Changes in GABAergic inhibition occur during physiological processes, during response to drugs and in various pathologies. These changes can be achieved through direct allosteric modifications at the γ-amino butyric acid (GABA) type A (GABAA) receptor protein level, or by altering the synthesis, trafficking and stability of the receptor. Neurosteroids (NSs) and protein kinase C (PKC) are potent...

GABAA receptors are a heterogeneous family of ligand-gated ion channels responsible for mediating inhibitory neurotransmission in the CNS. Since the identification of mammalian cDNAs encoding 13 GABAA-receptor subunits, the composition of native receptor molecules and their localization in the brain has been an area of intense study. We conclude that the number of major subtypes is probably les...

GABA receptors of bipolar cells from the skate retina: actions of zinc on GABA-mediated membrane currents. J. Neurophysiol. 78: 2402-2412, 1997. gamma-Aminobutyric acid (GABA)-induced currents were recorded from isolated bipolar cells of the skate retina using perforated patch-clamp methodology. Pharmacological analysis of the responses, using selective agonists and antagonists of the major cla...

objective(s):painful diabetic neuropathy is associated with hyperexcitability and hyperactivity of spinal cord neurons. however, its underlying pathophysiological mechanisms have not been fully clarified. induction of excitatory/inhibitory neurotransmission imbalance at the spinal cord seems to account for the abnormal neuronal activity in diabetes. protective properties of neurosteroids have b...

Sadeghi H, Taylor HS. HOXA10 regulates endometrial GABAA receptor expression and membrane translocation. Am J Physiol Endocrinol Metab 298: E889 –E893, 2010. First published January 26, 2010; doi:10.1152/ajpendo.00577.2009.—Expression of the GABAA receptor has been described previously in the human endometrium in both luminal epithelium and stroma. Its expression is increased during decidualiza...

In the CNS, gamma-aminobutyric acid (GABA) affects neuronal activity through both the ligand-gated GABAA receptor channel and the G protein-coupled GABAB receptor. In the mature nervous system, both receptor subtypes decrease neural excitability, whereas in most neurons during development, the GABAA receptor increases neural excitability and raises cytosolic Ca2+ levels. We used Ca2+ digital im...

Feng, Hua-Jun and Robert L. Macdonald. Proton modulation of 1 3 GABAA receptor channel gating and desensitization. J Neurophysiol 92: 1577–1585, 2004. First published May 19, 2004; 10.1152/jn.00285.2004. GABAA receptor currents are phasic and desensitizing, whereas GABAA receptor currents are tonic and have no fast desensitization. receptors are subsynaptic and mediate phasic inhibition, wherea...

Classical benzodiazepine drugs are in wide clinical use as anxiolytics, hypnotics, anticonvulsants, and muscle relaxants. They act by enhancing the -aminobutyric acidA (GABAA) receptor function in the central nervous system. The pharmacological relevance of the multitude of structurally diverse GABAA receptor subtypes has only recently been identified. Based on an in vivo point mutation strateg...

introduction: 17&beta-estradiol; modulates nociception by binding to the estrogenic receptors and also by allosteric interaction with other membrane-bound receptors like glutamate and gabaa receptors. in addition to its autonomic functions, paragigantocellularis lateralis (lpgi) is involved in the pain modulation, too. the aim of the current study was to investigate the involvement of the membr...

Autonomic dysregulation accompanies type-1 diabetes, and synaptic regulation of parasympathetic preganglionic motor neurons in the dorsal motor nucleus of the vagus (DMV) is altered after chronic hyperglycemia/hypoinsulinemia. Tonic gamma-aminobutyric acid A (GABAA) inhibition prominently regulates DMV neuron activity, which contributes to autonomic control of energy homeostasis. This study inv...