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),...

There are coflicting reports regarding the role of GABA in morphine analgesia. While-sorne investigators have reported that treatment with GABAA receptor agonist muscimol and GABA transaminase inhibitors potentiates morphine analgesia (2.4.6) others have reported antagonism of morphine analgesia (8.10). In view of these conflicting reports and since the analgesic profile 'of THIP, a GABAA recep...

objective(s):the mechanism of hypothermia action of acetaminophen (apap) remains unclear even 125 years after its synthesis. acetaminophen produces hypothermia. the mechanism of this reduction in core body temperature is not clear but evidence shows that it is not dependent on opioid and cannabinoid receptors. because of strong documents about the roles of gaba and benzodiazepine receptors in h...

GABAA receptors are a pivotal inhibitory influence in the nervous system, and modulators of the GABAA receptor are important anesthetics, sedatives, anticonvulsants, and anxiolytics. Current views of receptor modulation suggest that many exogenous drugs access and bind to an extracellular receptor domain. Using novel synthetic steroid analogs, we examined the access route for neuroactive steroi...

g -aminobutiric acid (gaba), the major inhibitory neurotransmitter in the central nervous system has two major receptor subtypes (gabaa and gabab). gabab receptors are activated by the antispastic and muscle relaxant agent, baclofen, which is a lipophilic derivative of gaba. since 1962 several strategies have been reported for the synthesis of baclofen.in this study an approach has been made to...

objective: argemone mexicana is a papaveracea plant; some reports have shown their antibacterial, anti-cancer, sedative and probably anti-anxiety properties. from their aerial parts, flavonoids and alkaloids have been isolated, which are intrinsically related to some actions on the central nervous system. the aim of this study was to evaluate the anxiolytic-like effects of the plant, using its ...

Atomic resolution structures of cys-loop receptors, including one of a γ-aminobutyric acid type A receptor (GABAA receptor) subtype, allow amazing insights into the structural features and conformational changes that these pentameric ligand-gated ion channels (pLGICs) display. Here we present a comprehensive analysis of more than 30 cys-loop receptor structures of homologous proteins that revea...

An N-methyl-D-aspartate (NMDA)-independent form of long-term potentiation (LTP), which depends on postsynaptic, voltage-dependent calcium channels (VDCCs), has been demonstrated in area CA1 of hippocampus. GABA acting at GABAA receptors limits postsynaptic depolarization during LTP induction. Blockade of GABAA receptors should therefore enhance activation of postsynaptic VDCCs and facilitate th...

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