Background γ-Aminobutyric acid (GABA) is considered to be the predominant inhibitory neurotransmitter in mammalian central nervous systems (CNS). There are two major classes of GABA receptors: GABAARs and GABABRs. The GABAA receptor is derived from various subunits such as alpha1-alpha 6, beta1-beta 3, gamma1-gamma 4, delta, epsilon, pi, and rho1-3. Intensive research has been performed to und...

Background: GABAA receptor γ2 and δ subunits are thought to be responsible for synaptic and extrasynaptic targeting. Results: We demonstrate here that α2 and α6 subunits can target δ/γ2 chimeras to synaptic and extrasynaptic sites. Conclusion: The α subunits play a direct role in GABAA receptor targeting. Significance: Different subunits of GABAA receptors encode intrinsic signals to control su...

BACKGROUND Anaesthetic steroids are established positive allosteric modulators of GABAA receptors, but little is known concerning steroid modulation of strychnine-sensitive glycine receptors, the principal mediators of fast, inhibitory neurotransmission in the brain stem and spinal cord. This study compared the modulatory actions of five anaesthetic pregnane steroids and two non-anaesthetic iso...

Wu J, Chang Y, Li G, Xue F, DeChon J, Ellsworth K, Liu Q, Yang K, Bahadroani N, Zheng C, Zhang J, Rekate H, Rho JM, Kerrigan JF. Electrophysiological properties and subunit composition of GABAA receptors in patients with gelastic seizures and hypothalamic hamartoma. J Neurophysiol 98: 5–15, 2007. First published April 11, 2007; doi:10.1152/jn.00165.2007. Abnormalities in GABAA receptor structur...

The mAb 62-3G1 to the GABAA receptor/benzodiazepine receptor/Cl- channel complex was used with light-microscopy immunocytochemistry for studying the localization of the GABAA receptors (GABAR) in the rat brain. The results have shown a receptor distribution identical to the one obtained by others using 3H-muscimol binding in combination with autoradiographic techniques. The external plexiform l...

The properties of GABA receptor-mediated responses were examined in noncultured astrocytes, acutely isolated from the mature rat hippocampus. Whole-cell patch clamping revealed a GABA-activated Cl- conductance that was mimicked by the GABAA receptor agonist muscimol and depressed by the GABAA antagonists bicuculline and picrotoxin. The GABAA-activated currents were potentiated by the barbiturat...

Introduction: Estradiol is a neuroactive steroid, which is found in several brain areas such as locus coeruleus (LC). Estradiol modulates nociception by binding to its receptors and also by allosteric interaction with other membranebound receptors like glutamate and GABAA receptors. LC is involved in noradrenergic descending pain modulation. Methods: In order to study the effect of 17β-estra...

Whole cell recordings were obtained from ventral horn neurons in spontaneously active spinal cords isolated from the chick embryo [embryonic days 10 to 11 (E10-E11)] to examine the post-episode depression of GABAergic transmission. Spontaneous activity occurred as recurrent, rhythmic episodes approximately 60 s in duration with 10- to 15-min quiescent inter-episode intervals. Current-clamp reco...

Protein tyrosine phosphorylation is a key event in diverse intracellular signaling pathways and has been implicated in modification of neuronal functioning. We investigated the role of tyrosine phosphorylation in regulating type A GABA (GABAA) receptors in cultured CNS neurons. Extracellular application of genistein (50 microM), a membrane-permeable inhibitor of protein tyrosine kinases (PTKs),...

Several protein kinases are known to phosphorylate Ser/Thr residues of certain GABAA receptor subunits. Yet, the effect of phosphorylation on GABAA receptor function in neurons remains controversial, and the functional consequences of phosphorylating synaptic GABAA receptors of adult CNS neurons are poorly understood. We used whole-cell patch-clamp recordings of GABAA receptor-mediated miniatur...