatric Genetics · doi:10.1002/ajmg.b.30091 · Cited by 273
Mutations in GABAAreceptor subunits associated with genetic epilepsies
Macdonald, R. L., Kang, J., & Gallagher, M. J. (2010) · The Journal of Physiology · doi:10.1113/jphysiol.2010.186999 · Cited by 272
GABAergic dysfunction in schizophrenia: new treatment strategies on the horizon
Guidotti, A., Auta, J., Davis, J. M., Dong, E., Grayson, D. R., Veldic, M., Zhang, X., & Costa, E. (2005) · Psychopharmacology · doi:10.1007/s00213-005-2212-8 · Cited by 262
DOG BITES IN CHILDREN
Lillington, A. W., & Ross, M. (1976) · The Lancet · doi:10.1016/s0140-6736(76)92316-3 · Cited by 261
The Mechanistic Classification of Addictive Drugs
Lüscher, C., & Ungless, M. A. (2006) · PLoS Medicine · doi:10.1371/journal.pmed.0030437 · Cited by 255 · cited 1×
“All addictive drugs increase dopamine levels in the mesolimbic dopamine syste”
Background
Evidence for a Significant Role of α3-Containing GABAAReceptors in Mediating the Anxiolytic Effects of Benzodiazepines
Dias, R., Sheppard, W. F. A., Fradley, R. L., Garrett, E. M., Stanley, J. L., Tye, S. J., Goodacre, S., Lincoln, R. J., Cook, S. M., Conley, R., et al. (2005) · The Journal of Neuroscience · doi:10.1523/jneurosci.1166-05.2005 · Cited by 247 · cited 1×
“2a ), which has been described to have a selective efficacy at recombinant α3-containing GABA A receptors in vitro , is anxiolytic in the elevated plus maze test in rat”
Background
Molecular Targets for the Myorelaxant Action of Diazepam
Crestani, F., Löw, K., Keist, R., Mandelli, M.-J., Möhler, H., & Rudolph, U. (2001) · Molecular Pharmacology · doi:10.1124/mol.59.3.442 · Cited by 239 · cited 1×
“In α2(H101R) mice, the anxiolytic-like action of diazepam was absent and its myorelaxant action (which is observed at higher doses than the anxiolytic-like action) was reduced, whereas the sedative action was presen”
BackgroundSelf-citation
Diazepam-induced changes in sleep: Role of the α1 GABA A receptor subtype
Tobler, I., Kopp, C., Deboer, T., & Rudolph, U. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.111055398 · Cited by 230
Self-citation
Different GABA A receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates
Rowlett, J. K., Platt, D. M., Lelas, S., Atack, J. R., & Dawson, G. R. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0405621102 · Cited by 212
GABAB receptors: synaptic functions and mechanisms of diversity
Ulrich, D., & Bettler, B. (2007) · Current Opinion in Neurobiology · doi:10.1016/j.conb.2007.04.001 · Cited by 205
GABAergic Control of Adult Hippocampal Neurogenesis in Relation to Behavior Indicative of Trait Anxiety and Depression States
Earnheart, J. C., Schweizer, C., Crestani, F., Iwasato, T., Itohara, S., Mohler, H., & Lüscher, B. (2007) · The Journal of Neuroscience · doi:10.1523/jneurosci.3609-06.2007 · Cited by 203 · cited 1×
“and a depressive-like phenotype in conflict- and despair-based test”
Background
A schizophrenia-related sensorimotor deficit links α3-containing GABA A receptors to a dopamine hyperfunction
Yee, B. K., Keist, R., von Boehmer, L., Studer, R., Benke, D., Hagenbuch, N., Dong, Y., Malenka, R. C., Fritschy, J.-M., Bluethmann, H., et al. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0508752102 · Cited by 201 · cited 1×
“α3 knockout mice and α5(H105R) partial knockout mice with a reduced expression of the α5 subunit display deficits in sensorimotor gating, as determined by prepulse inhibition of acoustic startle, supporting a potential involvement of α3- and α5-containing GABA A receptors in the pathophysiology of schizophreni”
BackgroundSelf-citation
Construct Validity of the Animal Latent Inhibition Model of Selective Attention Deficits in Schizophrenia
Lubow, R. E. (2005) · Schizophrenia Bulletin · doi:10.1093/schbul/sbi005 · Cited by 192 · cited 1×
“Deficits in this form of learning have also been described in schizophreni”
Background
Association of GABRA2 with drug dependence in the collaborative study of the genetics of alcoholism sample
Agrawal, A., Edenberg, H. J., Foroud, T., Bierut, L. J., Dunne, G., Hinrichs, A. L., Nurnberger, J. I., Crowe, R., Kuperman, S., Schuckit, M. A., et al. (2006) · Behavior Genetics · doi:10.1007/s10519-006-9069-4 · Cited by 189
TPA023 [7-(1,1-Dimethylethyl)-6-(2-ethyl-2 H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an Agonist Selective for α2- and α3-Containing GABAA Receptors, Is a Nonsedating Anxiolytic in Rodents and Primates
Atack, J. R., Wafford, K. A., Tye, S. J., Cook, S. M., Sohal, B., Pike, A., Sur, C., Melillo, D., Bristow, L., Bromidge, F., et al. (2006) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.105.089920 · Cited by 188
L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for α5-containing GABAA receptors
Atack, J. R., Bayley, P. J., Seabrook, G. R., Wafford, K. A., McKernan, R. M., & Dawson, G. R. (2006) · Neuropharmacology · doi:10.1016/j.neuropharm.2006.04.018 · Cited by 174 · cited 1×
“L-655708 also enhanced performance in the Morris water maze during acquisition and in a probe tria”
Background
A randomized clinical trial of MK-0777 for the treatment of cognitive impairments in people with schizophrenia
Buchanan, R. W., Keefe, R. S. E., Lieberman, J. A., Barch, D. M., Csernansky, J. G., Goff, D. C., Gold, J. M., Green, M. F., Jarskog, L. F., Javitt, D. C., et al. (2011) · Biological Psychiatry · doi:10.1016/j.biopsych.2010.09.052 · Cited by 172 · cited 1×
“However, a follow-up study including 60 patients, with some of the same tests, did not confirm these result”
Result
Specific Subtypes of GABA A Receptors Mediate Phasic and Tonic Forms of Inhibition in Hippocampal Pyramidal Neurons
Prenosil, G., Gasser, E. M. S., Rudolph, U., Keist, R., Fritschy, J., & Vogt, K. E. (2006) · Journal of Neurophysiology · doi:10.1152/jn.01199.2005 · Cited by 169 · cited 1×
“(and are therefore extrasynaptic (see also Box 1 )) and mediate both tonic and slow phasic inhibitio”
BackgroundSelf-citation
A Novel α5GABAAR-Positive Allosteric Modulator Reverses Hyperactivation of the Dopamine System in the MAM Model of Schizophrenia
Gill, K. M., Lodge, D. J., Cook, J. M., Aras, S., & Grace, A. A. (2011) · Neuropsychopharmacology · doi:10.1038/npp.2011.76 · Cited by 163
RO4938581, a novel cognitive enhancer acting at GABAA α5 subunit-containing receptors
Ballard, T. M., Knoflach, F., Prinssen, E. P. M., Borroni, E., Vivian, J. A., Basile, J., Gasser, R., Moreau, J., Wettstein, J. G., Buettelmann, B., et al. (2008) · Psychopharmacology · doi:10.1007/s00213-008-1357-7 · Cited by 156 · cited 1×
“Prototypes for drugs with binding selectivity are RO4938581 (Ref”
BackgroundSelf-citation
Requirement of α5-GABAAReceptors for the Development of Tolerance to the Sedative Action of Diazepam in Mice
van Rijnsoever, C., Täuber, M., Choulli, M. K., Keist, R., Rudolph, U., Mohler, H., Fritschy, J. M., & Crestani, F. (2004) · The Journal of Neuroscience · doi:10.1523/jneurosci.1067-04.2004 · Cited by 144 · cited 1×
“Moreover, the development of tolerance to the sedative action of benzodiazepines has been linked to α5-containing GABA A receptor”
BackgroundSelf-citation
Benzodiazepines as antidepressants: Does GABA play a role in depression?
Petty, F., Trivedi, M. H., Fulton, M., & Rush, A. J. (1995) · Biological Psychiatry · doi:10.1016/0006-3223(95)00049-7 · Cited by 143 · cited 1×
“Moreover, clinical studies have revealed that the benzodiazepines alprazolam and adinazolam elicit antidepressant responses that are similar to those elicited by widely prescribed antidepressants in patients with major depressive disorde”
Background
Benzodiazepines on trial: a research strategy for their rehabilitation
Costa, E., & Guidetti, A. (1996) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(96)10015-8 · Cited by 140
γ-Aminobutyric Acid-Type A Receptor Deficits Cause Hypothalamic-Pituitary-Adrenal Axis Hyperactivity and Antidepressant Drug Sensitivity Reminiscent of Melancholic Forms of Depression
Shen, Q., Lal, R., Luellen, B. A., Earnheart, J. C., Andrews, A. M., & Luscher, B. (2010) · Biological Psychiatry · doi:10.1016/j.biopsych.2010.04.024 · Cited by 139 · cited 1×
“These mice also have elevated baseline cortico-sterone concentration”
Background
Strong genetic evidence for a selective influence of GABAA receptors on a component of the bipolar disorder phenotype
Craddock, N. J., Jones, L. A., Jones, I. R., Kirov, G., Green, E., Grozeva, D., Moskvina, V., Nikolov, I., Hamshere, M. L., Vukcevic, D., et al. (2008) · Molecular Psychiatry · doi:10.1038/mp.2008.66 · Cited by 134
GABAA receptors containing the α5 subunit mediate the trace effect in aversive and appetitive conditioning and extinction of conditioned fear
Yee, B. K., Hauser, J., Dolgov, V. V., Keist, R., Möhler, H., Rudolph, U., & Feldon, J. (2004) · European Journal of Neuroscience · doi:10.1111/j.1460-9568.2004.03642.x · Cited by 134
Self-citation
Benzodiazepine Prescribing to the Swiss Adult Population: Results from a National Survey of Community Pharmacies
Petitjean, S., Ladewig, D., Meier, C. R., Amrein, R., & Wiesbeck, G. A. (2007) · International Clinical Psychopharmacology · doi:10.1097/yic.0b013e328105e0f2 · Cited by 132
Genetic investigation of chromosome 5q GABAA receptor subunit genes in schizophrenia
Petryshen, T. L., Middleton, F. A., Tahl, A. R., Rockwell, G. N., Purcell, S., Aldinger, K. A., Kirby, A. W., Morley, C. P., McGann, L., Gentile, K. L., et al. (2005) · Molecular Psychiatry · doi:10.1038/sj.mp.4001739 · Cited by 132
Effects of benzodiazepine microinjection into the amygdala or periaqueductal gray on the expression of conditioned fear and hypoalgesia in rats.
Harris, J. A., & Westbrook, R. F. (1995) · Behavioral Neuroscience · doi:10.1037//0735-7044.109.2.295 · Cited by 126 · cited 1×
“Central GABA A receptors, such as those in the periaqueductal grey (PAG), an area known to be involved in the regulation of descending antinociceptive tracts, are pro-nociceptive at supraspinal site”
Background
Selective anxiolysis produced by ocinaplon, a GABA A receptor modulator
LIPPA, A. S., Czobor, P., Stark, J., Beer, B., Kostakis, E., Gravielle, M. C., Bandyopadhyay, S., Russek, S. J., Gibbs, T. T., Farb, D. H., et al. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0502579102 · Cited by 125
Positioning of the α-subunit isoforms confers a functional signature to γ-aminobutyric acid type A receptors
Minier, F., & Sigel, E. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0400220101 · Cited by 116
GABAergic analgesia: new insights from mutant mice and subtype-selective agonists
Zeilhofer, H. U., Möhler, H., & Lio, A. D. (2009) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2009.05.007 · Cited by 116
The Missing P in Psychiatric Training
Elman, I., Zubieta, J.-K., & Borsook, D. (2011) · Archives of General Psychiatry · doi:10.1001/archgenpsychiatry.2010.174 · Cited by 115
Preclinical and clinical pharmacology of the GABAA receptor α5 subtype-selective inverse agonist α5IA
Atack, J. R. (2009) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2009.09.001 · Cited by 115
The rise of a new GABA pharmacology
Möhler, H. (2010) · Neuropharmacology · doi:10.1016/j.neuropharm.2010.10.020 · Cited by 111 · cited 1×
“In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1, 2,4-triazol-5-ylme thoxy)-pyrazolo[1,5-d]-[1,2,4] triazine (MRK-016), a GABAA receptor α5 subtypeselective inverse agonist.”
Background
Long-lasting Modulation of Glutamatergic Transmission in VTA Dopamine Neurons after a Single Dose of Benzodiazepine Agonists
Panhelainen, A. E., Möykkynen, T. P., & Korpi, E. R. (2008) · Neuropsychopharmacology · doi:10.1038/npp.2008.89 · Cited by 109
Hippocampal α5 subunit-containing GABAA receptors modulate the expression of prepulse inhibition
Hauser, J., Rudolph, U., Keist, R., Möhler, H., Feldon, J., & Yee, B. K. (2004) · Molecular Psychiatry · doi:10.1038/sj.mp.4001554 · Cited by 109
Self-citation
Blockade of alcohol's amnestic activity in humans by an α5 subtype benzodiazepine receptor inverse agonist
Nutt, D., Besson, M. J., Wilson, S. J., Dawson, G. R., & Lingford-Hughes, A. R. (2007) · Neuropharmacology · doi:10.1016/j.neuropharm.2007.08.008 · Cited by 109 · cited 1×
“2b ), a functionally selective compound, was able to reverse memory deficits induced by alcohol consumption in a small study involving human volunteer”
Background
Linkage and linkage disequilibrium mapping of ERP and EEG phenotypes
Bernice Porjesz, A., Begleiter, H., Wang, K., Almasy, L. A., Chorlian, D. B., Stimus, A. T., Samuel Kuperman, C., O’Connor, S., Rohrbaugh, J., Bauer, L. O., et al. (2002) · Biological Psychology · doi:10.1016/s0301-0511(02)00060-1 · Cited by 109
GABA A Receptor α5 Subunits Contribute to GABA A,slow Synaptic Inhibition in Mouse Hippocampus
Żarnowska, E. D., Keist, R., Rudolph, U., & Pearce, R. A. (2008) · Journal of Neurophysiology · doi:10.1152/jn.91203.2008 · Cited by 105
Self-citation
Comparison of the Novel Subtype-Selective GABAA Receptor-Positive Allosteric Modulator NS11394 [3′-[5-(1-Hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with Diazepam, Zolpidem, Bretazenil, and Gaboxadol in Rat Models of Inflammatory and Neuropathic Pain
Munro, G., Lopez-Garcia, J. A., Rivera‐Arconada, I., Erichsen, H. K., Nielsen, E. Ø., Larsen, J. S., Ahring, P. K., & Mirza, N. R. (2008) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.108.144568 · Cited by 103 · cited 1×
“NS11394 is antihyperalgesic in rat models of inflammatory and neuropathic pai”
Background
Antidepressant-like properties of α2-containing GABAA receptors
Vollenweider, I., Smith, K. S., Keist, R., & Rudolph, U. (2011) · Behavioural Brain Research · doi:10.1016/j.bbr.2010.10.009 · Cited by 96 · cited 1×
“Indeed, α2 knockout mice display increased anxiety and depression-like behaviour in the conflict-based novelty-suppressed feeding test, and increased depression-like behaviour in the despair-based forced swim and tail suspension test”
BackgroundSelf-citation
Association Between GABRA1 and Drinking Behaviors in the Collaborative Study on the Genetics of Alcoholism Sample
Dick, D. M., Plunkett, J., Wetherill, L. F., Xuei, X., Goate, A., HESSELBROCK, V. M., Schuckit, M. A., Crowe, R., Edenberg, H. J., & Foroud, T. (2006) · Alcoholism Clinical and Experimental Research · doi:10.1111/j.1530-0277.2006.00136.x · Cited by 94
Dynamic GABAAReceptor Subtype-Specific Modulation of the Synchrony and Duration of Thalamic Oscillations
Sohal, V. S., Keist, R., Rudolph, U., & Huguenard, J. R. (2003) · Journal of Neuroscience · doi:10.1523/jneurosci.23-09-03649.2003 · Cited by 92
Self-citation
Effects of benzodiazepine microinjection into the amygdala or periaqueductal gray on the expression of conditioned fear and hypoalgesia in rats.
Harris, J. A., & Westbrook, R. F. (1995) · Behavioral Neuroscience · doi:10.1037/0735-7044.109.2.295 · Cited by 92
An Historical Perspective on Gabaergic Drugs
Froestl, W. (2011) · Future Medicinal Chemistry · doi:10.4155/fmc.10.285 · Cited by 89 · cited 1×
“In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1, 2,4-triazol-5-ylme thoxy)-pyrazolo[1,5-d]-[1,2,4] triazine (MRK-016), a GABAA receptor α5 subtypeselective inverse agonist.”
Background
HZ166, a novel GABAA receptor subtype-selective benzodiazepine site ligand, is antihyperalgesic in mouse models of inflammatory and neuropathic pain
Lio, A. D., Benke, D., Besson, M. J., Desmeules, J. A., Daali, Y., Wang, Z., Edwankar, R. V., Cook, J. M., & Zeilhofer, H. U. (2010) · Neuropharmacology · doi:10.1016/j.neuropharm.2010.11.026 · Cited by 88 · cited 1×
“Likewise, the compound HZ-166, a partial agonist with selectivity for α2- and α3-containing GABA A receptors, had antihyperalgesic action in mouse models of neuropathic and inflammatory pai”
Background
NS11394 [3′-[5-(1-Hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], a Unique Subtype-Selective GABAA Receptor Positive Allosteric Modulator: In Vitro Actions, Pharmacokinetic Properties and in Vivo Anxiolytic Efficacy
Mirza, N. R., Larsen, J. S., Mathiasen, C., Jacobsen, T. A., Munro, G., Erichsen, H. K., Nielsen, A. N., Troelsen, K. B., NIELSEN, E. O., & Ahring, P. K. (2008) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.108.138859 · Cited by 87
Relationship between benzodiazepine receptor occupancy and functional effects in vivo of four ligands of differing intrinsic efficacies.
Martin‐Facklam, M., Schoch, P., Bonetti, E. P., Jenck, F., Martin, J. R., Moreau, J., & Haefely, W. E. (1992) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)11126-9 · Cited by 85
Linkage disequilibrium, haplotype and association studies of a chromosome 4 GABA receptor gene cluster: candidate gene variants for addictions
Drgon, T., D'Addario, C., & Uhl, G. R. (2006) · American Journal of Medical Genetics Part B Neuropsychiatric Genetics · doi:10.1002/ajmg.b.30349 · Cited by 82
Analysis of the Presence and Abundance of GABAA Receptors Containing Two Different Types of α Subunits in Murine Brain Using Point-mutated α Subunits
Benke, D., Fakitsas, P., Roggenmoser, C., Michel, C., Rudolph, U., & Möhler, H. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m407154200 · Cited by 81
Self-citation
Modulation of Long-term Potentiation in CA1 Region of Mouse Hippocampal Brain Slices by GABAA Receptor Benzodiazepine Site Ligands
Seabrook, G. R., Easter, A., Dawson, G. R., & Bowery, B. J. (1997) · Neuropharmacology · doi:10.1016/s0028-3908(97)00040-3 · Cited by 76 · cited 1×
“Several studies in animals and humans have suggested that classical benzodiazepines can impair learning and memor”
Background
In Vitro and in Vivo Properties of 3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA Receptor α5 Subtype-Selective Inverse Agonist
Atack, J. R., Maubach, K. A., Wafford, K. A., O'Connor, D. V., Rodrigues, A. D., Evans, D. C., Tattersall, F. D., Chambers, M. S., MacLeod, A. M., Eng, W., et al. (2009) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.109.157636 · Cited by 72
GABAA Receptor α2/α3 Subtype-Selective Modulators as Potential Nonsedating Anxiolytics
Atack, J. R. (2009) · Current topics in behavioral neurosciences · doi:10.1007/7854_2009_30 · Cited by 71 · cited 1×
“In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1, 2,4-triazol-5-ylme thoxy)-pyrazolo[1,5-d]-[1,2,4] triazine (MRK-016), a GABAA receptor α5 subtypeselective inverse agonist.”
Background
Reducing Abuse Liability of GABAA/Benzodiazepine Ligands via Selective Partial Agonist Efficacy at α1 and α2/3 Subtypes
Ator, N. A., Atack, J. R., Hargreaves, R. J., Burns, H. D., & Dawson, G. R. (2010) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.109.158303 · Cited by 66 · cited 1×
“Furthermore, in self-administration experiments in baboons, a withdrawal syndrome was observed following cessation of TPA123 self-administration (this compound displays 23% efficacy at α1-containing GABA A receptors, 35% efficacy at α2-containing GABA A receptors, 43% efficacy at α3-containing GABA A receptors and 19%…”
Result
Diazepam impairs place learning in the Morris water maze
Arolfo, M. P., & Brioni, J. D. (1991) · Behavioral and Neural Biology · doi:10.1016/0163-1047(91)80133-y · Cited by 65
Preclinical and clinical pharmacology of TPA023B, a GABA A receptor α2/α3 subtype-selective partial agonist
Atack, J. R., Hallett, D. J., Tye, S. J., Wafford, K. A., Ryan, C. N., Bohorquez, S. M. S., Eng, W., Gibson, R., Burns, H. D., Dawson, G., et al. (2010) · Journal of Psychopharmacology · doi:10.1177/0269881109354928 · Cited by 63
Identification of amino acid residues responsible for the α5 subunit binding selectivity of L‐655,708, a benzodiazepine binding site ligand at the GABAA receptor
Casula, M. A., Bromidge, F. A., Pillai, G. V., et al. (2001) · Journal of Neurochemistry · doi:10.1046/j.1471-4159.2001.00289.x · Cited by 61
MRK-409 (MK-0343), a GABA A receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans
Atack, J. R., Wafford, K. A., Street, L. O. N. D. O. N. G., Dawson, G., Tye, S. J., Laere, K. V., Bormans, G. M., Bohorquez, S. M. S., Lepeleire, I. D., de Hoon, J., et al. (2010) · Journal of Psychopharmacology · doi:10.1177/0269881109354927 · Cited by 60
GABAA-receptor α-subunit is an essential prerequisite for receptor formation in vivo
Fritschy, J., Benke, D., Johnson, D. K., et al. (1997) · Neuroscience · doi:10.1016/s0306-4522(97)00244-3 · Cited by 60 · cited 1×
“α5-containing GABA A receptors are predominantly expressed in the hippocampus (where they make up approximately 20% of all GABA A receptor”
BackgroundSelf-citation
A reduction in hippocampal GABA A receptor α5 subunits disrupts the memory for location of objects in mice
Prut, L., Prenosil, G., Willadt, S., Vogt, K., Fritschy, J. ‐., & Crestani, F. (2010) · Genes, Brain and Behavior · doi:10.1111/j.1601-183x.2010.00575.x · Cited by 53
A question of balance – Positive versus negative allosteric modulation of GABAA receptor subtypes as a driver of analgesic efficacy in rat models of inflammatory and neuropathic pain
Munro, G., Erichsen, H. K., Rae, M. G., & Mirza, N. R. (2011) · Neuropharmacology · doi:10.1016/j.neuropharm.2011.03.017 · Cited by 51
Rodent pharmacokinetics and receptor occupancy of the GABAA receptor subtype selective benzodiazepine site ligand L‐838417
Scott‐Stevens, P., Atack, J. R., Sohal, B., & Worboys, P. D. (2004) · Biopharmaceutics & Drug Disposition · doi:10.1002/bdd.423 · Cited by 50 · cited 1×
“However, unfavourable pharmacokinetic properties have precluded further development of this compoun”
Background
β3-Containing Gamma-Aminobutyric AcidA Receptors Are Not Major Targets for the Amnesic and Immobilizing Actions of Isoflurane
Liao, M. Y., Sonner, J. M., Jurd, R., Rudolph, U., Borghese, C. M., Harris, R. A., Laster, M. J., & Eger, E. I. (2005) · Anesthesia & Analgesia · doi:10.1213/01.ane.0000154196.86587.35 · Cited by 49
Self-citation
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Vinkers, C. H., Mirza, N. R., Olivier, B., & Kahn, R. S. (2010) · Expert Opinion on Investigational Drugs · doi:10.1517/13543784.2010.513382 · Cited by 39
Reversal of Ketamine-Induced Working Memory Impairments by the GABAAα2/3 Agonist TPA023
Castner, S. A., Arriza, J. L., Roberts, J. C., Mrzljak, L., Christian, E. P., & Williams, G. V. (2010) · Biological Psychiatry · doi:10.1016/j.biopsych.2010.01.001 · Cited by 37 · cited 1×
“It is interesting to note that TPA023 reversed ketamine-induced impairments in spatial working memory in rhesus monkeys but not the ketamine-induced hallucinatory-like behaviours, emphasizing the functional specificity of this approac”
Background
Efficacy of alprazolam in reducing fluoxetine-induced jitteriness in patients with major depression.
Amsterdam, J. D., Hornig, M., & Maislin, G. (1994) · PubMed · Cited by 36
Antipsychotic effects of bretazenil, a partial benzodiazepine agonist in acute schizophrenia—A study group report
Delini‐Stula, A., & Berdah-Tordjman, D. (1996) · Journal of Psychiatric Research · doi:10.1016/0022-3956(96)00003-9 · Cited by 35 · cited 1×
“Before the functions of the different GABA A receptor subtypes were known, the non-selective partial agonist and anxiolytic bretazenil was shown to be efficacious as monotherapy in approximately 40% of patients with acute episodes of schizophrenia of moderate to marked severit”
Background
Isoflurane-induced surgical tolerance mediated only in part by β3-containing GABAA receptors
Lambert, S., Arras, M., Vogt, K. E., & Rudolph, U. (2005) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2005.04.030 · Cited by 35
Self-citation
The role of GABA-A receptor subtypes as analgesic targets
Mirza, N. R., & Munro, G. (2010) · Drug News & Perspectives · doi:10.1358/dnp.2010.23.6.1489909 · Cited by 31
A Multicenter, Placebo‐Controlled, Double‐Blind, Randomized Study of Efficacy and Safety of Ocinaplon (DOV 273,547) in Generalized Anxiety Disorder
Czobor, P., Skolnick, P., Beer, B., & Lippa, A. (2010) · CNS Neuroscience & Therapeutics · doi:10.1111/j.1755-5949.2009.00109.x · Cited by 29 · cited 1×
“2a ), had anxiolytic but not sedative effects in rodents and in humans, as demonstrated in Phase I and Phase II studies with 127 and 60 patients, respectivel”
Background
Contribution of GABAA receptors containing α3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys
Fischer, B. D., Atack, J. R., Platt, D. M., Reynolds, D. S., Dawson, G. R., & Rowlett, J. K. (2010) · Psychopharmacology · doi:10.1007/s00213-010-2142-y · Cited by 26
ASSESSMENT OF BENZODIAZEPINE DEPENDENCE IN ALCOHOL AND DRUG DEPENDENT OUTPATIENTS: A RESEARCH REPORT
Kan, C. C., Breteler, M., van der Ven, A., Timmermans, M. A., & Zitman, F. (2001) · Substance Use & Misuse · doi:10.1081/ja-100104491 · Cited by 21 · cited 1×
“However, in alcohol- and drug-dependent outpatients, benzodiazepine dependence was found to be prevalen”
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Authors: Rudolph, U., & Knoflach, F.
Affiliations: Harvard University (US)
F. Hoffmann-La Roche AG (CH)
Corresponding author: Rudolph, Uwe
ORCID: Rudolph, Uwe
Knoflach, Frédéric
Venue: Nature Reviews Drug Discovery
Publisher: Springer Science and Business Media LLC
Published: 2011-07-29
Volume: 10
Issue: 9
Pages: 685-697
ISSN: 1474-1776 (ISSN-L)
1474-1784
DOI: 10.1038/nrd3502
PMC: PMC3375401
OpenAlex: W2013775967
Semantic Scholar: bfb4fcd647899053b94eaf5edf1fe9e748076c6b
Cited by: 733
References: 111
Citations by year: 2026: 41 · 2025: 42 · 2024: 35 · 2023: 46 · 2022: 43 · 2021: 55 · 2020: 49 · 2019: 56 · 2018: 51 · 2017: 58 · 2016: 52 · 2015: 45 · 2014: 62 · 2013: 58 · 2012: 38
FWCI: 4.90
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.springer.com/tdm (tdm)
Locations: Nature Reviews Drug Discovery (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Funders: National Institute of Mental Health (R21MH087829, R01MH080006, R03MH085149, MH087829, MH085149, MH080006)
National Institute on Drug Abuse (DA027051, DA026578, R03DA026578, R03DA027051)
National Institute of General Medical Sciences (R01GM086448, GM086448)
Topics: Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
Health Sciences › Medicine › Clinical Neurology › Epilepsy research and treatment
Keywords: GABAA receptor, benzodiazepines, GABAA receptor subtypes, ligand-gated ion channels, chronic pain, depression, schizophrenia, cognitive enhancement, stroke, drug addiction
MeSH terms: Analgesics, Animals, Anxiety Disorders, Benzodiazepines, Depressive Disorder, Humans, Hypnotics and Sedatives, Sleep Initiation and Maintenance Disorders, Mutation, Receptors, GABA-A, Schizophrenia, Nootropic Agents, GABA Modulators, Substance-Related Disorders, Stroke

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Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes

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