Search results for "Zolpidem"
showing 10 items of 13 documents
Zaleplon displays a selectivity to recombinant GABAA receptors different from zolipdem, zopiclone and benzodiazepines
1999
A chemically heterogeneous group of compounds acts at the benzodiazepine (BZ) recognition site of the γ-aminobutyric acid type A (GABAA) receptor complex. Whereas most 1,4-BZs recognize all GABAA/BZ receptors with similar affinity, other compounds differentiate between the large number of native GABAA receptors which assemble from the more than 14 known subunits. Here we describe the in vitro binding properties of the BZs lorazepam and Ro 15-4513 plus the three hypnotics zaleplon, zolpidem and zopiclone to eight receptors subtypes. Lorazepam fits well into the general shceme for other 1,4-BZs with respect to its receptor subtype selectivity in spite of its clinically different use. Zaleplon…
Behavioural responsiveness to picrotoxin and desipramine in adult rats prenatally exposed to different benzodiazepine receptor agonists
1995
The behavioural responsiveness to picrotoxin and desipramine was investigated in adult rats prenatally exposed to different benzodiazepine receptor agonists such as diazepam, alprazolam and zolpidem. Prenatal exposure to diazepam and alprazolam similarly potentiated the anti-immobility effect on the forced swimming test and the inhibitory effect on spontaneous motor activity of picrotoxin and desipramine and increased the seizure sensitivity to picrotoxin. Prenatal zolpidem seems to be ineffective. These data suggest that, despite the differences in their pharmacodynamic profile, prenatal exposure to diazepam and alprazolam, but not zolpidem, may have similar permanent consequences on the b…
Alteraciones del ritmo del sueño en modelos animales de encefalopatia hepática
2016
Introducción: La encefalopatía hepática (EH) es un síndrome neuropsiquiátrico presente en pacientes con enfermedades hepáticas que conduce a diferentes alteraciones neurológicas que pueden llevar al coma y la muerte. Dentro de las manifestaciones neurológicas precoces de la enfermedad, están las alteraciones del sueño con una prevalencia casi del 50% en pacientes con cirrosis hepática sin evidencia clínica. En la actualidad, varios grupos de investigación han demostrado que el deterioro cognitivo y motor de los pacientes con enfermedades hepáticas se reproduce en modelos animales con EH e hiperamonémia sin fallo hepático, así que del mismo modo, estos deben reproducir las alteraciones del s…
Intrinsic activation of GABAA receptors suppresses epileptiform activity in the cerebral cortex of immature mice
2010
SUMMARY Purpose: Activation of ionotropic c-aminobutyric acid type A (GABAA) receptors induces in immature neocortical neurons a membrane depolarization that may contribute to the higher epilepsy susceptibility in newborns. To elucidate whether depolarizing GABAergic responses enhance or attenuate epileptiform activity in the immature neocortex, we investigated the effect of agonists, antagonists, and positive modulators of GABAA receptors on epileptiform activity. Methods: We performed in vitro field potential recordings on isolated whole neocortex preparations and whole cell recordings of identified pyramidal neurons in 400-lm slices of immature (postnatal day 1–7) mice. Epileptiform acti…
Combination of open field and elevated plus-maze: a suitable test battery to assess strain as well as treatment differences in rat behavior.
1998
Abstract 1. 1. A test battery consisting of a standard open field, an enriched open field and an elevated plus maze was used to study behavior in rats. 2. 2. Male rats of the strains PVG/OlaHsd (PVG) and Sprague-Dawely-Hsd (SPRD) (150–200g body wt) were used to assess interstrain differences as well as handling effects. In a subsequent experiment an other set of male PVG rats (150–200g body wt) treated either with diazepam or zolpidem was used to evaluate the test battery for pharmacological purposes. 3. 3. SPRD rats displayed higher motor activity levels and also higher levels of exploratory behavior than the PVG rats. In contrast plus-maze activity indicated more anxiety of SPRD than PVG …
GABAA receptors in the ventral tegmental area control the outcome of a social competition in rats
2018
Social dominance can be attained through social competitions. Recent work in both humans and rodents has identified trait anxiety as a crucial predictor of social competitiveness. In addition, the anxiolytic GABAA positive modulator, diazepam, injected either systemically or into the ventral tegmental area (VTA) was shown to increase social dominance. Here, we investigated the impact of pharmacologically targeting GABAA receptors in the VTA for the outcome of a social competition between two unfamiliar male rats, one of them infused with vehicle and the other one with the drug under study. We show that infusion of the GABAA receptor agonist, muscimol, reduced anxiety-like behaviors and enha…
GABAA-receptor Subtypes: Clinical Efficacy and Selectivity of Benzodiazepine Site Ligands
1997
The main inhibitory neurotransmitter receptor of the brain, the gamma-aminobutyric acid type A receptor (GABA[A]), mediates the actions of several classes of clinically important drugs, such as benzodiazepines, barbiturates and general anaesthetics. This review summarizes the current knowledge on how classical benzodiazepines and novel nonbenzodiazepine compounds act on the benzodiazepine site of GABA(A) receptors and on their clinical pharmacology related to anxiolytic, sedative, hypnotic and cognitive effects or side-effects. Partial agonism, receptor subtype selectivity and novel binding sites are discussed as possible strategies to develop new drugs with fewer adverse effects than are s…
Prenatal exposure to diazepam and alprazolam, but not to zolpidem, affects behavioural stress reactivity in handling-naïve and handling-habituated ad…
2002
A gentle long-lasting handling produces persistent neurochemical and behavioural changes and attenuates the impairment in the behavioural reactivity to novelty induced by the prenatal exposure to diazepam (DZ) in adult male rat progeny. This study investigated the consequences of a late prenatal treatment with three GABA/BDZ R agonists (DZ) alprazolam (ALP) and zolpidem (ZOLP)), on different stress-related behavioural patterns, in non-handled (NH), short-lasting handled (SLH) and long-lasting handled (LLH) adult male rats exposed to forced swim test (FST), acoustic startle reflex (ASR) and Vogel test (VT). The effects on motor activity were evaluated in the open field and in the Skinner box…
Anxiolytic-like effects of acute and chronic GABA transporter inhibition in rats.
2002
Acute GABA transporter inhibition can induce anxiolytic-like behaviors. The present analysis addressed whether chronic treatment (23 days via drinking water) with a GABA transporter inhibitor affects rat behavior similar to acute treatment and interferes with additional benzodiazepine-receptor agonistic treatment. Seventy-one rats divided into seven groups were acutely treated with either vehicle, diazepam (2 mg/kg), zolpidem (0.05 mg/kg), tiagabine (19 mg/kg) or chronically with tiagabine with or without acute diazepam or zolpidem. Animals were behaviorally characterized in an elevated plus-maze. None of the treatments induced changes in the activity of the animals. Acute and chronic treat…
Postnatal alterations of the inhibitory synaptic responses recorded from cortical pyramidal neurons in the Lis1/sLis1 mutant mouse
2006
Mutations in the mouse Lis1 gene produce severe alterations in the developing cortex. We have examined some electrophysiological responses of cortical pyramidal neurons during the early postnatal development of Lis/sLis1 mutant mice. In P7 and P30 Lis1/sLis1 neurons we detected a lower frequency and slower decay phase of mIPSCs, and at P30 the mIPSCs amplitude and the action potential duration were reduced. Zolpidem (an agonist of GABAA receptors containing the alpha1 subunit) neither modified the amplitude nor the decay time of mIPSCs at P7 in Lis1/sLis1 neurons, whereas it increased the decay time at P30. The levels of GABAA receptor alpha1 subunit mRNA were reduced in the Lis1/sLis1 brai…