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Review ArticleReview Article

Regulation of GABAA Receptor Subunit Expression by Pharmacological Agents

Mikko Uusi-Oukari and Esa R. Korpi
Pharmacological Reviews March 2010, 62 (1) 97-135; DOI: https://doi.org/10.1124/pr.109.002063
Mikko Uusi-Oukari
Department of Pharmacology, Drug Development and Therapeutics, University of Turku, Turku, Finland (M.U.-O.); and Institute of Biomedicine, Pharmacology, Biomedicum Helsinki, University of Helsinki, Finland (E.R.K.)
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Esa R. Korpi
Department of Pharmacology, Drug Development and Therapeutics, University of Turku, Turku, Finland (M.U.-O.); and Institute of Biomedicine, Pharmacology, Biomedicum Helsinki, University of Helsinki, Finland (E.R.K.)
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Abstract

The γ-aminobutyric acid (GABA) type A receptor system, the main fast-acting inhibitory neurotransmitter system in the brain, is the pharmacological target for many drugs used clinically to treat, for example, anxiety disorders and epilepsy, and to induce and maintain sedation, sleep, and anesthesia. These drugs facilitate the function of pentameric GABAA receptors that exhibit widespread expression in all brain regions and large structural and pharmacological heterogeneity as a result of composition from a repertoire of 19 subunit variants. One of the main problems in clinical use of GABAA receptor agonists is the development of tolerance. Most drugs, in long-term use and during withdrawal, have been associated with important modulations of the receptor subunit expression in brain-region-specific manner, participating in the mechanisms of tolerance and dependence. In most cases, the molecular mechanisms of regulation of subunit expression are poorly known, partly as a result of neurobiological adaptation to altered neuronal function. More knowledge has been obtained on the mechanisms of GABAA receptor trafficking and cell surface expression and the processes that may contribute to tolerance, although their possible pharmacological regulation is not known. Drug development for neuropsychiatric disorders, including epilepsy, alcoholism, schizophrenia, and anxiety, has been ongoing for several years. One key step to extend drug development related to GABAA receptors is likely to require deeper understanding of the adaptational mechanisms of neurons, receptors themselves with interacting proteins, and finally receptor subunits during drug action and in neuropsychiatric disease processes.

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  • This article is available online at http://pharmrev.aspetjournals.org.

    doi:10.1124/pr.109.002063.

  • © 2010 by The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 62 (1)
Pharmacological Reviews
Vol. 62, Issue 1
1 Mar 2010
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Review ArticleReview Article

Regulation of GABAA Receptor Subunit Expression by Pharmacological Agents

Mikko Uusi-Oukari and Esa R. Korpi
Pharmacological Reviews March 1, 2010, 62 (1) 97-135; DOI: https://doi.org/10.1124/pr.109.002063

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Review ArticleReview Article

Regulation of GABAA Receptor Subunit Expression by Pharmacological Agents

Mikko Uusi-Oukari and Esa R. Korpi
Pharmacological Reviews March 1, 2010, 62 (1) 97-135; DOI: https://doi.org/10.1124/pr.109.002063
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  • Article
    • Abstract
    • I. Introduction
    • II. Expression of GABAA Receptors
    • III. Regulation of GABAA Receptor Expression By Pharmacological Agents
    • IV. Novel Opportunities to Target the GABAA Receptor System with Therapeutics
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