In fact, Imidazenil blocks the sedative effects of diazepam, yet without lowering the convulsion threshold, and so potentially could be a more flexible antidote than the antagonist flumazenil which is commonly used to treat benzodiazepine overdose at present. Imidazenil is a highly potent benzodiazepine receptor partial agonist with an unusual profile of effects, producing some of the effects associated with normal benzodiazepines such as anticonvulsant and anxiolytic effects, yet without any notable sedative or amnestic effects. Imidazenil is an experimental anxiolytic drug which is derived from the benzodiazepine family, and is most closely related to other imidazobenzodiazepines such as midazolam, flumazenil, and bretazenil. There is evidence that α1 containing GABAA receptors directly contributes to the downstream effects of tolerance because α1 (H101R) mice have been shown to maintain expressions in neuroplasticity-coding transcripts after diazepam administration.120 This perfectly agrees with data from animal studies regarding the lack of tolerance in α1 subtype inactive compounds such as TPA023B and imidazenil.121–126 Future drug discovery involving tranquilizers should look for partial agonists of α2, α3, and α5 containing GABAA receptors Valium without its side effects is potentially achievable. In the light of current evidence, α1 dormant, α2, α3, and α5 subtype partial agonists not only possess low abuse potential but are also low or devoid of tolerance building. Valium without dependence? Individual GABAA receptor subtype contribution toward benzodiazepine addiction, tolerance, and therapeutic effects
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