An internal standard for the quantification of flumazenil
Flumazenil-d5 is intended for use as an internal standard for the quantification of flumazenil by GC- or LC-MS. Flumazenil is an imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors with an IC50 value of 2 nM.1 Flumazenil is non-selective for α1, α2, α3, or α5 subunit-containing GABAA receptors and antagonizes the actions of benzodiazepines on the central nervous system without producing the behavioral or neurological effects typical of the benzodiazepines.1,2 Formulations containing flumazenil have been used to reverse sedation induced by benzodiazepines and in the treatment of benzodiazepine overdose or withdrawal.
参考文献
1. Hunkeler, W., M?hler, H., Pieri, L., et al. Selective antagonists of benzodiazepines. Nature 290(5806), 514-516 (1981).
2. Atack, J.R., Smith, A.J., Emms, F., et al. Regional differences in the inhibition of mouse in vivo [3H]Ro 15-1788 binding reflect selectivity for α1 versus α2 and α3 subunit-containing GABAA receptors. Neuropsychopharmacology 20(3), 255-262 (1999).
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