Desmethylflunitrazepam Explained

Desmethylflunitrazepam (also known as norflunitrazepam, Ro05-4435 and fonazepam) is a benzodiazepine that is a metabolite of flunitrazepam^{[1] [2] [3]} and has been sold online as a designer drug.^{[4] [5]} It has an IC₅₀ value of 1.499 nM for the GABA_A receptor.^{[6] [7]}

See also

• Nitrazolam
• Phenazepam
• List of benzodiazepine designer drugs

Notes and References

1. Busker RW, van Henegouwen GM, Kwee BM, Winkens JH . Photobinding of flunitrazepam and its major photo-decomposition product N-desmethylflunitrazepam. International Journal of Pharmaceutics. May 1987. 113–120. 36. 2–3. 10.1016/0378-5173(87)90145-1.
2. Coller JK, Somogyi AA, Bochner F . Quantification of flunitrazepam's oxidative metabolites, 3-hydroxyflunitrazepam and desmethylflunitrazepam, in hepatic microsomal incubations by high-performance liquid chromatography . Journal of Chromatography. B, Biomedical Sciences and Applications . 719 . 1–2 . 87–92 . November 1998 . 9869368 . 10.1016/S0378-4347(98)00383-1 .
3. Kilicarslan T, Haining RL, Rettie AE, Busto U, Tyndale RF, Sellers EM . Flunitrazepam metabolism by cytochrome P450S 2C19 and 3A4 . Drug Metabolism and Disposition . 29 . 4 Pt 1 . 460–5 . April 2001 . 11259331 .
4. Moosmann B, Bisel P, Franz F, Huppertz LM, Auwärter V . Characterization and in vitro phase I microsomal metabolism of designer benzodiazepines - an update comprising adinazolam, cloniprazepam, fonazepam, 3-hydroxyphenazepam, metizolam and nitrazolam . Journal of Mass Spectrometry . 51 . 11 . 1080–1089 . November 2016 . 27535017 . 10.1002/jms.3840 . 2016JMSp...51.1080M .
5. Katselou M, Papoutsis I, Nikolaou P, Spiliopoulou C, Athanaselis S . Metabolites replace the parent drug in the drug arena. The cases of fonazepam and nifoxipam . Forensic Toxicology . 35 . 1 . 1–10 . 2016 . 28127407 . 5214877 . 10.1007/s11419-016-0338-5 .
6. Maddalena DJ, Johnston GA . Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks . Journal of Medicinal Chemistry . 38 . 4 . 715–24 . February 1995 . 7861419 . 10.1021/jm00004a017 .
7. So SS, Karplus M . Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors . Journal of Medicinal Chemistry . 39 . 26 . 5246–56 . December 1996 . 8978853 . 10.1021/jm960536o .