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| Anexate, an imidazobenzodiazepine, is a benzodiazepine antagonist which specifically blocks the central effects of agents acting through the benzodiazepine-receptor complex by competitive inhibition. In animal experiments the effects of compounds showing no affinity for the benzodiazepine receptor, e.g. barbiturates, ethanol, meprobamate, GABA mimetics and adenosine receptor agonists, were not affected by Anexate, whereas the effects of non-benzodiazepine agonists of benzodiazepine receptors, such as cyclopyrrolones and triazolo-pyridazines, were blocked. Anexate, a weak lipophilic base, is about 50% bound to plasma proteins. Albumin accounts for two thirds of the plasma protein binding. |
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