ArticleThe Journal of physiology2004
Activation of GABA(A) receptors containing the alpha4 subunit by GABA and pentobarbital.
Article in The Journal of physiology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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Who cites it
36 citing papers in PubMed, 58 citations in OpenAlex.
- Pharmacological Analysis of GABAInternational journal of molecular sciences · 2023Article
- Steady-state activation of the high-affinity isoform of the α4β2δ GABAScientific reports · 2019Article
- Chemogenetic Isolation Reveals Synaptic Contribution of δ GABAThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2018Article
- GABA beyond the synapse: defining the subtype-specific pharmacodynamics of non-synaptic GABAThe Journal of physiology · 2018Article
- Comparison of αβδ and αβγ GABAPharmacological research · 2018Review
- Article
- The dual modulatory effects of efavirenz on GABANeuropharmacology · 2017Article
- The Influence of Regional Distribution and Pharmacologic Specificity of GABAFrontiers in systems neuroscience · 2017Review
- Article
- Contrasting actions of a convulsant barbiturate and its anticonvulsant enantiomer on the α1 β3 γ2L GABAA receptor account for their in vivo effects.The Journal of physiology · 2015Article
- Assessment of subunit-dependent direct gating and allosteric modulatory effects of carisoprodol at GABA(A) receptors.Neuropharmacology · 2015Article
- γ-aminobutyric acid type A α4, β2, and δ subunits assemble to produce more than one functionally distinct receptor type.Molecular pharmacology · 2014Article
- Mutations in the main cytoplasmic loop of the GABA(A) receptor α4 and δ subunits have opposite effects on surface expression.Molecular pharmacology · 2014Article
- Energetic contributions to channel gating of residues in the muscle nicotinic receptor β1 subunit.PloS one · 2013Article
- α4βδ GABAA receptors and tonic inhibitory current during adolescence: effects on mood and synaptic plasticity.Frontiers in neural circuits · 2013Review
- Characteristics of concatemeric GABA(A) receptors containing α4/δ subunits expressed in Xenopus oocytes.British journal of pharmacology · 2012Article
- Beyond the HPA Axis: Progesterone-Derived Neuroactive Steroids in Human Stress and Emotion.Frontiers in endocrinology · 2011Article
- Barbiturates require the N terminus and first transmembrane domain of the delta subunit for enhancement of alpha1beta3delta GABAA receptor currents.The Journal of biological chemistry · 2010Article
- Distinct activities of GABA agonists at synaptic- and extrasynaptic-type GABAA receptors.The Journal of physiology · 2010Article
- Kinetic and structural determinants for GABA-A receptor potentiation by neuroactive steroids.Current neuropharmacology · 2010Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
The activation properties of GABA(A) receptors containing alpha4beta2gamma2 and alpha4beta2delta subunits were examined in the presence of GABA or pentobarbital. The receptors were expressed transiently in HEK 293 cells, and the electrophysiological experiments were carried out using cell-attached single-channel patch clamp or whole-cell macroscopic recordings. The data show that GABA is a stronger activator of alpha4beta2gamma2 receptors than alpha4beta2delta receptors. Single-channel clusters were recorded from alpha4beta2gamma2 receptors in the presence of 10-5000 microm GABA. The maximal intracluster open probability was 0.35, with a half-maximal response elicited by 32 microm GABA. Simultaneous kinetic analysis of single-channel currents obtained at various GABA concentrations yields a channel opening rate constant of 250 s(-1), and a K(D) of 20 microm. In contrast, only isolated openings were observed in the presence of GABA for the alpha4beta2delta receptor. Pentobarbital was a strong activator of both alpha4beta2gamma2 and alpha4beta2delta receptors. The maximal cluster open probability, recorded in the presence of 100 microm pentobarbital, was 0.7. At higher pentobarbital concentrations, the cluster open probability was reduced, probably due to channel block. The results from single-channel experiments were confirmed by macroscopic recordings from HEK cells in the presence of GABA or pentobarbital.
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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.