Actions of pentobarbitone and derivatives with modified 5-butyl substituents on GABA and diazepam binding to rat brain synaptosomal membranes
| Autor: | Graham M. Nicholson, T. Katsikas, J. Tabar, P. R. Andrews, John H. Skerritt, Graham A.R. Johnston |
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| Rok vydání: | 1983 |
| Předmět: |
Male
Pentobarbital medicine.drug_class medicine.medical_treatment Receptors Cell Surface Pharmacology Biochemistry Structure-Activity Relationship Cellular and Molecular Neuroscience medicine Animals gamma-Aminobutyric Acid Synaptosome Diazepam binding Diazepam Chemistry Brain Rats Inbred Strains Intracellular Membranes General Medicine GABA receptor antagonist Receptors GABA-A Rats Kinetics Anticonvulsant Mechanism of action Barbiturate medicine.symptom Synaptosomes medicine.drug |
| Zdroj: | Neurochemical Research. 8:1337-1350 |
| ISSN: | 1573-6903 0364-3190 |
| Popis: | The effects of a variety of factors known to influence the enhancement of GABA binding by diazepam, were studied upon pentobarbitone stimulation of GABA binding to washed synaptosomal membranes prepared from whole rat brains. The differential kinetics of, and effects of temperature, chloride ions, a benzodiazepine receptor antagonist (Ro15-1788) and picrotoxinin upon pentobarbitone and diazepam enhancement of GABA binding, suggest that these drugs exert their actions upon GABA binding at different loci. The degree of enhancement of diazepam binding and of high affinity GABA binding in chloride-containing media at 25 degrees C by members of a series of twelve side chain methyl substituted and/or unsaturated derivatives of 5-butyl-5-ethyl-barbituric acid (pentobarbitone analogs) correlated significantly. For the sedative members of the series, enhancement of high affinity GABA binding correlated with their anaesthetic but not their anticonvulsant activities. It appears likely that the anaesthetic and anticonvulsant activities of barbiturates arise from different molecular actions. |
| Databáze: | OpenAIRE |
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