GABA (γ-aminobutyric acid), the predominant inhibitory neurotransmitter in the mature mammalian brain, is excitatory for neurons during early development upon GABAA receptor activation. In astrocytes, GABA induces intracellular Ca2+ transients by activation of both, GABAA and GABAB receptors. GABAB receptor-mediated [Ca]i increases are involved in neuron-glia interaction by potentiating inhibit...

Gamma-aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the brain and is implicated in the pathophysiology of a number of neuropsychiatric disorders. The GABAB receptors are G-protein coupled receptors consisting of principle subunits and auxiliary potassium channel tetramerization domain (KCTD) subunits. The KCTD subunits 8, 12, 12b and 16 are cytosolic proteins that determi...

BACKGROUND Chemical stimulation of white adipose tissue (WAT) induces adipose afferent reflex (AAR), and thereby causes a general sympathetic activation. Paraventricular nucleus (PVN) is important in control of sympathetic outflow. This study was designed to investigate the role of γ-aminobutyric acid (GABA) in PVN in regulating the AAR. METHODOLOGY/PRINCIPAL FINDINGS Experiments were carried...

Colorectal cancer is one of the leading causes of highly fatal cancer-related deaths in the whole world. Fast growth is critical characteristic of colorectal cancer, the underlying regulatory mechanism of colorectal cell fast proliferation remains largely unknown. Here, we reported that activation of metabotropic γ-Aminobutyric acid receptor (GABAB R) signaling significantly inhibited the color...

Oxycodone is a μ-opioid receptor agonist, used for the treatment of a large variety of painful disorders. Several studies have reported that oxycodone is a more potent pain reliever than morphine, and that it improves the quality of life of patients. However, the neurobiological mechanisms underlying the therapeutic action of these two opioids are only partially understood. The aim of this stud...

Transient lower esophageal sphincter (LES) relaxation is the major mechanism of gastroesophageal reflux. This study uses an established ferret model to evaluate GABAB receptor agonists' ability to reduce triggering of transient LES relaxations. One hundred sixty manometric/pH studies were performed on 18 conscious ferrets. In untreated animals, intragastric infusion of 25 ml glucose (pH 3.5) le...

It is now well established that G protein-coupled receptors can exist not only as homodimers, but also as heterodimers or higher order oligomers. However, whether and how dimerization of the receptors is regulated is poorly understood. In this issue of The EMBO Journal, the team of Marc Landry provides evidence for an intriguing mechanism by which—under pathological conditions—GABAB receptor he...

Intracellular recordings were made from presumed dopamine-containing neurons in slices cut from the midbrain of the rat. Focal electrical stimulation produced a hyperpolarizing synaptic potential that was reduced by 75-95% by the GABAB-receptor antagonist 2-hydroxysaclofen (300 microM). 5-HT (3-100 microM) reduced the amplitude of the GABAB synaptic potential by 20-74%, with a 50% reduction at ...

26 Besides its quintessential role in reproduction, 17β-estradiol (E2) is a potent anorexigenic 27 hormone. E2 and the selective Gq-coupled membrane estrogen receptor (Gq-mER) ligand, 28 STX, rapidly increase membrane excitability in proopiomelanocortin (POMC) neurons by 29 desensitizing the coupling of GABAB receptors to G protein-coupled inwardly rectifying K 30 channels (GIRKs), which upon a...