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Glossary GABA receptor

protein in the brain that inhibits neuronal activity

A GABA receptor is a protein in the brain that responds to the neurotransmitter gamma-aminobutyric acid (GABA). It plays a crucial role in reducing neuronal excitability throughout the nervous system. There are two main types: GABA(A) receptors, which are ion channels that allow chloride ions to enter the neuron, leading to inhibition, and GABA(B) receptors, which are G-protein-coupled receptors that influence neuronal activity through secondary messenger systems.

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Progesterone-Independent Neurosteroid Regulation of Alpha2-GABA-A Receptors in the Hippocampus Subfields

research PR-independent neurosteroid regulation of α2-GABA-A receptors in the hippocampus subfields

14 citations , March 2017 in “Brain research”

This study suggests that ovarian cycle-related progesterone and neurosteroids regulate α2-subunit expression of GABA-A receptors in the hippocampus through a pathway independent of progesterone receptors, potentially affecting brain conditions linked to the menstrual cycle.

research Ovarian Cycle‐Related Neurosteroid Regulation of GABA‐A Receptor Subunit Plasticity in the Hippocampus Subfields

1 citations , April 2011 in “The FASEB Journal”

This study suggests that the regulation of GABA‐A δ subunit expression by ovarian progesterone-derived neurosteroids may influence seizure susceptibility in catamenial epilepsy.

research Effect of Neurosteroid Withdrawal on Hippocampal GABA‐A Receptor α4‐Subunit Expression in Female Mice

March 2008 in “The FASEB Journal”

This study found that neurosteroid withdrawal significantly increased hippocampal GABA-A receptor α4 subunit expression in female mice, confirming an association between neurosteroid withdrawal and altered receptor expression.

research Catamenial-like seizure exacerbation in mice with targeted ablation of extrasynaptic δGABA-a receptors in the brain

12 citations , February 2017 in “Journal of neuroscience research”

This study suggests that extrasynaptic δGABA-A receptors may have a protective role in modulating the severity of catamenial-like seizures by influencing neurosteroid and benzodiazepine responses in mice.

Realizing the Therapeutic Potential of Neuroactive Steroid Modulators of the GABAA Receptor

research Realising the therapeutic potential of neuroactive steroid modulators of the GABAA receptor

40 citations , December 2019 in “Neurobiology of Stress”

This review focuses on neuroactive steroids' influence on GABA-ergic signaling and discusses challenges in developing them for various therapeutic uses, citing recent excitement from FDA approval of allopregnanolone for postpartum depression but reporting no new results.

research Effects of Subchronic Finasteride Treatment and Withdrawal on Neuroactive Steroid Levels and Their Receptors in the Male Rat Brain

33 citations , December 2015 in “Neuroendocrinology”

This study found that subchronic finasteride treatment in male rats altered neuroactive steroid levels and steroid receptor expression in the brain, with some changes persisting after drug withdrawal.

research Changes in expression of the δ subunit of the GABA_Areceptor and in receptor function induced by progesterone exposure and withdrawal

25 citations , July 2006 in “Journal of Neurochemistry”

This study found that chronic exposure to and withdrawal of progesterone influenced the expression and function of GABA A receptors in rat hippocampal neurons through its metabolite 3α,5α‐THPROG.

research Allopregnanolone is required for prepulse inhibition deficits induced by D1 dopamine receptor activation

12 citations , June 2019 in “Psychoneuroendocrinology”

This study found that in rodent models, the ability of D1 dopamine receptor activation to impair sensory gating is facilitated by 5α-reductase type 1, which produces allopregnanolone.

research Aqueous extract of Asiasari radix inhibits formalin-induced hyperalgesia via NMDA receptors

17 citations , February 2009 in “Journal of Ethnopharmacology”

This study found that Asiasari radix extract may reduce hyperalgesia in mice by modulating NMDA and GABAA receptor activities without affecting cyclooxygenase activity.

Joint Public Review: Touch Receptor End-Organ Innervation and Function Require Sensory Neuron Expression of the Transcription Factor Meis2

research Joint Public Review: Touch receptor end-organ innervation and function require sensory neuron expression of the transcription factor Meis2

February 2024

This study found that the transcription factor Meis2 is crucial for the maturation and innervation of sensory neurons responsible for light touch in mice, with its absence leading to reduced touch sensitivity.

research Social isolation alters GABAA receptors plasticity and function: effect of voluntary consumption of ethanol

April 2008 in “Annals of General Psychiatry”

This study found that social isolation in rats enhanced the effects of ethanol on certain brain steroids, increased GABAA receptor subunits, and amplified ethanol's inhibitory effects on seizures.

research Stress-Induced Deoxycorticosterone-Derived Neurosteroids Modulate GABA_AReceptor Function and Seizure Susceptibility

269 citations , May 2002 in “Journal of Neuroscience”

This study observed that acute stress in rats increased neurosteroid levels linked to enhanced GABA(A) receptor function, raising seizure thresholds, while similar effects were seen in mice with deoxycorticosterone administration.

research Neurosteroidogenesis Is Required for the Physiological Response to Stress: Role of Neurosteroid-Sensitive GABA_AReceptors

248 citations , December 2011 in “Journal of Neuroscience”

This study demonstrated that stress-derived neurosteroid THDOC shifts from inhibiting to activating the HPA axis under stress, presenting potential therapeutic targets for stress-related disorders.

research Neurosteroid Synthesis-Mediated Regulation of GABA_AReceptors: Relevance to the Ovarian Cycle and Stress

238 citations , February 2007 in “Journal of Neuroscience”

This study found that neurosteroids can reorganize GABA A receptors in mice, mimicking ovarian cycle changes, with the process being mediated by neurosteroid levels rather than direct hormone receptor activation.

Production of 5α-Reduced Neurosteroids Is Developmentally Regulated and Shapes GABA A Miniature IPSCs in Lamina II of the Spinal Cord

research Production of 5α-Reduced Neurosteroids Is Developmentally Regulated and Shapes GABA_AMiniature IPSCs in Lamina II of the Spinal Cord

88 citations , January 2004 in “Journal of Neuroscience”

This study found that inhibiting neurosteroidogenesis affected GABA A receptor-mediated synaptic inhibition in immature rats but not in adults, suggesting age-dependent modulation of synaptic strength in the spinal dorsal horn.

research Mechanism of progesterone neuroprotection of rat cerebellar Purkinje cells following oxygen–glucose deprivation

83 citations , November 2006 in “European Journal of Neuroscience”

This study found that progesterone protects rat Purkinje cells during oxygen-glucose deprivation by activating GABA A receptors through its metabolite, allopregnanolone.

research Social isolation‐induced increase in α₄and δ subunit gene expression is associated with a greater efficacy of ethanol on steroidogenesis and GABA_Areceptor function

60 citations , May 2006 in “Journal of Neurochemistry”

This study found that social isolation in rats enhanced ethanol's effects on brain steroidogenesis and GABA A receptor function, altering related behavior more than in non-isolated rats.

research GABAergic neurosteroids mediate the effects of ethanol on long‐term potentiation in rat hippocampal slices

48 citations , September 2007 in “European Journal of Neuroscience”

This study found that ethanol's ability to block long-term potentiation in rat hippocampal slices is influenced by neurosteroids that enhance GABA A receptor activity.

research Enhanced remyelination during late pregnancy: involvement of the GABAergic system

30 citations , May 2019 in “Scientific Reports”

This study found enhanced remyelination in the corpus callosum of late pregnant rats compared to virgin and postpartum rats, suggesting a pregnancy-associated promyelinating effect mediated, in part, by the GABA A receptor system.

research Roles of Type 10 17beta-Hydroxysteroid Dehydrogenase in Intracrinology and Metabolism of Isoleucine and Fatty Acids

26 citations , March 2006 in “Endocrine, metabolic & immune disorders. Drug targets”

This article discusses the functions of the enzyme 17beta-HSD10, including its role in steroid metabolism and potential links to Alzheimer's disease, but reports no new experimental findings.

research Relating neurosteroid modulation of inhibitory neurotransmission to behaviour

18 citations , September 2021 in “Journal of Neuroendocrinology”

This review discusses how neurosteroids acting on GABAA receptors may influence behavior and explores the potential for developing selective modulators for treating psychiatric disorders, but reports no new clinical results.

research Inhibitory respiratory responses to progesterone and allopregnanolone in newborn rats chronically treated with caffeine

17 citations , October 2015 in “The Journal of Physiology”

This study found that in newborn rats treated with caffeine, progesterone increased apnoea frequency by inhibiting breathing, suggesting it may not be suitable for preterm neonates without addressing allopregnanolone's effects.

research Local Changes in Neurosteroid Levels in the Substantia Nigra Reticulata and the Ventral Tegmental Area Alter Chronic Ethanol Withdrawal Severity in Male Withdrawal Seizure‐Prone Mice

11 citations , December 2012 in “Alcoholism Clinical and Experimental Research”

This study found that in Withdrawal Seizure-Prone mice, ethanol withdrawal decreased the sensitivity of GABA A receptors to GABAergic neurosteroids in certain areas of the brain.

Antidepressant-Like Effect of Fluoxetine May Depend on Translocator Protein Activity and Pretest Session Duration in Forced Swimming Test in Mice

research Antidepressant-like effect of fluoxetine may depend on translocator protein activity and pretest session duration in forced swimming test in mice

7 citations , October 2017 in “Behavioural Pharmacology”

This study found that the antidepressant-like effect of fluoxetine in mice was only observed when a 5-minute pretest session was conducted, and this effect was blocked by the TSPO antagonist PK11195.

Brain Allopregnanolone Induces Marked Scratching Behavior in Diet-Induced Atopic Dermatitis Mouse Model

research Brain allopregnanolone induces marked scratching behaviour in diet-induced atopic dermatitis mouse model

6 citations , February 2019 in “Scientific reports”

This study demonstrated that allopregnanolone administration caused significant scratching in atopic dermatitis mice, and ethanol-induced scratching may be linked to increased brain allopregnanolone levels.

research Synthesis and Actions of 5α-Reduced Metabolites of Testosterone in the Nervous System

1 citations , December 2021 in “Androgens”

This review discusses the effects of neuroactive testosterone metabolites on CNS functions and suggests their potential as therapeutic options for neurological disorders, but reports no new clinical results.

research Neuroactive Steroids: Functions, Mechanisms of Action and Physiologic Relevance

November 2003 in “Journal of Neurochemistry”

This study suggests that the neurosteroid allopregnanolone may play a crucial role in how ethanol affects neurons related to alcohol addiction vulnerability.

research Neurosteroids as Endogenous Regulators of Seizure Susceptibility

September 2002 in “Epiliepsy currents/Epilepsy currents”

This study found that deoxycorticosterone-derived neurosteroids modulate GABA A receptor function and may influence stress-induced changes in seizure susceptibility by elevating seizure thresholds in animal models.

research Unraveling the Complex: Changes in Secondary Science Preservice Teachers' Assessment Expertise

January 2012 in “ProQuest LLC eBooks”

This study found that neonatal finasteride and allopregnanolone alterations were associated with anxiety-related behavior changes and impaired aversive learning in adult rats, potentially due to GABA(A) receptor system changes in the hippocampus.

research Neurosteroids, neuroactive steroids, and symptoms of affective disorders

82 citations , August 2006 in “Pharmacology, Biochemistry and Behavior”

This review proposes focusing on relationships between neuroactive steroids and psychiatric disorder symptoms, rather than relying on traditional disorder classifications, and reports no new clinical findings.