Search results for "GABA"
showing 10 items of 390 documents
Anticonvulsant and antidepressant activity of the selected terpene GABA derivatives in experimental tests in mice
2006
The present study was designed to investigate the central nervous system activity of terpene GABA (and piracetam) derivatives designated as BF-1, BF-2, BF-3, BF-4, BF-5, BF-6. We assessed their anticonvulsant activity in the two main mouse models of seizures (MES-test, PTZ-test), an antidepressant-like effect in the forced swim test (FST), as well as an influence on spontaneous locomotor activity. Our study demonstrated the strong anticonvulsant activity of (1S,3R,7R)-(-)-3,8,8-trimethyl-4-aza-bicyclo[5.1.0]acetate-5-one hydrochloride (compound BF-2) in the PTZ-test. Activity of BF-2 was equipotent to ethosuximide (380 mg/kg, po) in the PTZ-test, when used at a dose of 100 mg/kg, po. No neu…
Combination of alpha lipoic acid and gabapentin, its efficacy in the treatment of burning mouth syndrome : a randomized, double-blind, placebo contro…
2010
Burning Mouth Syndrome (BMS) is a disease that manifests as burning in the tongue or in any area of the oral mucosa, in the absence of clinically verifiable injuries. Objectives: To verify the efficacy of alpha lipoic acid (ALA) and gabapentin (GABA), used individually and jointly, to reduce the burning in patients with burning mouth and establish a drug therapy for the BMS. Study Design: During April and May 2008, we conducted a randomized, double-blind, placebo-controlled trial in the Department of Clinical Stomatology, Faculty of Dentistry, Rosario, Argentina. The gathering of patients was between those ones with BMS who were treated in our service between March 2003 and March 2008 witho…
Comparative pharmacological activity of optical isomers of phenibut
2007
Phenibut (3-phenyl-4-aminobutyric acid) is a GABA (gamma-aminobutyric acid)-mimetic psychotropic drug which is clinically used in its racemic form. The aim of the present study was to compare the effects of racemic phenibut and its optical isomers in pharmacological tests and GABAB receptor binding studies. In pharmacological tests of locomotor activity, antidepressant and pain effects, S-phenibut was inactive in doses up to 500 mg/kg. In contrast, R-phenibut turned out to be two times more potent than racemic phenibut in most of the tests. In the forced swimming test, at a dose of 100 mg/kg only R-phenibut significantly decreased immobility time. Both R-phenibut and racemic phenibut showed…
Beta-carbolines as benzodiazepine receptor ligands II: Synthesis and benzodiazepine receptor affinity of beta-carboline-3-carboxylic acid amides.
1985
Numerous beta-carboline-3-carboxamides were synthesized by amidation of beta-carboline-3-carboxylic acid, with various amino acids and amino acid esters serving as amine components, and tested in respect to their affinity for the benzodiazepine receptor in mouse brain membranes. The title compounds have affinities in the low micromolar range. The results are discussed with respect to their relevance for a possible beta-carboline structure containing the endogenous ligand of the benzodiazepine receptor.
Hippocampal GABAergic Synapses Possess the Molecular Machinery for Retrograde Nitric Oxide Signaling
2007
Nitric oxide (NO) plays an important role in synaptic plasticity as a retrograde messenger at glutamatergic synapses. Here we describe that, in hippocampal pyramidal cells, neuronal nitric oxide synthase (nNOS) is also associated with the postsynaptic active zones of GABAergic symmetrical synapses terminating on their somata, dendrites, and axon initial segments in both mice and rats. The NO receptor nitric oxide-sensitive guanylyl cyclase (NOsGC) is present in the brain in two functional subunit compositions: α1β1and α2β1. The β1subunit is expressed in both pyramidal cells and interneurons in the hippocampus. Using immunohistochemistry andin situhybridization methods, we describe that the …
Neuroprotective effect of ceftriaxone on the penumbra in a rat venous ischemia model.
2012
Glutamate transporter-1 (GLT-1) maintains low concentrations of extracellular glutamate by removing glutamate from the extracellular space. It is controversial, however, whether upregulation of GLT-1 is neuroprotective under all ischemic/hypoxic conditions. Recently, a neuroprotective effect of preconditioning with a β-lactam antibiotic ceftriaxone (CTX) that increases expression of GLT-1 has been reported in animal models of focal ischemia. On the other hand, it is said that CTX does not play a neuroprotective role in an in vitro study. Thus, we examined the effect of CTX on ischemic injury in a rat model of two-vein occlusion (2VO). This model mimics venous ischemia during, e.g. tumor sur…
A repetitive intracortical microstimulation pattern induces long-lasting synaptic depression in brain slices of the rat primary somatosensory cortex.
2000
Repetitive intracortical microstimulation (ICMS) applied to the rat primary somatosensory cortex (SI) in vivo was reported to induce reorganization of receptive fields and cortical maps. The present study was designed to exam- ine the effect of such an ICMS pattern applied to layer IV of brain slices containing SI on the efficacy of synaptic in- put to layer II/III. Effects of ICMS on the synaptic strength was quantified for the first synaptic component ( s1) of cor- tical field potentials (FPs) recorded from layer II/III of SI. FPs were evoked by stimulation in layer IV. The pattern of ICMS was identical to that used in vivo. However, stimula- tion intensity had to be raised to induce an a…
Understanding Cannabinoid Psychoactivity with Mouse Genetic Models
2007
Marijuana and its main psychotropic ingredient Δ9-tetrahydrocannabinol (THC) exert a plethora of psychoactive effects through the activation of the neuronal cannabinoid receptor type 1 (CB1), which is expressed by different neuronal subpopulations in the central nervous system. The exact neuroanatomical substrates underlying each effect of THC are, however, not known. We tested locomotor, hypothermic, analgesic, and cataleptic effects of THC in conditional knockout mouse lines, which lack the expression of CB1 in different neuronal subpopulations, including principal brain neurons, GABAergic neurons (those that release γ aminobutyric acid), cortical glutamatergic neurons, and neurons expres…
Opposite motor responses elicited by ethanol in the posterior VTA: The role of acetaldehyde and the non-metabolized fraction of ethanol
2013
Recent electrophysiological evidence suggests that ethanol simultaneously exerts opposite effects on the activity of dopamine (DA) neurons in the ventral tegmental area (VTA) through two parallel mechanisms, one promoting and the other reducing the GABA release onto VTA DA neurons. Here we explore the possible behavioural implications of these findings by investigating the role displayed by acetaldehyde (the main metabolite of ethanol) and the non-metabolized fraction of ethanol in motor activity of rats. We analyse the appearance of motor activation or depression after intra-VTA administration of ethanol in rats subjected to different pharmacological pre-treatments designed to preferential…
Intermittent cortical stimulation evokes sensitization to cocaine and enduring changes in matrix and striosome neuron responsiveness
2005
Both the behavioral sensitization syndrome and the changes in the responsiveness of striatal neurons evoked by chronic cocaine exposure may be linked to enhanced neocortical activity, yet a direct demonstration of the effects of cortical stimulation on these parameters is lacking. We have found that repeated stimulation of the rat prelimbic cortex with picrotoxin (0.25 microg/0.25 microl, five injections on alternate days followed by 7-day withdrawal) contributed to increase c-Fos protein expression in the striosomes of the dorsolateral striatum, while producing the opposite effect in the matrix compartment, after a single exposure to cocaine (25 mg/kg). Moreover, rats exposed to cortical s…