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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Eccleston, R. C., & Furnham, N. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.06.27.662060
“For example, benzodiazepines act as positive allosteric modulator as they enhance the effect of GABA A , a neurotransmitter that inhibits neuronal activity [5].”
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Vanillin Modulates the Sedative Effect of Diazepam, Possibly Through GABAergic Interaction Pathways in Thiopental Sodium‐Induced Sleeping Mice
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“Each sedative drug has different levels of potency (Saari et al. 2011). α ‐1 and β ‐2 GABA A receptor subtypes apparently mediate sedative and hypnotic effects (Reynolds et al. 2003; Rudolph and Knoflach 2011).”
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Cho, J., Lee, K., Woo, S., Park, J., Jo, H., Oh, J., Kim, T. H., Wen, X., Fond, G. B., Boyer, L., et al. (2025) · Journal of Affective Disorders · doi:10.1016/j.jad.2025.120629
Anxiolytics (tranquilizers)
Vardanyan, R., & Vardanyan, G. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-33869-4.00013-2
Additional file 5 of γ-Aminobutyric acid type A receptor β1 subunit gene polymorphisms are associated with the sedative and amnesic effects of midazolam
Kosaki, Y., 西澤大輔, Hasegawa, J., et al. (2024) · Figshare · doi:10.6084/m9.figshare.27123907
Additional file 6 of γ-Aminobutyric acid type A receptor β1 subunit gene polymorphisms are associated with the sedative and amnesic effects of midazolam
Kosaki, Y., 西澤大輔, Hasegawa, J., et al. (2024) · Figshare · doi:10.6084/m9.figshare.27123910
Additional file 4 of γ-Aminobutyric acid type A receptor β1 subunit gene polymorphisms are associated with the sedative and amnesic effects of midazolam
Kosaki, Y., 西澤大輔, Hasegawa, J., et al. (2024) · Figshare · doi:10.6084/m9.figshare.27123904
Additional file 3 of γ-Aminobutyric acid type A receptor β1 subunit gene polymorphisms are associated with the sedative and amnesic effects of midazolam
Kosaki, Y., 西澤大輔, Hasegawa, J., et al. (2024) · Figshare · doi:10.6084/m9.figshare.27123901
Additional file 1 of γ-Aminobutyric acid type A receptor β1 subunit gene polymorphisms are associated with the sedative and amnesic effects of midazolam
Kosaki, Y., 西澤大輔, Hasegawa, J., et al. (2024) · Figshare · doi:10.6084/m9.figshare.27123895
Additional file 1 of MD2 contributes to the pathogenesis of perioperative neurocognitive disorder via the regulation of α5GABAA receptors in aged mice
Zuo, W., Zhao, J., Zhang, J., Fang, Z., Deng, J., Fan, Z., Guo, Y., Han, J., Hou, W., Dong, H., et al. (2021) · Figshare · doi:10.6084/m9.figshare.16633539
Additional file 7 of γ-Aminobutyric acid type A receptor β1 subunit gene polymorphisms are associated with the sedative and amnesic effects of midazolam
Kosaki, Y., 西澤大輔, Hasegawa, J., et al. (2024) · Figshare · doi:10.6084/m9.figshare.27123913
Additional file 2 of γ-Aminobutyric acid type A receptor β1 subunit gene polymorphisms are associated with the sedative and amnesic effects of midazolam
Kosaki, Y., 西澤大輔, Hasegawa, J., et al. (2024) · Figshare · doi:10.6084/m9.figshare.27123898
Anticonvulsant Potential of the Essential Oil of Croton Heliotropiifolius Kunth: In Vivo and In Silico Approach
da Cunha, M. E. S., Soares, A. L., Lima, E. M. S., et al. (2026) · ACS Omega · doi:10.1021/acsomega.5c04107
“…at the GABA A /BDZ binding site, which enhances the activity of the inhibitory neurotransmitter GABA, responsible for reducing neuronal hyperexcitability and the subsequent development of convulsive or epileptic seizures, 7 which justifies the choice of GABA A as an important molecular target.”
Fluorine-18 Radiolabeled Single-Chain Antibody Variable Fragment 1F4 Targets α1-Subunit Gamma-Aminobutyric Acid Type A Receptors in Mice
de Lucas, Á. G., Samani, N. A., Moisio, O., Kovacs, L., Savela, R., Soini, S. L., Oksanen, S., Helin, J. S., Rajander, J., Airaksinen, A. J., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c02984
A Novel Functional Ingredient Derived From a Mixture of Mulberry ( Morus alba L.) Leaves and Butterfly Pea ( Clitoria ternatea L.) Flowers Enhances Rapid Eye Movement Sleep, Cognitive Function, and Anxiolytic Behavior via GABA A Receptor‐Dependent Mechanism in Rats
Nukitram, J., Kanjanavattana, A., Rungruang, P., Yotyatthai, N., Kaewudom, P., Promkasikorn, P., Kaowsuwan, P., Zaima, N., Cheaha, D., Thukham-mee, W., et al. (2026) · Oxidative Medicine and Cellular Longevity · doi:10.1155/omcl/2305848
Wichtige Rezeptoren
Schalk, R., & Kitz, V. M. (2026) · Im OP · doi:10.1055/a-2739-6064
Classification of Excitatory and Inhibitory Neurons in Animal Data Using Machine Learning and CNN Models
Mollaei, M., Mashghdoust, A., & Khadem, A. A. (2025) · National and International Iranian Conference on Biomedical Engineering (ICBME) · doi:10.1109/icbme68496.2025.11392565
“Besides, several drugs work preferably on glutamatergic (excitatory) and GABAergic pathways [20, 21].”

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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