ArticleBritish journal of pharmacology2012
Characteristics of concatemeric GABA(A) receptors containing α4/δ subunits expressed in Xenopus oocytes.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
30 citing papers in PubMed, 48 citations in OpenAlex.
- AlphaFold-Multimer modelling of linked nAChR subunits challenges concatemer design assumptions.Scientific reports · 2026Article
- Peripheral cyclical expression of GABA-A receptor subunit genes and menstrual cycle affective change: a dimensional, transdiagnostic study.Translational psychiatry · 2025Article
- New directions in neurosteroid therapeutics in neuropsychiatry.Neuroscience and biobehavioral reviews · 2025Review
- Gain-of-function variants in GABRD reveal a novel pathway for neurodevelopmental disorders and epilepsy.Brain : a journal of neurology · 2022Article
- Neurobehavioural complications of sleep deprivation: Shedding light on the emerging role of neuroactive steroids.Journal of neuroendocrinology · 2020Review
- GABAFrontiers in cellular neuroscience · 2020Article
- Lack of Neurosteroid Selectivity at δ vs. γ2-Containing GABAFrontiers in molecular neuroscience · 2020Article
- Neurosteroids as novel antidepressants and anxiolytics: GABA-A receptors and beyond.Neurobiology of stress · 2019Article
- Concatenated γ-aminobutyric acid type A receptors revisited: Finding order in chaos.The Journal of general physiology · 2019Article
- Chemogenetic Isolation Reveals Synaptic Contribution of δ GABAThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2018Article
- Comparison of αβδ and αβγ GABAPharmacological research · 2018Review
- Concatenated nicotinic acetylcholine receptors: A gift or a curse?The Journal of general physiology · 2018Article
- Biomarkers for PTSD at the Interface of the Endocannabinoid and Neurosteroid Axis.Frontiers in neuroscience · 2018Article
- Combining Mutations and Electrophysiology to Map Anesthetic Sites on Ligand-Gated Ion Channels.Methods in enzymology · 2018Review
- Neurosteroid biosynthesis down-regulation and changes in GABABritish journal of pharmacology · 2017Review
- Article
- Toward Understanding Functional Properties and Subunit Arrangement of α4β2δ γ-Aminobutyric Acid, Type A (GABAA) Receptors.The Journal of biological chemistry · 2016Article
- Neurosteroid Structure-Activity Relationships for Functional Activation of Extrasynaptic δGABA(A) Receptors.The Journal of pharmacology and experimental therapeutics · 2016Article
- Etomidate uniquely modulates the desensitization of recombinant α1β3δ GABA(A) receptors.Neuroscience · 2015Article
- Probing α4βδ GABAA receptor heterogeneity: differential regional effects of a functionally selective α4β1δ/α4β3δ receptor agonist on tonic and phasic inhibition in rat brain.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Article
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 2 countries.
Funding
Abstract
background and purposeGABA(A) receptors mediate both synaptic and extrasynaptic actions of GABA. In several neuronal populations, α4 and δ subunits are key components of extrasynaptic GABA(A) receptors that strongly influence neuronal excitability and could mediate the effects of neuroactive agents including neurosteroids and ethanol. However, these receptors can be difficult to study in native cells and recombinant δ subunits can be difficult to express in heterologous systems. EXPERIMENTAL APPROACH: We engineered concatemeric (fused) subunits to ensure δ and α4 subunit expression. We tested the pharmacology of the concatemeric receptors, compared with a common synaptic-like receptor subunit combination (α1 +β2 +γ2L), and with free-subunit α4/δ receptors, expressed in Xenopus oocytes. KEY
resultsδ-β2 -α4 +β2-α4 cRNA co-injected into Xenopus oocytes resulted in GABA-gated currents with the expected pharmacological properties of α4/δ-containing receptors. Criteria included sensitivity to agonists of different efficacy, sensitivity to the allosteric activator pentobarbital, and modulation of agonist responses by DS2 (4-chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridine-3-yl benzamide; a δ-selective positive modulator), furosemide, and Zn(2+) . We used the concatemers to examine neurosteroid sensitivity of extrasynaptic-like, δ-containing receptors. We found no qualitative differences between extrasynaptic-like receptors and synaptic-like receptors in the actions of either negative or positive neurosteroid modulators of receptor function. Quantitative differences were explained by the partial agonist effects of the natural agonist GABA and by a mildly increased sensitivity to low steroid concentrations. CONCLUSIONS AND IMPLICATIONS: The neurosteroid structure-activity profile for α4/δ-containing extrasynaptic receptors is unlikely to differ from that of synaptic-like receptors such as α1/β2/γ2-containing receptors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.