ArticleThe Journal of physiology2010
Distinct activities of GABA agonists at synaptic- and extrasynaptic-type GABAA receptors.
Article in The Journal of physiology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 99 papers.
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99 citing papers in PubMed, 158 citations in OpenAlex.
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- A Non-Classical Neuroactive Steroid Exhibiting Potent, Efficacious GABAbioRxiv : the preprint server for biology · 2026Article
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- Properties of Acute Activation and Inhibition of the β3 Homomeric GABAACS chemical neuroscience · 2025Article
- Chronic ethanol exposure in mice evokes pre- and postsynaptic deficits in GABAergic transmission in ventral tegmental area GABA neurons.British journal of pharmacology · 2025Article
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- Acidic pH reduces agonist efficacy and responses to synaptic-like glycine applications in zebrafish α1 and rat α1β recombinant glycine receptors.The Journal of physiology · 2022Article
- Optimization of Neurite Tracing and Further Characterization of Human Monocyte-Derived-Neuronal-like Cells.Brain sciences · 2021Article
- Structural determinants and regulation of spontaneous activity in GABANature communications · 2021Article
- Mechanisms of GABAergic and cholinergic neurotransmission in auditory thalamus: Impact of aging.Hearing research · 2021Review
- Pharmacological and Biophysical Characteristics of Picrotoxin-Resistant, δSubunit-Containing GABAFrontiers in synaptic neuroscience · 2021Article
- The desensitization pathway of GABANature communications · 2020Article
- Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABAScientific reports · 2020Article
- Social experience and sex-dependent regulation of aggression in the lateral septum by extrasynaptic δGABAPsychopharmacology · 2020Article
- Expression and Function of GABA Receptors in Myelinating Cells.Frontiers in cellular neuroscience · 2020Article
- Steady-state activation of the high-affinity isoform of the α4β2δ GABAScientific reports · 2019Article
39 more citing papers are in PubMed but not listed here.
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
The activation characteristics of synaptic and extrasynaptic GABA(A) receptors are important for shaping the profile of phasic and tonic inhibition in the central nervous system, which will critically impact on the activity of neuronal networks. Here, we study in isolation the activity of three agonists, GABA, muscimol and 4,5,6,7-tetrahydoisoxazolo[5,4-c]pyridin-3(2H)-one (THIP), to further understand the activation profiles of alpha 1 beta 3 gamma 2, alpha 4 beta 3 gamma 2 and alpha 4 beta 3 delta receptors that typify synaptic- and extrasynaptic-type receptors expressed in the hippocampus and thalamus. The agonists display an order of potency that is invariant between the three receptors, which is reliant mostly on the agonist dissociation constant. At delta subunit-containing extrasynaptic-type GABA(A) receptors, both THIP and muscimol additionally exhibited, to different degrees, superagonist behaviour. By comparing whole-cell and single channel currents induced by the agonists, we provide a molecular explanation for their different activation profiles. For THIP at high concentrations, the unusual superagonist behaviour on alpha 4 beta 3 delta receptors is a consequence of its ability to increase the duration of longer channel openings and their frequency, resulting in longer burst durations. By contrast, for muscimol, moderate superagonist behaviour was caused by reduced desensitisation of the extrasynaptic-type receptors. The ability to specifically increase the efficacy of receptor activation, by selected exogenous agonists over that obtained with the natural transmitter, may prove to be of therapeutic benefit under circumstances when synaptic inhibition is compromised or dysfunctional.
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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.