introduction: neuropathic pain can be very difficult to treat and it is one of the important medical challenging about pain treatments. muscimol as a new agonist of gamma-aminobutyric acid receptor type a (gaba a ) have been introduced for pain management. thus, the present study was performed to evaluate the pain alleviating effect of intrathecal injection of different doses of muscimol as gab...

In the present study, the effect of GABA (γ-aminobutyric acid) receptor agonists and antagonists on morphine-induced antinociception was investigated in formalin test in rats. Intraperitoneal (i.p.) injection of different doses of morphine (1, 3, 6 and 9 mg/kg) and intracerebroventricular (i.c.v.) injection of different doses of muscimol (0.5, 1 and 2 g/rat) or baclofen (0.25, 0.5 and 1 g/rat) ...

in the present study, the effect of gaba (γ-aminobutyric acid) receptor agonists and antagonists on morphine-induced antinociception was investigated in formalin test in rats. intraperitoneal (i.p.) injection of different doses of morphine (1, 3, 6 and 9 mg/kg) and intracerebroventricular (i.c.v.) injection of different doses of muscimol (0.5, 1 and 2 g/rat) or baclofen (0.25, 0.5 and 1 g/rat) ...

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...

Using human g-aminobutyric acid type A (GABAA) receptor subunit combinations, expressed in cell lines and Xenopus laevis oocytes, the pharmacology of a number of ligands interacting directly with the GABA recognition site has been studied in [H]muscimol binding and electrophysiologically. The binding affinity of GABAA agonist and antagonist ligands showed small but statistically significant dep...

Using human gamma-aminobutyric acid type A (GABAA) receptor subunit combinations, expressed in cell lines and Xenopus laevis oocytes, the pharmacology of a number of ligands interacting directly with the GABA recognition site has been studied in [3H]muscimol binding and electrophysiologically. The binding affinity of GABAA agonist and antagonist ligands showed small but statistically significan...

Exposure to acute psychological or physical stress increases core body temperature (stress-induced hyperthermia, SIH) which is part of the autonomic stress response. SIH is used as a putative rodent anxiety paradigm in which anxiolytic drugs reduce the SIH response. The predictive validity of the SIH paradigm has proven to be good, making it suitable to detect the putative anxiolytic properties...

Over the last several years, evidence has accumulated that the GABAA receptor is compromised in animal models for fragile X syndrome (FXS), a common hereditary form of intellectual disability. In mouse and fly models, agonists of the GABAA receptor were able to rescue specific consequences of the fragile X mutation. Here, we imaged and quantified GABAA receptors in vivo in brain of fragile X pa...

..................................................................................................... 6 ABBREVIATIONS....................................................................................... 7 LIST OF ORIGINAL PAPERS............................................................ 8 INTRODUCTION .......................................................................................... ...

Imidazo[1,5-a][1,4]benzodiazepines are well documented to exhibit potent activity at GABAA/Bz receptors. This series belongs to one of the very few chemical families, which have been extensively investigated for GABAA/Bz receptor mediated activity.1,2 Flumazenil (Ro 15-1788), an imidazo[1,5-a][1,4]benzodiazepine, was earlier shown to bind to central GABAA receptors with little or no intrinsic a...