Several new benzodiazepines selectively interact with a benzodiazepine receptor subtype

@article{Sieghart1983SeveralNB,
  title={Several new benzodiazepines selectively interact with a benzodiazepine receptor subtype},
  author={Werner Sieghart},
  journal={Neuroscience Letters},
  year={1983},
  volume={38},
  pages={73-78}
}
  • W. Sieghart
  • Published 15 July 1983
  • Biology, Psychology, Chemistry
  • Neuroscience Letters
View on Elsevier
doi.org
62 Citations
Background Citations
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62 Citations

Citation Type

Citation Type

Affinity of various ligands for benzodiazepine receptors in rat cerebellum and hippocampus.
Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites.
Selective Ligands for Benzodiazepine Receptors: Recent Developments
TLDR
The scientific community also has its misconceptions about the term benzodiazepine, which is perhaps not surprising given the speed of evolution of the authors' knowledge about these drugs, their receptors and the uniqueness of their pharmacology.
Photoaffinity Labeling of Different Benzodiazepine Receptors at Physiological Temperature
TLDR
Differential inhibition at 37°C of irreversible [3H]flunitrazepam binding to the individual proteins by several selective benzodiazepine receptor ligands supports the hypothesis that P51 and P55 are associated with different benzodiazine receptors.
Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain
Benzodiazepine receptor binding of benzodiazepine hypnotics: Receptor and ligand specificity
Comparison of benzodiazepine receptor binding in membranes from human or rat brain
Comparison of Benzodiazepine Receptors in Cerebellum and Inferior Colliculus
  • W. Sieghart
  • Biology, Psychology
    Journal of neurochemistry
  • 1986
TLDR
Results indicate that in adult animals predominantly BZ1 receptors are enriched in both brain regions, however, in the brains of newborn animals, additional benzodiazepine receptor subtypes seem to exist in cerebellum as well as in inferior colliculus.
Benzodiazepine binding site heterogeneity in the purified GABAA receptor.
Use of the selective benzodiazepine-1 (BZ-1) ligand [3H]2-oxo-quazepam (SCH 15–725) to localize BZ-1 receptors in the rat brain
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TLDR
During structural modification of ethyl beta-carboline-3-carboxylate an agent was discovered which has high affinity for brain benzodiazepine receptors but which is a potent convulsant, which may explain the convulsive properties.
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GABA reduces binding of 3H-methyl β-carboline-3-carboxylate to brain benzodiazepine receptors
TLDR
Binding of the methyl ester of β-carboline-3-carboxylic acid (β-CCM), which by itself is a convulsant, is investigated and it is reported that 3H-β- CCM binds to brain benzodiazepine receptors and that, in contrast to binding of3H-diazepam, 2H- β-CCC binding is reduced by GABA in a bicuculline-sensitive manner.
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It is found that in hippocampus and several other brain regions at least two different types of benzodiazepine receptors exist, each seems to be associated with a γ-aminobutyric acid (GABA) receptor.
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TLDR
3H-Ro 15-1788 interacts with the same number of BR sites as the agonist 3H-clonazepam in various brain regions, but their mode of receptor interaction is different and the thermodynamics of agonist and antagonist receptor interaction are different, but only at temperatures above 21 °C.
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TLDR
Evidence indicates that the benzodiazepines exert their therapeutic effects by interacting with a high-affinity binding site (receptor) in the brain and several naturally occurring compounds, including the purines and nicotinamide, are candidates for this role.
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Valium is a safe, potent anxiolytic with pronounced muscle relaxant properties, and is the best known tranquilizer of its kind.
[3H]Propyl β‐Carboline‐3‐Carboxylate as a Selective Radioligand for the BZ1 Benzodiazepine Receptor Subclass
TLDR
Hofstee analyses of the shallow inhibition curves seen in hippocampus and cerebral cortex when [3H]FNM binding was inhibited by β‐CCE indicate that β‐ CCE and some other β‐carboline‐3‐carboxylate derivatives interact preferentially with a subclass of receptors, and that the percentage of this subclass is equivalent to the number of receptors labelled by [3h]PrCC.
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Results suggest that quazepam is likely to be a safe and effective sleep-promoting agent and potent anticonvulsant activity.
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