Enhancement of γ‐Aminobutyric Acid Binding by Quazepam, a Benzodiazepine Derivative with Preferential Affinity for Type I Benzodiazepine Receptors

  title={Enhancement of $\gamma$‐Aminobutyric Acid Binding by Quazepam, a Benzodiazepine Derivative with Preferential Affinity for Type I Benzodiazepine Receptors},
  author={M. G. Corda and Enrico Sanna and A Concas and Osvaldo Giorgi and Ennio Ongini and Valeria Marina Nurchi and Teresa Pintori and Guido Crisponi and Giovanni Biggio},
  journal={Journal of Neurochemistry},
Abstract: We evaluated the effect of the two N‐trifluoroethyl benzodiazepines, quazepam and its 2‐oxo metabolite SCH 15725, which possess preferential affinity for type I benzodiazepine recognition sites, on the binding of [3H]γ‐aminobutyric acid ([3H]GABA) to rat brain membrane preparations. The study also included compounds such as diazepam and N‐desalkyl‐2‐oxoquazepam (SCH 17514), which have equal affinity for the type I and type II receptor subtypes. Binding of [3H]GABA was studied in… 
17 Citations
Distribution and Pharmacological Properties of the GABAA/ Benzodiazepine/Chloride Ionophore Receptor Complex in the Brain of the Fish Anguilla anguilla
Abstract: In the present study, we characterized the distribution and the pharmacological properties of the different components of the GABAA receptor complex in the brain of the eel (Anguilla
Modulation of GABA-gated chloride ion flux in rat brain by acute and chronic benzodiazepine administration.
The results show that benzodiazepine tolerance involves reduced functional coupling between the benzodiazine recognition site and the GABA recognition site-Cl- channel, which might result from alterations in neuronal activity that occur subsequently to activation of the GABA receptor-gated anion channel.


[3H]Propyl β‐Carboline‐3‐Carboxylate as a Selective Radioligand for the BZ1 Benzodiazepine Receptor Subclass
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.
Two distinct solubilized benzodiazepine receptors: differential modulation by ions
  • M. Lo, S. Snyder
  • Biology, Chemistry
    The Journal of neuroscience : the official journal of the Society for Neuroscience
  • 1983
Modulation of solubilized type 1 and type 2 benzodiazepine receptors from cow brain by gamma-aminobutyric acid, divalent cations, and anions suggests that they may exert their modulating effects on type 2 receptors through different mechanisms.
Enhancement of GABA binding by benzodiazepines and related anxiolytics.
Increase in the Bmax of gamma-aminobutyric acid-A recognition sites in brain regions of mice receiving diazepam.
It is proposed that the facilitatory action on GABAergic transmission elicited in vivo by diazepam is mediated by an increase in the Bmax of the binding sites of GABAA receptors.
beta-Carbolines enhance shock-induced suppression of drinking in rats.
Pentylenetetrazole, which causes convulsions by interacting with a subunit of the gamma-aminobutyric acid receptor that is different from the benzodiazepine recognition site, induces a proconflict action that is antagonized by anxiolytic Benzodiazepines but not by RO 15-1788.
Stress and β-carbolines decrease the density of low affinity gaba binding sites An effect reversed by diazepam
Interaction of convulsive ligands with benzodiazepine receptors.
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.