A characteristic of both hypertension and pregnancy is increased sympathetic nerve activity. The level of sympathetic activation is determined, in part, by a tonic GABAergic inhibition arising from the hypothalamic paraventricular nucleus (PVN). In hypertension, decreases in GABAergic inhibition and increases in glutamatergic excitation within the PVN contribute to this sympatho-excitation. In ...

Extracts from Glycyrrhiza are traditionally used for the treatment of insomnia and anxiety. Glabridin is one of the main flavonoid compounds from Glycyrrhiza glabra and displays a broad range of biological properties. In the present work, we investigated the effect of glabridin on GABAA receptors. For this purpose, we employed the two-electrode voltage-clamp technique on Xenopus laevis oocytes ...

In cerebellum, 75% of all GABAA receptors contain alpha1 subunits. Here, we investigated compensatory changes in GABAA receptor subunit expression and composition in alpha1 subunit-knockout mice. In these mice the total number of cerebellar GABAA receptors was reduced by 46%. Whereas the number of receptors containing alpha6 subunits was unchanged, the total amount of alpha6 subunits was signif...

Editor’s key points † Inhaled anaesthetics act by potentiating inhibitory type A GABA (GABAA) receptors to produce some of their desired, and perhaps undesired, effects. † Using cultured hippocampal neurones, inverse agonists selective for a5 subunit containing GABAA receptors reduced receptor potentiation by volatile anaesthetics. † Potentiation of a5 subunit-containing GABAA receptors might c...

The inhibition of gamma-aminobutyric acid (GABA)-gated chloride currents by the protein kinase C (PKC) activator 4beta-phorbol 12-myristate 13-acetate (PMA) was investigated using recombinant human GABAA receptors expressed in Xenopus oocytes. PMA (5 nM) reduced the GABA response in oocytes expressing the alpha1 beta2 gamma2L receptor construct, as measured by the two-electrode voltage-clamp me...

The GABAergic synapse undergoes structural and functional maturation during early brain development. Maternal stress alters GABAergic synapses in the pup's brain that are associated with the pathophysiology of neuropsychiatric disorders in adults; however, the mechanism for this is still unclear. In this study, we examined the effects of maternal restraint stress on the development of Cation-Ch...

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...

Seven monkey-specific GABAA receptor subunit cDNAs were isolated and cloned; radioactive cDNA and cRNA probes derived from them were used for Northern blot analysis and in situ hybridization histochemistry of the primary visual cortex (area 17), with comparative observations on other cortical areas. cDNAs corresponding to alpha 1, alpha 2, alpha 4, alpha 5, beta 1, beta 2, and gamma 2 GABAA rec...

20 We previously reported that gastric activity is controlled by a robust GABAA 21 receptor–mediated inhibition in the medial nucleus of the tractus solitarius (mNTS) 22 (Herman et al. 2009) and that μ-opioid receptor activation inhibits gastric tone by 23 suppression of this GABA signaling (Herman et al. 2010). These data raised two 24 questions: (1) whether any of this inhibition was due to t...

BACKGROUND Gamma-aminobutyric acid type A (GABAA) receptors provide the main inhibitory control in the brain. Their heterogeneity may make it possible to precisely target drug effects to selected neuronal populations. In situ hybridization using rat brain sections has revealed a unique expression of GABAA receptor epsilon and theta subunit transcripts in the locus coeruleus, where they are acco...