3h Flunitrazepam
Mostrando 1-12 de 20 artigos, teses e dissertações.
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1. Pharmacologycal and auto-radiographical study of GABAA/benzodiazepine site, and biochemical assays of the Na+/K+-ATPase and of the glutamatergic receptors in rats susceptible and non-susceptible to clonic convulsions induced by DMCM, a benzodiazepine inverse agonist. / Estudo farmacológico e auto-radiográfico do complexo GABAA/Sítio benzodiazepínico, e ensaios bioquímicos da enzima Na+/K+- Atpase e de receptores glutamatérgicos em regiões encefálicas de ratos susceptíveis e não-susceptíveis às convulsões clônicas induzidas pelo DMCM, um agonista inverso benzodiazepínico.
Objective: The aim of this work was to verify if rats susceptible and non-susceptible to clonic convulsions induced by DMCM, a benzodiazepine inverse agonist, differ: 1) in the sensitivity to the hypnotic effect induced by diazepam and by others positive allosteric modulators of GABAA receptors; 2) in auto-radiographical analysis of [3H]-flunitrazepam bindin
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 26/12/2008
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2. Investigação da atividade ansiolítica de passiflora alata curtis (passifloraceae) / Anti-anxiety studies on passiflora alata Curtis (PASSIFLORACEAE)
Passiflora alata Curtis (PASSIFLORACEAE) é utilizada como tranqüilizante, seja popularmente ou pela indústria farmacêutica na produção de fitoterápicos. O objetivo desse trabalho foi avaliar, em camundongos, a atividade geral sobre o Sistema Nervoso Central e o efeito ansiolítico de um extrato hidroetanólico (70%) (EXT) e de duas frações enriqueci
Publicado em: 2007
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3. Avaliação dos efeitos de variações temporais relacionadas à apresentação de estímulos aversivos sobre a memória emocional de ratos expostos ao labirinto em cruz elevado
Fármacos benzodiazepínicos (BZP) reduzem o comportamento de ansiedade associado aos braços abertos (BA) do Labirinto em Cruz Elevado (LCE) durante uma primeira exposição. Numa segunda exposição a administração do BZP não apresenta tal efeito, este fenômeno é denominado One-Trial Tolerance (OTT). Durante a primeira exposição, a manipulação do
Publicado em: 2006
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4. Diazepam receptor: specific nuclear binding of [3H]flunitrazepam.
Autoradiographic localization of [3H]flunitrazepam in nuclei of the rat cerebral cortex was further confirmed by biochemical analysis of specific nuclear binding. Highly purified rat cerebral cortex nuclei were shown to bind [3H]flunitrazepam specifically. The Kd(app) for nuclear binding was 28 nM for the nuclei compared with a Kd(app) of 1.1 nM for binding
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5. Benzodiazepine receptor protein identified and visualized in brain tissue by a photoaffinity label.
Flunitrazepam, a potent benzodiazepine, reversibly binds to the benzodiazepine receptor with high affinity. When irradiated with UV light, flunitrazepam was irreversibly linked to brain tissue. Incorporation of [3H]flunitrazepam was inhibited by other benzodiazepines with a potency corresponding to their affinity for the benzodiazepine receptor. Photolabelin
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6. gamma-Aminobutyric acid and benzodiazepine receptors: copurification and characterization.
gamma-Aminobutyric acid (GABA) and benzodiazepine receptors have been solubilized and purified by procedures such as gel filtration, ion-exchange, lectin, and affinity chromatographies. All of these procedures enhance the specific activity of each receptor to a similar extent. The drug specificities of [3H]muscimol and [3H]flunitrazepam binding sites are the
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7. Autoradiography of benzodiazepine receptor binding in the central nervous system of the normal C57BL6J mouse.
[3H]flunitrazepam has been used as a photoaffinity label for the specific, clonazepam-displaceable 1,4-benzodiazepine binding sites in sections of normal C57BL6J mouse brain and spinal cord. Binding was visualized by light microscope autoradiography and quantified by a simple microdensitometric procedure. Specific flunitrazepam binding was seen to be highest
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8. Isolation and identification in bovine cerebral cortex of n-butyl beta-carboline-3-carboxylate, a potent benzodiazepine binding inhibitor.
A substance having benzodiazepine-binding inhibitory activity has been extracted from 18 kg of gray matter of bovine cerebral cortex and purified to homogeneity. This substance inhibits competitively [3H]flunitrazepam and ethyl beta-[3H]carboline-3-carboxylate binding with high affinity (Ki, 3 nM), but it is inactive upon 3H-labeled Ro 5-4864, [3H]quinuclidi
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9. Changes in benzodiazepine receptor binding as seen autoradiographically in the central nervous system of the spastic mouse.
Quantitative light-microscope autoradiography has been used to compare the specific, clonazepam-displaceable binding of [3H]flunitrazepam, a photoaffinity label for the 1,4-benzodiazepine receptor, in different regions of the brain and spinal cord of spastic mice and their unaffected littermates. Specific binding of [3H]flunitrazepam in the central nervous s
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10. Study of an octadecaneuropeptide derived from diazepam binding inhibitor (DBI): biological activity and presence in rat brain.
An endogenous brain neuropeptide with 104 amino acid residues that modulates gamma-aminobutyric acid receptor function was termed DBI because it displaces diazepam from its specific brain binding sites. Tryptic digestion of DBI generates an octadecaneuropeptide (ODN) that is more potent than the parent compound in the displacement of specifically bound beta-
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11. Benzodiazepine/gamma-aminobutyric acid receptor deficit in the midbrain of the seizure-susceptible gerbil.
The density of benzodiazepine/gamma-aminobutyric acid receptor binding sites was lower in the midbrain of seizure-susceptible gerbils compared to control seizure-resistant gerbils. Binding of [3H]diazepam to high-affinity brain-specific sites in membrane homogenates of gerbil brain showed a 20-30% lower binding in midbrain (but not other regions) in adult se
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12. Benzodiazepines have high-affinity binding sites and induce melanogenesis in B16/C3 melanoma cells.
We found that two markers of differentiation, tyrosinase (monophenol, dihydroxyphenylalanine:oxygen oxidoreductase, EC 1.14.18.1) activity and melanin synthesis, are induced by diazepam in B16/C3 mouse melanoma cells. We also demonstrated high-affinity binding sites for [3H]diazepam in these cells by radioreceptor assay, and we visualized binding to the cell