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Neurosteroids: endogenous regulators of the GABAA receptor

Belelli, Delia, Lambert, Jeremy J.·2005·Nature reviews. Neuroscience

DOI 10.1038/nrn1703

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Abstract

GABA(A) (gamma-aminobutyric acid type A) receptors mediate most of the 'fast' synaptic inhibition in the mammalian brain and are targeted by many clinically important drugs. Certain naturally occurring pregnane steroids can potently and specifically enhance GABA(A) receptor function in a nongenomic (direct) manner, and consequently have anxiolytic, analgesic, anticonvulsant, sedative, hypnotic and anaesthetic properties. These steroids not only act as remote endocrine messengers, but also can be synthesized in the brain, where they modify neuronal activity locally by modulating GABA(A) receptor function. Such 'neurosteroids' can influence mood and behaviour in various physiological and pathophysiological situations, and might contribute to the behavioural effects of psychoactive drugs.

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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
Excitatory actions of gaba during development: the nature of the nurture
Ben-Ari, Y. (2002) · Nature Reviews Neuroscience · doi:10.1038/nrn920 · Cited by 2,448
Variations on an inhibitory theme: phasic and tonic activation of GABAA receptors
Farrant, M., & Nusser, Z. (2005) · Nature Reviews Neuroscience · doi:10.1038/nrn1625 · Cited by 2,081
Neuroactive steroids
Paul, S. M., & Purdy, R. H. (1992) · The FASEB Journal · doi:10.1096/fasebj.6.6.1347506 · Cited by 1,413
International Union of Pharmacology. XV. Subtypes of gamma-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor function.
Barnard, E. A., Skolnick, P., Olsen, R. W., Möhler, H., Sieghart, W., Biggio, G., Bræstrup, C., Bateson, A. N., & Langer, S. Z. (1998) · PubMed · Cited by 1,204
Is there more to gaba than synaptic inhibition?
Owens, D. F., & Kriegstein, A. R. (2002) · Nature reviews. Neuroscience · doi:10.1038/nrn919 · Cited by 1,172
Receptor trafficking and synaptic plasticity
Collingridge, G. L., Isaac, J. T. R., & Wang, Y. T. (2004) · Nature Reviews Neuroscience · doi:10.1038/nrn1556 · Cited by 1,046
Stress-induced elevations of gamma-aminobutyric acid type A receptor-active steroids in the rat brain.
Purdy, R. H., Morrow, A. L., Moore, P. H., & Paul, S. M. (1991) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.88.10.4553 · Cited by 951
Subunit Composition, Distribution and Function of GABA-A Receptor Subtypes
Sieghart, W., & Sperk, G. (2002) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026023393507 · Cited by 914
Neuroactive steroids reduce neuronal excitability by selectively enhancing tonic inhibition mediated by δ subunit-containing GABA A receptors
Stell, B. M., Brickley, S. G., Tang, C., Farrant, M., & Módy, I. (2003) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2435457100 · Cited by 799
Molecular and neuronal substrates for general anaesthetics
Rudolph, U., & Antkowiak, B. (2004) · Nature reviews. Neuroscience · doi:10.1038/nrn1496 · Cited by 771
Neurosteroids and GABAA receptor function
Lambert, J. J., Belelli, D., Hill-Venning, C., & Peters, J. A. (1995) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(00)89058-6 · Cited by 746
Self-citation
Non-genomic and genomic effects of steroids on neural activity
McEwen, B. S. (1991) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(91)90531-v · Cited by 722
Increase in the cerebrospinal fluid content of neurosteroids in patients with unipolar major depression who are receiving fluoxetine or fluvoxamine
Uzunova, V., Sheline, Y. I., Davis, J. M., Rasmusson, A. M., Uzunov, D. P., Costa, E., & Guidotti, A. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.6.3239 · Cited by 672
Pharmacological characterization of a novel cell line expressing human α4β3δ GABAA receptors
Brown, N. A., Kerby, J., Bonnert, T. P., Whiting, P. J., & Wafford, K. A. (2002) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0704795 · Cited by 603
The benzodiazepine binding site of GABAA receptors
Sigel, E. (1997) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(97)01118-8 · Cited by 598
Tonic inhibition in mouse hippocampal CA1 pyramidal neurons is mediated by α5 subunit-containing γ-aminobutyric acid type A receptors
Caraiscos, V. B., Elliott, E. M., You-Ten, K. E., Cheng, V., Belelli, D., Newell, J. G., Jackson, M. F., Lambert, J. J., Rosahl, T. W., Wafford, K. A., et al. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0307231101 · Cited by 571
Self-citation
Neurosteroids: biochemistry and clinical significance
Mellon, S. H., & Griffin, L. D. (2002) · Trends in Endocrinology & Metabolism · doi:10.1016/s1043-2760(01)00503-3 · Cited by 538
Analysis of GABA A Receptor Function and Dissection of the Pharmacology of Benzodiazepines and General Anesthetics Through Mouse Genetics
Rudolph, U., & Möhler, H. (2004) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.44.101802.121429 · Cited by 528
Attenuated sensitivity to neuroactive steroids in γ-aminobutyrate type A receptor delta subunit knockout mice
Mihalek, R., Banerjee, P., Korpi, E. R., Quinlan, J. J., Firestone, L. L., Mi, Z.-P., Lagenaur, C. F., Tretter, V. E., Sieghart, W., Anagnostaras, S., et al. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.22.12905 · Cited by 520
Modulation of the GABA receptor complex by a steroid anaesthetic
Harrison, N. L., & Simmonds, M. A. (1984) · Brain Research · doi:10.1016/0006-8993(84)90299-3 · Cited by 501
Neurosteroid modulation of GABAA receptors
Lambert, J. J., Belelli, D., Peden, D. R., Vardy, A., & Peters, J. A. (2003) · Progress in Neurobiology · doi:10.1016/j.pneurobio.2003.09.001 · Cited by 498
Self-citation
Constructing inhibitory synapses
Moss, S. J., & Smart, T. G. (2001) · Nature reviews. Neuroscience · doi:10.1038/35067500 · Cited by 467
Ethanol enhances α 4 β 3 δ and α 6 β 3 δ γ-aminobutyric acid type A receptors at low concentrations known to affect humans
Wallner, M., Hanchar, H. J., & Olsen, R. W. (2003) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2435171100 · Cited by 463
Neuroactive steroids: mechanisms of action and neuropsychopharmacological properties
Rupprecht, R. (2003) · Psychoneuroendocrinology · doi:10.1016/s0306-4530(02)00064-1 · Cited by 427
Insensitivity to anaesthetic agents conferred by a class of GABAA receptor subunit
Davies, P. A., Hanna, M. C., Hales, T. G., & Kirkness, E. F. (1997) · Nature · doi:10.1038/385820a0 · Cited by 404
Enhanced Neurosteroid Potentiation of Ternary GABAAReceptors Containing the δ Subunit
Wohlfarth, K., Bianchi, M. T., & Macdonald, R. L. (2002) · Journal of Neuroscience · doi:10.1523/jneurosci.22-05-01541.2002 · Cited by 397
Niemann-Pick type C disease involves disrupted neurosteroidogenesis and responds to allopregnanolone
Griffin, L. D., Gong, W., Verot, L., & Mellon, S. H. (2004) · Nature Medicine · doi:10.1038/nm1073 · Cited by 395
The interaction of the general anesthetic etomidate with the γ-aminobutyric acid type A receptor is influenced by a single amino acid
Belelli, D., Lambert, J. J., Peters, J. A., Wafford, K. A., & Whiting, P. J. (1997) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.94.20.11031 · Cited by 392
Self-citation
Neurosteroids: Expression of Steroidogenic Enzymes and Regulation of Steroid Biosynthesis in the Central Nervous System
Mensah‐Nyagan, A. G., do Rego, J. L., Beaujean, D., Luu-The, V., Pelletier, G., & Vaudry, H. (1999) · Pharmacological Reviews · doi:10.1016/s0031-6997(24)01395-4 · Cited by 389
Selective serotonin reuptake inhibitors directly alter activity of neurosteroidogenic enzymes
Griffin, L. D., & Mellon, S. H. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.23.13512 · Cited by 387
Tissue distribution and kinetic characteristics of rat steroid 5 alpha-reductase isozymes. Evidence for distinct physiological functions.
Normington, K., & Russell, D. W. (1992) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)41809-1 · Cited by 379
Anesthetic Effect of Steroid Hormones.
Selye, H. (1941) · Experimental Biology and Medicine · doi:10.3181/00379727-46-11907 · Cited by 375
Tonic and Spillover Inhibition of Granule Cells Control Information Flow through Cerebellar Cortex
Hamann, M., Rossi, D. J., & Attwell, D. (2002) · Neuron · doi:10.1016/s0896-6273(02)00593-7 · Cited by 347
The influence of subunit composition on the interaction of neurosteroids with GABAA receptors
Belelli, D., Casula, A. M., Ling, A., & Lambert, J. J. (2002) · Neuropharmacology · doi:10.1016/s0028-3908(02)00172-7 · Cited by 335
Self-citation
Neurosteroid quantification in human brain regions: comparison between Alzheimer’s and nondemented patients
Weill-Engerer, S., David, J.-P., Sazdovitch, V., Liere, P., Eychenne, B., Pianos, A., Schumacher, M., Delacourte, A., Baulieu, E.-E., & Akwa, Y. (2002) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2002-020878 · Cited by 333
Supersensitivity to allosteric GABAA receptor modulators and alcohol in mice lacking PKCε
Hodge, C. W., Mehmert, K. K., Kelley, S. P., McMahon, T., Haywood, A., Olive, M. F., Wang, D., Sánchez‐Pérez, A. M., & Messing, R. O. (1999) · Nature Neuroscience · doi:10.1038/14795 · Cited by 323
Formation and plasticity of GABAergic synapses: physiological mechanisms and pathophysiological implications
Fritschy, J., & Brünig, I. (2003) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(03)00037-8 · Cited by 322
Sedation and Anesthesia Mediated by Distinct GABA A Receptor Isoforms
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., et al. (2003) · The Journal of Neuroscience · doi:10.1523/jneurosci.23-24-08608.2003 · Cited by 318
Self-citation
Biosynthesis and action of neurosteroids
Mellon, S. H., Griffin, L. D., & Compagnone, N. A. (2001) · Brain Research Reviews · doi:10.1016/s0165-0173(01)00109-6 · Cited by 305
Steroid hormones and neurosteroids in normal and pathological aging of the nervous system
Schumacher, M., Weill‐Engerer, S., Lière, P., Robert, F., Franklin, R. J. M., García‐Segura, L. M., Lambert, J. J., Mayo, W., Melcangi, R. C., Párducz, Á., et al. (2003) · Progress in Neurobiology · doi:10.1016/j.pneurobio.2003.09.004 · Cited by 299
Self-citation
Modulation of the GABAA receptor by depressant barbiturates and pregnane steroids
Peters, J. A., Kirkness, E. F., Callachan, H., Lambert, J. J., & Turner, A. J. (1988) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1988.tb11646.x · Cited by 294
Self-citation
The benzodiazepine binding site of GABAA receptors
Sigel, E., & Buhr, A. (1997) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(97)90675-1 · Cited by 290
Regulation of GABAA receptor trafficking, channel activity, and functional plasticity of inhibitory synapses
Lüscher, B., & Keller, C. A. (2004) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2004.04.003 · Cited by 280
Gamma-hydroxybutyrate: an emerging drug of abuse that causes physical dependence
Galloway, G. P., Frederick, S. L., Staggers, F. E., Gonzales, M., Stalcup, S. A., & Smith, D. E. (1997) · Addiction · doi:10.1111/j.1360-0443.1997.tb03640.x · Cited by 277
Benzodiazepine receptor protein identified and visualized in brain tissue by a photoaffinity label.
Möhler, H., Battersby, M. K., & Richards, J. G. (1980) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.77.3.1666 · Cited by 273
Characterization of the Anticonvulsant Properties of Ganaxolone (CCD 1042; 3α-Hydroxy-3β-methyl-5α-pregnan-20-one), a Selective, High-Affinity, Steroid Modulator of the γ-Aminobutyric AcidA Receptor
Carter, R. B., Wood, P. L., Wieland, S., Hawkinson, J. E., Belelli, D., Lambert, J. J., White, H. S., Wolf, H. H., Mirsadeghi, S., Tahir, S. H., et al. (1997) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)36511-5 · Cited by 269
Self-citation
Brain 5α-dihydroprogesterone and allopregnanolone synthesis in a mouse model of protracted social isolation
Dong, E., Matsumoto, K., Uzunova, V., Sugaya, I., Takahata, H., Nomura, H., Watanabe, H., Costa, E., & Guidotti, A. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.051628598 · Cited by 261
Modulation of the GABAA receptor by progesterone metabolites
Callachan, H., Cottrell, G. A., Hather, N. Y., Lambert, J. J., Nooney, J. M., & Peters, J. A. (1987) · Proceedings of the Royal Society B Biological Sciences · doi:10.1098/rspb.1987.0049 · Cited by 256
Self-citation
Analysis of the set of GABAA receptor genes in the human genome
Simon, J., Wakimoto, H., Fujita, N., Lalande, M., & Barnard, E. A. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m401354200 · Cited by 253
Characterization of the anticonvulsant properties of ganaxolone (CCD 1042; 3alpha-hydroxy-3beta-methyl-5alpha-pregnan-20-one), a selective, high-affinity, steroid modulator of the gamma-aminobutyric acid(A) receptor.
Carter, R. B., Wood, P. L., Wieland, S., Hawkinson, J. E., Belelli, D., Lambert, J. J., White, H. S., Wolf, H. H., Mirsadeghi, S., Tahir, S. H., et al. (1997) · PubMed · Cited by 251
Self-citation
Benzodiazepines act on GABAA receptors via two distinct and separable mechanisms
Walters, R. J., Hadley, S. H., Morris, K. D. W., & Αmin, J. (2000) · Nature Neuroscience · doi:10.1038/81800 · Cited by 243
Low Ethanol Concentrations Selectively Augment the Tonic Inhibition Mediated by δ Subunit-Containing GABAAReceptors in Hippocampal Neurons
Wei, W., Faria, L. C., & Módy, I. (2004) · Journal of Neuroscience · doi:10.1523/jneurosci.2040-04.2004 · Cited by 242
Plasticity in Fast Synaptic Inhibition of Adult Oxytocin Neurons Caused by Switch in GABAA Receptor Subunit Expression
Brussaard, A. B., Kits, K. S., Baker, R. E., Willems, W. P. A., Leyting-Vermeulen, J. W., Voorn, P., Smit, A. B., Bicknell, R. J., & Herbison, A. E. (1997) · Neuron · doi:10.1016/s0896-6273(00)80401-8 · Cited by 227
Neuroactive steroids: potential therapeutic use in neurological and psychiatric disorders
Ga̧sior, M., Carter, R. B., & Witkin, J. M. (1999) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(99)01318-8 · Cited by 218
Neuronally Restricted RNA Splicing Regulates the Expression of a Novel GABA A Receptor Subunit Conferring Atypical Functional Properties
Whiting, P. J., McAllister, G., Vassilatis, D. K., Bonnert, T. P., HEAVENS, R. P., Smith, D. W., Hewson, L., O’Donnell, R., Rigby, M. R., SIRINATHSINGHJI, D. J. S., et al. (1997) · Journal of Neuroscience · doi:10.1523/jneurosci.17-13-05027.1997 · Cited by 211
Brain Steroidogenesis Mediates Ethanol Modulation of GABAAReceptor Activity in Rat Hippocampus
Sanna, E., Talani, G., Busonero, F., Pisu, M. G., Purdy, R. H., Serra, M., & Biggio, G. (2004) · Journal of Neuroscience · doi:10.1523/jneurosci.0075-04.2004 · Cited by 211
Neurosteroids Shift Partial Agonist Activation of GABAAReceptor Channels from Low- to High-Efficacy Gating Patterns
Bianchi, M. T., & Macdonald, R. L. (2003) · Journal of Neuroscience · doi:10.1523/jneurosci.23-34-10934.2003 · Cited by 206
Effect of Zolpidem on Miniature IPSCs and Occupancy of Postsynaptic GABAAReceptors in Central Synapses
Perrais, D., & Ropert, N. (1999) · Journal of Neuroscience · doi:10.1523/jneurosci.19-02-00578.1999 · Cited by 188
Catamenial Epilepsy: A Review
Newmark, M. E., & Penry, J. K. (1980) · Epilepsia · doi:10.1111/j.1528-1157.1980.tb04074.x · Cited by 186
The socially-isolated mouse: a model to study the putative role of allopregnanolone and 5α-dihydroprogesterone in psychiatric disorders
Guidotti, A., Dong, E., Matsumoto, K., Pinna, G., Rasmusson, A. M., & Costa, E. (2001) · Brain Research Reviews · doi:10.1016/s0165-0173(01)00129-1 · Cited by 169
Ovarian hormones, anticonvulsant drugs, and seizures during the menstrual cycle in women with epilepsy.
Rościszewska, D., Buntner, B., Guz, I., & Zawisza, L. (1986) · Journal of Neurology Neurosurgery & Psychiatry · doi:10.1136/jnnp.49.1.47 · Cited by 169
Identification of a [3H]muscimol photoaffinity substrate in the bovine gamma-aminobutyric acidA receptor alpha subunit.
Smith, G. B., & Olsen, R. W. (1994) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(17)32003-3 · Cited by 165
Ethanol regulation of γ-aminobutyric acidA receptors: genomic and nongenomic mechanisms
Kumar, S., Fleming, R. L., & Morrow, A. L. (2004) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2003.12.001 · Cited by 158
Potentiation of inhibition by general anaesthetics in neurones of the olfactory cortex in vitro
Scholfield, C. N. (1980) · Pflügers Archiv - European Journal of Physiology · doi:10.1007/bf00587527 · Cited by 152
Actions of synthetic and endogenous steroids on the GABAA receptor
Lambert, J. J., Peters, J. A., & Cottrell, G. A. (1987) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(87)90067-8 · Cited by 147
Self-citation
Role of neurosteroids in catamenial epilepsy
Reddy, D. S. (2004) · Epilepsy Research · doi:10.1016/j.eplepsyres.2004.09.003 · Cited by 144
The C Terminus of the Human Nicotinic α4β2 Receptor Forms a Binding Site Required for Potentiation by an Estrogenic Steroid
Paradiso, K. G., Zhang, J., & Steinbach, J. H. (2001) · Journal of Neuroscience · doi:10.1523/jneurosci.21-17-06561.2001 · Cited by 144
Anticonvulsant steroids and the GABA/benzodiazepine receptor-chloride ionophore complex
Belelli, D., Lan, N. C., & Gee, K. W. (1990) · Neuroscience & Biobehavioral Reviews · doi:10.1016/s0149-7634(05)80041-7 · Cited by 142
Self-citation
Decreased anxiety-like behavior, reduced stress hormones, and neurosteroid supersensitivity in mice lacking protein kinase Cε
Hodge, C. W., Raber, J., McMahon, T., Walter, M. H., Sánchez‐Pérez, A. M., Olive, M. F., Mehmert, K. K., Morrow, A. L., & Messing, R. O. (2002) · Journal of Clinical Investigation · doi:10.1172/jci200215903 · Cited by 135
Aspects of the homeostaic plasticity of GABAA receptor‐mediated inhibition
Módy, I. (2004) · The Journal of Physiology · doi:10.1113/jphysiol.2004.077362 · Cited by 135
Brain allopregnanolone regulates the potency of the GABAA receptor agonist muscimol
Pinna, G., Uzunova, V., Matsumoto, K., Puia, G., Mienville, J., Costa, E., & Guidotti, A. (2000) · Neuropharmacology · doi:10.1016/s0028-3908(99)00149-5 · Cited by 134
General anaesthetic action at transmitter-gated inhibitory amino acid receptors
Belelli, D., Pistis, M., Peters, J. A., & Lambert, J. J. (1999) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(99)01405-4 · Cited by 132
Self-citation
Oxytocin Regulates Neurosteroid Modulation of GABAAReceptors in Supraoptic Nucleus around Parturition
Koksma, J.-J., van Kesteren, R. E., Rosahl, T. W., Zwart, R., Smit, A. B., Lüddens, H., & Brussaard, A. B. (2003) · Journal of Neuroscience · doi:10.1523/jneurosci.23-03-00788.2003 · Cited by 130
Seizure exacerbation associated with inhibition of progesterone metabolism
Herzog, A. G., & Frye, C. A. (2003) · Annals of Neurology · doi:10.1002/ana.10508 · Cited by 129
Specific GABAA circuits in brain development and therapy
Möhler, H., Fritschy, J., Crestani, F., Hensch, T. K., & Rudolph, U. (2004) · Biochemical Pharmacology · doi:10.1016/j.bcp.2004.07.025 · Cited by 127
The Contraceptive Agent Provera Enhances GABAAReceptor-Mediated Inhibitory Neurotransmission in the Rat Hippocampus: Evidence for Endogenous Neurosteroids?
Belelli, D., & Herd, M. B. (2003) · Journal of Neuroscience · doi:10.1523/jneurosci.23-31-10013.2003 · Cited by 123
Self-citation
Slow Actions of Neuroactive Steroids at GABAAReceptors
Shu, H., Eisenman, L. N., Jinadasa, D., Covey, D. F., Zorumski, C. F., & Mennerick, S. J. (2004) · Journal of Neuroscience · doi:10.1523/jneurosci.1399-04.2004 · Cited by 122
The antagonism between anesthetic steroid hormones and pentamethylenetetrazol (Metrazol)
Selye, H. (1942) · Journal of Laboratory and Clinical Medicine · Cited by 118
The Major Site of Photoaffinity Labeling of the γ-Aminobutyric Acid Type A Receptor by [3H]Flunitrazepam Is Histidine 102 of the α Subunit
Duncalfe, L. L., Carpenter, M. R., Smillie, L. B., Martin, I. L., & Dunn, S. M. J. (1996) · Journal of Biological Chemistry · doi:10.1074/jbc.271.16.9209 · Cited by 113
Modulation of GABAergic synaptic transmission by the non-benzodiazepine anxiolytic etifoxine
Schlichter, R., Rybalchenko, V., Poisbeau, P., Verleye, M., & Gillardin, J. M. (2000) · Neuropharmacology · doi:10.1016/s0028-3908(99)00253-1 · Cited by 111
Intact Synaptic GABAergic Inhibition and Altered Neurosteroid Modulation of Thalamic Relay Neurons in Mice Lacking δ Subunit
Porcello, D. M., Huntsman, M. M., Mihalek, R., Homanics, G. E., & Huguenard, J. R. (2003) · Journal of Neurophysiology · doi:10.1152/jn.00899.2002 · Cited by 110
Effects of a naturally occurring neurosteroid on GABAA IPSCs during development in rat hippocampal or cerebellar slices
Cooper, E. J., Johnston, G. A. R., & Edwards, F. A. (1999) · The Journal of Physiology · doi:10.1111/j.1469-7793.1999.00437.x · Cited by 109
The neurosteroid 3 alpha-hydroxy-5 alpha-pregnan-20-one induces cytoarchitectural regression in cultured fetal hippocampal neurons
Brinton, R. D. (1994) · Journal of Neuroscience · doi:10.1523/jneurosci.14-05-02763.1994 · Cited by 108
Neurosteroids A New Regulatory Function in the Nervous System
(2000) · Clinical Endocrinology · doi:10.1046/j.1365-2265.2000.01084.x · Cited by 107
Enantioselectivity of steroid-induced gamma-aminobutyric acidA receptor modulation and anesthesia.
Wittmer, L. L., Hu, Y., Kalkbrenner, M., Evers, A. S., Zorumski, C. F., & Covey, D. F. (1996) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)09617-8 · Cited by 102
Enantioselectivity of Pregnanolone-Induced γ-Aminobutyric AcidA Receptor Modulation and Anesthesia
Covey, D. F., Nathan, D., Kalkbrenner, M., Nilsson, K. R., Hu, Y., Zorumski, C. F., & Evers, A. S. (2000) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)39327-9 · Cited by 97
On the putative physiological role of allopregnanolone on GABAA receptor function
Puia, G., Mienville, J., Matsumoto, K., Takahata, H., Watanabe, H., Costa, E., & Guidotti, A. (2003) · Neuropharmacology · doi:10.1016/s0028-3908(02)00341-6 · Cited by 95
Regional distribution of cytosolic and particulate 5α-dihydroprogesterone 3α-hydroxysteroid oxidoreductases in female rat brain
Li, X., Bertics, P. J., & Karavolas, H. J. (1997) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/s0960-0760(96)00195-1 · Cited by 95
Enantioselectivity of pregnanolone-induced gamma-aminobutyric acid(A) receptor modulation and anesthesia.
Covey, D. F., Nathan, D., Kalkbrenner, M., Nilsson, K. R., Hu, Y., Zorumski, C. F., & Evers, A. S. (2000) · PubMed · Cited by 92
Phosphorylation influences neurosteroid modulation of synaptic GABAA receptors in rat CA1 and dentate gyrus neurones
Harney, S. C., Frenguelli, B. G., & Lambert, J. J. (2003) · Neuropharmacology · doi:10.1016/s0028-3908(03)00251-x · Cited by 91
Self-citation
Production of 5α-Reduced Neurosteroids Is Developmentally Regulated and Shapes GABAAMiniature IPSCs in Lamina II of the Spinal Cord
Keller, A. F., Breton, J., Schlichter, R., & Poisbeau, P. (2004) · Journal of Neuroscience · doi:10.1523/jneurosci.4642-03.2004 · Cited by 90
Selective Antagonism of 5α-Reduced Neurosteroid Effects at GABAA Receptors
Mennerick, S. J., He, Y., Jiang, X. Q., Manion, B. D., Wang, M., Shute, A. A., Benz, A. M., Evers, A. S., Covey, D. F., & Zorumski, C. F. (2004) · Molecular Pharmacology · doi:10.1124/mol.65.5.1191 · Cited by 88
Pharmacological plasticity of GABAA receptors at dentate gyrus synapses in a rat model of temporal lobe epilepsy
Leroy, C., Poisbeau, P., Keller, A. F., & Nehlig, A. (2004) · The Journal of Physiology · doi:10.1113/jphysiol.2003.059246 · Cited by 85
Neuroactive steroids have multiple actions to potentiate GABAA receptors
Akk, G., Bracamontes, J. R., Covey, D. F., Evers, A. S., Dao, T., & Steinbach, J. H. (2004) · The Journal of Physiology · doi:10.1113/jphysiol.2004.066571 · Cited by 83
GABAA receptor δ subunit deletion prevents neurosteroid modulation of inhibitory synaptic currents in cerebellar neurons
Vicini, S., Losi, G., & Homanics, G. E. (2002) · Neuropharmacology · doi:10.1016/s0028-3908(02)00126-0 · Cited by 82
Kinetics of Allopregnanolone Formation Catalyzed by Human 3α-Hydroxysteroid Dehydrogenase Type III (AKR1C2)
Trauger, J. W., Jiang, A., Stearns, B. A., & LoGrasso, P. V. (2002) · Biochemistry · doi:10.1021/bi026109w · Cited by 81
Protein kinase C regulation of GABAA receptors
Song, M., & Messing, R. O. (2005) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-004-4339-x · Cited by 79
Photoaffinity Labeling with a Neuroactive Steroid Analogue
Darbandi-Tonkabon, R., Hastings, W. R., Zeng, C., Akk, G., Manion, B. D., Bracamontes, J. R., Steinbach, J. H., Mennerick, S. J., Covey, D. F., & Evers, A. S. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m213168200 · Cited by 78
Perinatal Neurosteroid Levels Influence GABAergic Interneuron Localization in Adult Rat Prefrontal Cortex
Grobin, A. C., Heenan, E. J., Lieberman, J. A., & Morrow, A. L. (2003) · Journal of Neuroscience · doi:10.1523/jneurosci.23-05-01832.2003 · Cited by 76
Neurosteroidogenesis: Relevance to Neurosteroid Actions in Brain and Modulation by Psychotropic Drugs
Barbaccia, M. L. (2004) · Critical Reviews in Neurobiology · doi:10.1615/critrevneurobiol.v16.i12.70 · Cited by 76
Neurosteroids: A New Regulatory Function in the Nervous System
Ross, L. E., & Sellers, E. M. (1999) · Behavioural Neurology · doi:10.1155/1999/308037 · Cited by 75
Decreased plasma and cerebrospinal fluid content of neuroactive steroids in Parkinson’s disease
di Michele, F., Longone, P., Romeo, E., Lucchetti, S., Brusa, L., Pierantozzi, M., Bassi, A., Bernardi, G., & Stanzione, P. (2003) · Neurological Sciences · doi:10.1007/s10072-003-0115-1 · Cited by 72
Fluoxetine and norfluoxetine stereospecifically facilitate pentobarbital sedation by increasing neurosteroids
Pinna, G., Costa, E., & Guidotti, A. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0401479101 · Cited by 68
Differential modulation of the gamma-aminobutyric acid type C receptor by neuroactive steroids.
Morris, K. D. W., Moorefield, C., & Αmin, J. (1999) · PubMed · Cited by 61
Neurosteroids act on the GABAA receptor at sites on the N-terminal side of the middle of TM2
Rick, C., Ye, Q., Finn, S. E., & Harrison, N. L. (1998) · Neuroreport · doi:10.1097/00001756-199802160-00004 · Cited by 60
Techniques: Use of concatenated subunits for the study of ligand-gated ion channels
Minier, F., & Sigel, E. (2004) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2004.07.005 · Cited by 60
Steroid Effects on Neuronal Activity: When is the Genome Involved?
McEwen, B. S., Coirini, H., & Schumacher, M. (2007) · Novartis Foundation symposium · doi:10.1002/9780470513989.ch2 · Cited by 58
Overexpression of the GABAA receptor ε subunit results in insensitivity to anaesthetics
Thompson, S. A., Bonnert, T. P., Cagetti, E., Whiting, P. J., & Wafford, K. A. (2002) · Neuropharmacology · doi:10.1016/s0028-3908(02)00162-4 · Cited by 55
Effect of acute ethanol administration and acute allopregnanolone administration on spontaneous hippocampal pyramidal cell neural activity
Tokunaga, S., McDaniel, J. R., Morrow, A. L., & Matthews, D. B. (2003) · Brain Research · doi:10.1016/s0006-8993(02)04266-x · Cited by 53
A Single M1 Residue in the β2 Subunit Alters Channel Gating of GABAA Receptor in Anesthetic Modulation and Direct Activation
Chang, C.-S. S., Olcese, R., & Olsen, R. W. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m306978200 · Cited by 53
A single amino acid confers barbiturate sensitivity upon the GABA ρ1 receptor
Belelli, D., Pau, D., Cabras, G., Peters, J. A., & Lambert, J. J. (1999) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0702611 · Cited by 52
Self-citation
Slow Death of Postnatal Hippocampal Neurons by GABAAReceptor Overactivation
Xu, W., Cormier, R. J., Fu, T., Covey, D. F., Isenberg, K. E., Zorumski, C. F., & Mennerick, S. J. (2000) · Journal of Neuroscience · doi:10.1523/jneurosci.20-09-03147.2000 · Cited by 50
THE PHYSIOLOGICAL ACTION OF CHOLESTEROL
Cashin, M. F., & Morávek, V. (1927) · American Journal of Physiology-Legacy Content · doi:10.1152/ajplegacy.1927.82.2.294 · Cited by 49
Neurosteroid Effects in the Central Nervous System
Smith, S. S. (2003) · CRC Press eBooks · doi:10.1201/9780203508169 · Cited by 42
Neuroactive Steroid Interactions with Voltage-Dependent Anion Channels: Lack of Relationship to GABAA Receptor Modulation and Anesthesia
Darbandi-Tonkabon, R., Manion, B. D., Hastings, W. R., Craigen, W. J., Akk, G., Bracamontes, J. R., He, Y., Sheiko, T. V., Steinbach, J. H., Mennerick, S. J., et al. (2004) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.103.058123 · Cited by 40
Sites of positive allosteric modulation by neurosteroids on ionotropic γ‐aminobutyric acid receptor subunits
Ueno, S., Tsutsui, M., Toyohira, Y., Minami, K., & Yanagihara, N. (2004) · FEBS Letters · doi:10.1016/j.febslet.2004.04.030 · Cited by 34
Low doses of ethanol and a neuroactive steroid positively interact to modulate rat GABAA receptor function
Akk, G., & Steinbach, J. H. (2003) · The Journal of Physiology · doi:10.1113/jphysiol.2002.032300 · Cited by 32
Insight into the Mechanism of Action of Neuroactive Steroids
Morris, K. D. W., & Αmin, J. (2004) · Molecular Pharmacology · doi:10.1124/mol.66.1.56 · Cited by 32
Antinociceptive properties of neurosteroids IV: pilot study demonstrating the analgesic effects of alphadolone administered orally to humans
Goodchild, C. S., Robinson, A., & Nadeson, R. (2001) · British Journal of Anaesthesia · doi:10.1093/bja/86.4.528 · Cited by 28
Inter-ictal and post-ictal circulating levels of allopregnanolone, an anticonvulsant metabolite of progesterone, in epileptic children
Grosso, S., Luisi, S. V., Mostardini, R., Farnetani, M., Cobellis, L., Morgese, G., Balestri, P., & Petraglia, F. (2003) · Epilepsy Research · doi:10.1016/s0920-1211(03)00042-1 · Cited by 18
Heterologous Regulation of GABAA Receptors: Protein Phosphorylation
Smart, T. G., Thomas, P., Brandon, N. J., & Moss, S. J. (2001) · Handbook of experimental pharmacology · doi:10.1007/978-3-642-56833-6_7 · Cited by 9
Characterization of the discriminative stimulus effects of gamma-hydroxybutyric acid as a means for unraveling the neurochemical basis of gamma-hydroxybutyric acid actions and its similarities to those of ethanol
Colombo, G., Agabio, R., Carai, M. A. M., Lobina, C., Pani, M., Reali, R., & Gessa, G. L. (2000) · Alcohol · doi:10.1016/s0741-8329(99)00087-7 · Cited by 5

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Melcangi, R. C., Magnaghi, V., Galbiati, M. & Martini, L. in Neurosteroid and Brain Function (eds Biggio, G. & Purdy, R. H.) 146–176 (Academic, San Diego, 2001).
Sundstrom-Poromaa, I. in Neurosteroid Effects in the Central Nervous System: the Role of the GABAA Receptor (ed. Smith, S. S.) 291–304 (CRC, New York, 2004).
Mtchedlishvili, Z. & Kapur, J. in Neurosteroid Effects in the Central Nervous System: the Role of the GABAA Receptor (ed. Smith, S. S.) 305–316 (CRC, New York, 2004).
Gibbs, T. T. & Farb, D. H. in Neurosteroid Effects in the Central Nervous System: the Role of the GABAA Receptor (ed. Smith S. S.) 339–358 (CRC, New York, 2004).

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Rupprecht, R., Papadopoulos, V., Rammes, G., Baghai, T. C., Fan, J., Akula, N., Groyer, G., Adams, D., & Schumacher, M. (2010) · Nature Reviews Drug Discovery · doi:10.1038/nrd3295 · Cited by 930
Structure, Function, and Modulation of GABAA Receptors
Sigel, E., & Steinmann, M. E. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.r112.386664 · Cited by 819
Endogenous neurosteroids regulate GABAA receptors through two discrete transmembrane sites
Hosie, A. M., Wilkins, M. E., da Silva, H. M. A., & Smart, T. G. (2006) · Nature · doi:10.1038/nature05324 · Cited by 752
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Miller, P. S., & Aricescu, A. R. (2014) · Nature · doi:10.1038/nature13293 · Cited by 734
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Brickley, S. G., & Módy, I. (2012) · Neuron · doi:10.1016/j.neuron.2011.12.012 · Cited by 695

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Authors: Belelli, D., & Lambert, J. J.
Affiliations: University of Dundee (GB)
Corresponding author: Lambert, Jeremy J.
ORCID: Belelli, Delia
Lambert, Jeremy J.
Venue: Nature reviews. Neuroscience
Publisher: Springer Science and Business Media LLC
Published: 2005-06-15
Volume: 6
Issue: 7
Pages: 565-575
ISSN: 1471-003X (ISSN-L)
1471-0048
DOI: 10.1038/nrn1703
OpenAlex: W2070510853
Semantic Scholar: 1e15686792dd96994a0bd1337b50f1e4448b7965
Cited by: 1,159
References: 123
Citations by year: 2026: 32 · 2025: 40 · 2024: 45 · 2023: 51 · 2022: 49 · 2021: 52 · 2020: 53 · 2019: 49 · 2018: 54 · 2017: 43 · 2016: 57 · 2015: 57 · 2014: 71 · 2013: 64 · 2012: 55
FWCI: 5.43
Type: journal article
Language: en
Open access: closed
Licence: www.springer.com/tdm (tdm)
Locations: Nature reviews. Neuroscience (publishedVersion)
PubMed (publishedVersion)
Discovery Research Portal (University of Dundee) (publishedVersion)
Topics: Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacological Receptor Mechanisms and Effects
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords: neurosteroids, GABAA receptor, pregnane steroids, non-genomic steroid action, synaptic inhibition, anxiolytic effects, anticonvulsant activity, anesthesia, psychoactive substances
MeSH terms: Animals, Brain, Humans, Models, Biological, Neural Inhibition, Synaptic Transmission, Pregnanes, Receptors, GABA-A, Antipsychotic Agents, Mood Disorders

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Neurosteroids: endogenous regulators of the GABAA receptor

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