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[Brain GABA-receptor systems in functional thyroid disorders].

Probl Endokrinol (Mosk)

October 2009

Tashkent Medical Academy.

This experimental study was designed to evaluate effects of hypo- and hyperthyroidism on the density of 3H-muscimol and 3H-diazepam-binding sites in synaptic membranes of the rat brain. It was shown that density of both 3H-muscimol and 3H-diazepam-binding sites increases in animals with hypothyroidism and decreases in hyperthyroidism. This difference may account for the predominance of general inhibitory reaction in animals with hypothyroidism and general excitation in hyperthyroid rats.

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Caffeine analogs: effects on ryanodine-sensitive calcium-release channels and GABAA receptors.

Cell Mol Neurobiol

June 2003

Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland, USA.

1. Caffeine at 0.3-10 mM enhanced the binding of [3H]ryanodine to calcium-release channels of rabbit muscle sarcoplasmic reticulum.

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GABA(A) receptor sites were characterised in cerebral cortex tissue samples from deceased neurologically normal infants who had come to autopsy during the third trimester of pregnancy. Pharmacological parameters were obtained from homogenate binding studies which utilised the 'central-type' benzodiazepine ligands [3H]diazepam and [3H]flunitrazepam, and from the GABA activation of [3H]diazepam binding. It was found that the two radioligands behaved differently during development.

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The individual sensitivity of the male Wistar rats to acute pentylenetetrazole injection was studied, the density and the affinity of benzodiazepine receptors in the cerebellar cortex for 3H-diazepam was measured. It was demonstrated that the reactivity of benzodiazepine receptors underlies the individual sensitivity to pentylenetetrazole. The animals with higher sensitivity were characterized by more intensive reaction than the control and resistant animals, i.

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If the in vivo effects of anaesthesia are mediated through a specific receptor system, then a relationship could exist between the regional changes in brain metabolism caused by a particular agent and the underlying regional distribution of the specific receptors affected by that agent. Positron emission tomography data from volunteers studied while unconscious during propofol (n=8) or isoflurane (n=5) anaesthesia were used retrospectively to explore for evidence of relationships between regional anaesthetic effects on brain glucose metabolism and known (ex vivo) regional distribution patterns of human receptor binding sites. The regional metabolic reductions caused by propofol differed significantly from those of isoflurane.

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