Contrasting regulation by GABA of the displacement of benzodiazepine antagonist binding by benzodiazepine agonists and purines

@article{Skerritt1982ContrastingRB,
  title={Contrasting regulation by GABA of the displacement of benzodiazepine antagonist binding by benzodiazepine agonists and purines},
  author={John H. Skerritt and Les P. Davies and S. Chen Chow and Graham A. R. Johnston},
  journal={Neuroscience Letters},
  year={1982},
  volume={32},
  pages={169-174}
}
Gaba increases the potency of the benzodiazepines chlordiazepoxide, clonazepam, diazepam, nitrazepam and oxazepam, and the triazolopyridazine CL 218,872 in displacing specific binding of the benzodiazepine antagonist [3H]Ro 15-1788. In contrast, the potencies of the purines 1-methyl- and 1-ethylisoguanosine for benzodiazepine antagonist binding sites were decreased by GABA, while the potencies of inosine, hypoxanthine, 6-dimethylaminopurine, and the non-benzodiazepine anxiolytic, zopiclone… Expand
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CHAPTER 17 – SEARCHING FOR ENDOGENOUS LIGAND(S) OF CENTRAL BENZODIAZEPINE RECEPTORS
The discovery, in 1977, of the specific binding sites for benzodiazepines in the brain of mammals, notably in man, lends support to the possible existence of endogenous compounds acting as naturalExpand
Searching for endogenous ligand(s) of central benzodiazepine receptors
TLDR
The most recent data concerning benzodiazepine receptors suggest that the endogenous ligand would be, if it exists, a benzidiazepine-like compound (agonist) with an indolic structure. Expand
Molecular aspects of the action of benzodiazepine and nonbenzodiazepine anxiolytics: A hypothetical allosteric model of the benzodiazepine receptor complex
  • M. Williams
  • Medicine, Chemistry
  • Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 1984
TLDR
The majority of available evidence would indicate that the endogenous ligand for the Benzodiazepine receptor(s) is an antagonist of the benzodiazepines and other putative anxiolytic agents. Expand
Benzodiazepine receptor ligands with positive and negative efficacy.
TLDR
Biochemical studies, supported by published electrophysiological data, indicate that the benzodiazepine receptor allosterically up- or down-regulates the gain in the GABAergic system depending on the nature of the ligand. Expand
Benzodiazepine receptor ligands with positive and negative efficacy
TLDR
Biochemical studies, supported by published electrophysiological data, indicate that the benzodiazepine receptor allosterically up- or down-regulates the gain in the GABAergic system depending on the nature of the ligand. Expand
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