Unusual interactions of benzodiazepine receptor antagonists

@article{Nutt1982UnusualIO,
  title={Unusual interactions of benzodiazepine receptor antagonists},
  author={David J. Nutt and Philip J. Cowen and Hilary J. Little},
  journal={Nature},
  year={1982},
  volume={295},
  pages={436-438}
}
Two compounds have recently been described which act as potent benzodiazepine (BDZ) antagonists in vivo and which, in vitro, show high affinity and selectivity for the BDZ receptor of the mammalian central nervous system (CNS). One, ethyl β-carboline-3-carboxylate (β-CCE), was extracted from human urine and may be related to an endogenous ligand for the BDZ receptor1–3. It reverses the effects of BDZs in vivo4,5 and in vitro6, but also has intrinsic activity, as it lowers the seizure threshold… Expand
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TLDR
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. Expand
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The main properties of a representative of this novel class of specific benzodiazepine antagonists are described, whose unique pharmacological activity is to prevent or abolish in a highly selective manner at the receptor level all the characteristic centrally mediated effects of active Benzodiazepines. Expand
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TLDR
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. Expand
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