Pharmacological characterization of benzodiazepine receptors in the brain.

  title={Pharmacological characterization of benzodiazepine receptors in the brain.},
  author={Claus Braestrup and Richard Felt Squires},
  journal={European journal of pharmacology},
  volume={48 3},
Benzodiazepine receptor binding: the interactions of some non-benzodiazepine drugs with specific [3H] diazepam binding to rat brain synaptosomal membranes
It is suggested that interactions with benzodiazepine receptors may account for the anxiolytic and anticonvulsive side effects of this drug.
Benzodiazepine and GABA receptors are functionally related: Further electrophysiological evidence in vivo
  • J. Nestoros
  • Biology, Chemistry
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 1982
Is Receptor Heterogeneity Relevant to the Anxiolytic Actions of Benzodiazepine Receptor Ligands
This chapter will critically review the relationship of receptor heterogeneity to the putative ‘anxioselective’ actions of BDZR ligands.
Ethyl β-carboline-3-carboxylate shows differential benzodiazepine receptor interaction
It is reported here that β-CCE, in contrast to Benzodiazepines, can distinguish clearly between benzodiazepine receptors in cerebellum and hippocampus, which strongly indicates that benzodiazine receptors are not a single class of non-interacting entities.
Receptor-mediated model relating anticonvulsant effect to brain levels of camazepam in the presence of its active metabolites
A receptor-mediated model, including the Langmuir equation to describe the receptor binding-brain concentration relationship and the Hill equation to accommodate the anticonvulsant effect-receptor binding relationship, was constructed and was found to adequately relate the time course values of anticonVulsan effect and of brain levels of CZ and its active metabolites after oral administration.
Ethyl β-carboline carboxylate lowers seizure threshold and antagonizes flurazepam-induced sedation in rats
It is reported here that, in contrast to the benzodiazepines, β-CCE lowers seizure threshold and reverses the sedative effect of flurazepam, and if β- CCE has a close structural relationship to the endogenous ligand, benzodiazines may be antagonistic at the receptor site.


Benzodiazepine receptors in rat brain
Experiments suggest that another important group of psychoactive drugs, the benzodiazepines, bind to specific receptors on the membranes of rat brain cells, and this suggests that there may be an unknown endogenous neurotransmitter which is the natural ligand for the Benzodiazepine receptor.
Pharmacological studies on new potent central depressants, 8-chloro-6-phenyl-4H-s-triazolo [4,3a][1,4] benzodiazepine (D-40tA) and its 1-methyl analogue (D-65MT).
Two compounds, 8-chloro-6-phenyl-4H-s-triazolo and its 1-methyl analogue (D-65MT) were undergone more detailed pharmacological evaluation of effects on central nervous system, in comparison with other benzodiazepines and chlorpromazine.
High densities of benzodiazepine receptors in human cortical areas
It is reported here that benzodiazepine receptors are also present in the human brain, that the cerebral and cerebellar cortical regions contain the highest densities of binding sites and that the receptors in human brain are very similar to those in rat brain.
Benzodiazepine receptor: demonstration in the central nervous system
Competition for the receptor by various benzodiazepines closely parallels their pharmacological potency, and binding to the receptor is stereospecific.
Selective enhancement of [3H]opiate agonist binding by divalent cations.
There is a good correlation between the sensitivity of opiate receptor binding to sodium and manganese and the potency of sodium in inhibiting [3H]dihydromorphine binding is reduced 5-fold by the addition ofManganese ions.
Opiate Agonists and Antagonists Discriminated by Receptor Binding in Brain
Sodium enhances antagonist binding in vitro but decreases agonist binding, a qualitative difference that may be relevant to the divergent pharmacological properties of opiate agonists and antagonists.
Morphine-like peptides, leucine enkephalin and methionine enkephalin: interactions with the opiate receptor.
The morphine-like peptides leucine enkephalin and methionine enkephalin compete for opiate receptor binding with affinities resembling that of morphine. In the absence of added sodium, methionine