Structure and function of GABA(C) receptors: a comparison of native versus recombinant receptors.
- Authors
- Zhang, D; Pan, Z H; Awobuluyi, M; Lipton, S A
- Year
- 2001
- Journal
- Trends in pharmacological sciences
- PMID
- 11239575
- DOI
- 10.1016/s0165-6147(00)01625-4
In less than a decade our knowledge of the GABA(C) receptor, a new type of Cl(-)-permeable ionotropic GABA receptor, has greatly increased based on studies of both native and recombinant receptors. Careful comparison of properties of native and recombinant receptors has provided compelling evidence that GABA receptor rho-subunits are the major molecular components of GABA(C) receptors. Three distinct rho-subunits from various species have been cloned and the pattern of their expression in the retina, as well as in various brain regions, has been established. The pharmacological profile of GABA(C) receptors has been refined and more specific drugs have been developed. Molecular determinants that underlie functional properties of the receptors have been assigned to specific amino acid residues in rho-subunits. This information has helped determine the subunit composition of native receptors, as well as the molecular basis underlying subtle variations among GABA(C) receptors in different species. Finally, GABA(C) receptors play a unique functional role in retinal signal processing via three mechanisms: (1) slow activation; (2) segregation from other inhibitory receptors; and (3) contribution to multi-neuronal pathways.
No figures extracted from this document.
No chunks β full text not yet ingested.
No entities extracted from this document yet.
No uploaded files.
No citations found.
In this knowledge base
| Title | Year | PMID |
|---|---|---|
| GABRR1 and GABRR2, encoding the GABA-A receptor subunits rho1 and rho2, are associated with alcohol dependence. | 2010 | 19536785 |
External
| Title | Authors | Journal | Year | Link |
|---|---|---|---|---|
| Cardiac endogenous transmitter system: molecular features, functions, and clinical implications. | Xie D et al. | β | 2026 | β |
| The involvement of GABA-rho receptors in regulating ethanol-induced elevation of dopamine, glycine and taurine within the nucleus accumbens of Wistar rats. | Cadeddu D et al. | β | 2025 | β |
| Neuromodulator regulation and emotions: insights from the crosstalk of cell signaling. | Tsuboi D et al. | β | 2024 | β |
| Involvement of the GABAergic system in PTSD and its therapeutic significance. | Huang J et al. | β | 2023 | β |
| Ξ<sup>8</sup>-THC Induces Up-Regulation of Glutamatergic Pathway Genes in Differentiated SH-SY5Y: A Transcriptomic Study. | Anchesi I et al. | β | 2023 | β |
| Electrophysiology of ionotropic GABA receptors. | Sallard E et al. | β | 2021 | β |
| GABA<sub>A</sub> receptors in GtoPdb v.2021.3. | Belelli D et al. | β | 2021 | β |
| How do stupendous cannabinoids modulate memory processing via affecting neurotransmitter systems? | Vaseghi S et al. | β | 2021 | β |
| Influence of glutamate and GABA transport on brain excitatory/inhibitory balance. | Sears SM et al. | β | 2021 | β |
| Modulating Neuro-Immune-Induced Macrophage Polarization With Topiramate Attenuates Experimental Abdominal Aortic Aneurysm. | Chen X et al. | β | 2020 | β |
| Effects of dietary gamma-aminobutyric acid supplementation on the intestinal functions in weaning piglets. | Chen S et al. | β | 2019 | β |
| Directed, Palladium(II)-Catalyzed Intermolecular Aminohydroxylation of Alkenes Using a Mild Oxidation System. | Zeng T et al. | β | 2018 | β |
| Diversity of structure and function of GABA<sub>B</sub> receptors: a complexity of GABA<sub>B</sub>-mediated signaling. | Terunuma M | β | 2018 | β |
| Full rescue of an inactive olfactory receptor mutant by elimination of an allosteric ligand-gating site. | Sharma K et al. | β | 2018 | β |
| Negative modulation of the GABA<sub>A</sub> Ο1 receptor function by l-cysteine. | BeltrΓ‘n GonzΓ‘lez AN et al. | β | 2018 | β |
| GABA-Ο receptors: distinctive functions and molecular pharmacology. | Naffaa MM et al. | β | 2017 | β |
| Gene-based interaction analysis shows GABAergic genes interacting with parenting in adolescent depressive symptoms. | Van Assche E et al. | β | 2017 | β |
| Genetic Polymorphism of GABRR2 Modulates Individuals' General Cognitive Ability in Healthy Chinese Han People. | Ma Z et al. | β | 2017 | β |
| Investigating the Role of Loop C Hydrophilic Residue 'T244' in the Binding Site of Ο1 GABAC Receptors via Site Mutation and Partial Agonism. | Naffaa MM et al. | β | 2016 | β |
| Sodium and water intake are not affected by GABAC receptor activation in the lateral parabrachial nucleus of sodium-depleted rats. | Domingos-Souza G et al. | β | 2016 | β |
| Comparison of templates for homology model of Ο1 GABAC receptors: More insights to the orthosteric binding site's structure and functionality. | Naffaa MM et al. | β | 2015 | β |
| An intracellular redox sensor for reactive oxygen species at the M3-M4 linker of GABAA Ο1 receptors. | BeltrΓ‘n GonzΓ‘lez AN et al. | β | 2014 | β |
| Benzodiazepine modulation of homomeric GABAAΟ1 receptors: differential effects of diazepam and 4'-chlorodiazepam. | BeltrΓ‘n GonzΓ‘lez AN et al. | β | 2014 | β |
| Effects of essential amino acid deficiency: down-regulation of KCC2 and the GABAA receptor; disinhibition in the anterior piriform cortex. | Sharp JW et al. | β | 2013 | β |
| GABAergic synaptic inputs of locus coeruleus neurons in wild-type and Mecp2-null mice. | Jin X et al. | β | 2013 | β |
| Inhibitory Effects of Ginsenoside Metabolites, Compound K and Protopanaxatriol, on GABAC Receptor-Mediated Ion Currents. | Lee BH et al. | β | 2013 | β |
| Quercetin antagonism of GABAAΟβ receptors is prevented by ascorbic acid through a redox-independent mechanism. | Calero CI et al. | β | 2013 | β |
| The Concise Guide to PHARMACOLOGY 2013/14: ligand-gated ion channels. | Alexander SP et al. | β | 2013 | β |
| Ξ³-Aminobutyrate- and Glutamate-gated Chloride Channels as Targets of Insecticides | Ozoe Y | β | 2013 | β |
| Computational prediction of MicroRNAs targeting GABA receptors and experimental verification of miR-181, miR-216 and miR-203 targets in GABA-A receptor. | Zhao C et al. | β | 2012 | β |
| Histamine-gated ion channels in mammals? | Fleck MW et al. | β | 2012 | β |
| Nitric oxide potentiation of the homomeric Ο1 GABA(C) receptor function. | Gasulla J et al. | β | 2012 | β |
| Pharmacotherapy of insomnia. | Ioachimescu OC et al. | β | 2012 | β |
| Structural basis for selective GABA binding in bacterial pathogens. | Planamente S et al. | β | 2012 | β |
| Allosteric modulation of retinal GABA receptors by ascorbic acid. | Calero CI et al. | β | 2011 | β |
| Cloning and characterization of GABAA Ξ± subunits and GABAB subunits in Xenopus laevis during development. | Kaeser GE et al. | β | 2011 | β |
| Insights into the biophysical properties of GABA(A) ion channels: modulation of ion permeation by drugs and protein interactions. | Tierney ML | β | 2011 | β |
| Medicinal chemistry of Ο GABAC receptors. | Ng CK et al. | β | 2011 | β |
| Neurovascular interaction and the pathophysiology of diabetic retinopathy. | Qian H et al. | β | 2011 | β |
| Pharmacological analysis of the activation and receptor properties of the tonic GABA(C)R current in retinal bipolar cell terminals. | Jones SM et al. | β | 2011 | β |
| Aberrant regulation of alternative pre-mRNA splicing in schizophrenia. | Morikawa T et al. | β | 2010 | β |
| An Update on GABAΟ Receptors. | MartΓnez-Delgado G et al. | β | 2010 | β |
| GABAa and GABAc receptor-mediated modulation of responses to color stimuli: electroretinographic study in the turtle Emys orbicularis. | Kupenova P et al. | β | 2010 | β |
| GABRR1 and GABRR2, encoding the GABA-A receptor subunits rho1 and rho2, are associated with alcohol dependence. | Xuei X et al. | β | 2010 | β |
| Chloride accumulation drives volume dynamics underlying cell proliferation and migration. | Habela CW et al. | β | 2009 | β |
| Structural model of rho1 GABAC receptor based on evolutionary analysis: Testing of predicted protein-protein interactions involved in receptor assembly and function. | Adamian L et al. | β | 2009 | β |
| Cyclothiazide: a subunit-specific inhibitor of GABAC receptors. | Xie A et al. | β | 2008 | β |
| Electrophysiological evidence of GABAA and GABAC receptors on zebrafish retinal bipolar cells. | Connaughton VP et al. | β | 2008 | β |
| GABAa and GABAc receptor mediated influences on the intensity-response functions of the b- and d-wave in the frog ERG. | Kupenova P et al. | β | 2008 | β |
| GABAC-receptor stimulation activates cAMP-dependent protein kinase via A-kinase anchoring protein 220. | Yang L et al. | β | 2008 | β |
| Inhibitory interaction between P2X4 and GABA(C) rho1 receptors. | Xia R et al. | β | 2008 | β |
| Redox modulation of homomeric rho1 GABA receptors. | Calero CI et al. | β | 2008 | β |
| Structural determinants for antagonist pharmacology that distinguish the rho1 GABAC receptor from GABAA receptors. | Zhang J et al. | β | 2008 | β |
| 5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists. | Madsen C et al. | β | 2007 | β |
| A new inorganic photolabile protecting group for highly efficient visible light GABA uncaging. | Zayat L et al. | β | 2007 | β |
| A single amino acid in the second transmembrane domain of GABA rho receptors regulates channel conductance. | Zhu Y et al. | β | 2007 | β |
| Colocalization of synaptic GABA(C)-receptors with GABA (A)-receptors and glycine-receptors in the rodent central nervous system. | Frazao R et al. | β | 2007 | β |
| GABAA receptor subtypes: the "one glass of wine" receptors. | Olsen RW et al. | β | 2007 | β |
| Neuroactive steroids and human recombinant rho1 GABAC receptors. | Li W et al. | β | 2007 | β |
| Phosphonic acid analogs of GABA through reductive dealkylation of phosphonic diesters with lithium trialkylborohydrides. | Chowdhury S et al. | β | 2007 | β |
| Streptozotocin-induced diabetes modulates GABA receptor activity of rat retinal neurons. | Ramsey DJ et al. | β | 2007 | β |
| The cellular, molecular and ionic basis of GABA(A) receptor signalling. | Farrant M et al. | β | 2007 | β |
| Tonically active GABAA receptors in hippocampal pyramidal neurons exhibit constitutive GABA-independent gating. | McCartney MR et al. | β | 2007 | β |
| Evidence for a functional role of GABA receptors in the rat mature hippocampus. | Alakuijala A et al. | β | 2006 | β |
| Evidence that GABA rho subunits contribute to functional ionotropic GABA receptors in mouse cerebellar Purkinje cells. | Harvey VL et al. | β | 2006 | β |
| High pH accelerates GABA deactivation on perch-rho1B receptors. | Qian H et al. | β | 2006 | β |
| Mixed antagonistic effects of bilobalide at rho1 GABAC receptor. | Huang SH et al. | β | 2006 | β |
| Random assembly of GABA rho1 and rho2 subunits in the formation of heteromeric GABA(C) receptors. | Pan Y et al. | β | 2006 | β |
| A cation-pi binding interaction with a tyrosine in the binding site of the GABAC receptor. | Lummis SC et al. | β | 2005 | β |
| A yellow fluorescent protein-based assay for high-throughput screening of glycine and GABAA receptor chloride channels. | Kruger W et al. | β | 2005 | β |
| Functional characterization of rat rho2 subunits expressed in HEK 293 cells. | Alakuijala A et al. | β | 2005 | β |
| GABA receptor rho subunit expression in the developing rat brain. | Alakuijala A et al. | β | 2005 | β |
| Interactions between rho and gamma2 subunits of the GABA receptor. | Pan Y et al. | β | 2005 | β |
| Pharmacology of GABAC receptors: responses to agonists and antagonists distinguish A- and B-subtypes of homomeric rho receptors expressed in Xenopus oocytes. | Pan Y et al. | β | 2005 | β |
| The GABA rho1 subunit interacts with a cellular retinoic acid binding protein in mammalian retina. | Song XQ et al. | β | 2005 | β |
| Evidence for inhibition mediated by coassembly of GABAA and GABAC receptor subunits in native central neurons. | Milligan CJ et al. | β | 2004 | β |
| Sites of positive allosteric modulation by neurosteroids on ionotropic gamma-aminobutyric acid receptor subunits. | Ueno S et al. | β | 2004 | β |
| Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptor. | Goutman JD et al. | β | 2004 | β |
| Aza-THIP and related analogues of THIP as GABA C antagonists. | Krehan D et al. | β | 2003 | β |
| Flavonoid modulation of ionic currents mediated by GABA(A) and GABA(C) receptors. | Goutman JD et al. | β | 2003 | β |
| Function of gamma-aminobutyric acid receptor/channel rho 1 subunits in spinal cord. | Zheng W et al. | β | 2003 | β |
| GABAC receptor agonist suppressed ammonia-induced apoptosis in cultured rat hippocampal neurons by restoring phosphorylated BAD level. | Yang L et al. | β | 2003 | β |
| Glycine receptors and glycinergic synaptic input at the axon terminals of mammalian retinal rod bipolar cells. | Cui J et al. | β | 2003 | β |
| Phosphinic, phosphonic and seleninic acid bioisosteres of isonipecotic acid as novel and selective GABA(C) receptor antagonists. | Krehan D et al. | β | 2003 | β |
| Temporal modulation of scotopic visual signals by A17 amacrine cells in mammalian retina in vivo. | Dong CJ et al. | β | 2003 | β |
| The neurobiology and control of anxious states. | Millan MJ | β | 2003 | β |
| The Vogel conflict test: procedural aspects, gamma-aminobutyric acid, glutamate and monoamines. | Millan MJ et al. | β | 2003 | β |
| Two neuropharmacological types of rabbit ON-alpha ganglion cells express GABAC receptors. | Rotolo TC et al. | β | 2003 | β |
| Vigabatrin, but not gabapentin or topiramate, produces concentration-related effects on enzymes and intermediates of the GABA shunt in rat brain and retina. | Sills GJ et al. | β | 2003 | β |
| ZIP3, a new splice variant of the PKC-zeta-interacting protein family, binds to GABAC receptors, PKC-zeta, and Kv beta 2. | Croci C et al. | β | 2003 | β |
| Anxiety over GABA(A) receptor structure relieved by AChBP. | Cromer BA et al. | β | 2002 | β |
| Ectopic expression of the GABA(A) receptor alpha6 subunit in hippocampal pyramidal neurons produces extrasynaptic receptors and an increased tonic inhibition. | Wisden W et al. | β | 2002 | β |
| Elimination of the rho1 subunit abolishes GABA(C) receptor expression and alters visual processing in the mouse retina. | McCall MA et al. | β | 2002 | β |
| gamma-Aminobutyric acidA rho receptor subunits in the developing rat hippocampus. | Didelon F et al. | β | 2002 | β |
| Identification of a tyrosine in the agonist binding site of the homomeric rho1 gamma-aminobutyric acid (GABA) receptor that, when mutated, produces spontaneous opening. | Torres VI et al. | β | 2002 | β |
| Molecular structure and physiological function of chloride channels. | Jentsch TJ et al. | β | 2002 | β |
| Relative picrotoxin insensitivity distinguishes ionotropic GABA receptor-mediated IPSCs in hippocampal interneurons. | Semyanov A et al. | β | 2002 | β |
| Unique insecticide specificity of human homomeric rho 1 GABA(C) receptor. | Ratra GS et al. | β | 2002 | β |
| Modulation of native and recombinant GABA(A) receptors by endogenous and synthetic neuroactive steroids. | Lambert JJ et al. | β | 2001 | β |