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GABA(A) receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini‐review

GABA is a major inhibitory neurotransmitter that regulates the balance between excitatory and inhibitory circuits in the human nervous system. The GABA receptors are divided into three main subtypes, GABA(A), GABA(B), and GABA(C) (also termed GABA(A) rho) receptors. GABA(A) receptors are pentameric...

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Autores principales: Luo, Yujia, Balle, Thomas
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9538268/
https://www.ncbi.nlm.nih.gov/pubmed/36165608
http://dx.doi.org/10.1111/bcpt.13798
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author Luo, Yujia
Balle, Thomas
author_facet Luo, Yujia
Balle, Thomas
author_sort Luo, Yujia
collection PubMed
description GABA is a major inhibitory neurotransmitter that regulates the balance between excitatory and inhibitory circuits in the human nervous system. The GABA receptors are divided into three main subtypes, GABA(A), GABA(B), and GABA(C) (also termed GABA(A) rho) receptors. GABA(A) receptors are pentameric ligand‐gated ion channels widely expressed throughout the central and peripheral nervous system. The activation of GABA(A) receptors results in opening of an anion‐selective channel that mainly gates chloride ions and allows them to flow into the neuron, causing hyperpolarization of the cell membrane that dampens neural excitability. This makes GABA(A) receptors critical anaesthetic and analgesic targets for existing as well as for the development of novel drugs. In this review, we first summarize the biochemical properties of GABA(A) receptors and the clinical anaesthetics and analgesics targeting the receptors. In a forward‐looking section, we summarize the emerging role of GABAergic signalling in treatment of COVID‐19 related infections. Finally, we discuss the opportunities arising from targeting specific and unique subunit interfaces for the development of novel anaesthetics and analgesics leading to more efficient therapies.
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spelling pubmed-95382682022-10-11 GABA(A) receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini‐review Luo, Yujia Balle, Thomas Basic Clin Pharmacol Toxicol Minireviews GABA is a major inhibitory neurotransmitter that regulates the balance between excitatory and inhibitory circuits in the human nervous system. The GABA receptors are divided into three main subtypes, GABA(A), GABA(B), and GABA(C) (also termed GABA(A) rho) receptors. GABA(A) receptors are pentameric ligand‐gated ion channels widely expressed throughout the central and peripheral nervous system. The activation of GABA(A) receptors results in opening of an anion‐selective channel that mainly gates chloride ions and allows them to flow into the neuron, causing hyperpolarization of the cell membrane that dampens neural excitability. This makes GABA(A) receptors critical anaesthetic and analgesic targets for existing as well as for the development of novel drugs. In this review, we first summarize the biochemical properties of GABA(A) receptors and the clinical anaesthetics and analgesics targeting the receptors. In a forward‐looking section, we summarize the emerging role of GABAergic signalling in treatment of COVID‐19 related infections. Finally, we discuss the opportunities arising from targeting specific and unique subunit interfaces for the development of novel anaesthetics and analgesics leading to more efficient therapies. John Wiley and Sons Inc. 2022-10-05 /pmc/articles/PMC9538268/ /pubmed/36165608 http://dx.doi.org/10.1111/bcpt.13798 Text en © 2022 The Authors. Basic & Clinical Pharmacology & Toxicology published by John Wiley & Sons Ltd on behalf of Nordic Association for the Publication of BCPT (former Nordic Pharmacological Society). https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the terms of the http://creativecommons.org/licenses/by-nc-nd/4.0/ (https://creativecommons.org/licenses/by-nc-nd/4.0/) License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non‐commercial and no modifications or adaptations are made.
spellingShingle Minireviews
Luo, Yujia
Balle, Thomas
GABA(A) receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini‐review
title GABA(A) receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini‐review
title_full GABA(A) receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini‐review
title_fullStr GABA(A) receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini‐review
title_full_unstemmed GABA(A) receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini‐review
title_short GABA(A) receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini‐review
title_sort gaba(a) receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: a mini‐review
topic Minireviews
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9538268/
https://www.ncbi.nlm.nih.gov/pubmed/36165608
http://dx.doi.org/10.1111/bcpt.13798
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