Dimdazenil
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| Trade names | Junoenil |
| Other names | EVT-201 |
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| Formula | C17H17ClN6O2 |
| Molar mass | 372.81g·mol−1 |
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Dimdazenil(trade nameJunoenil) is a pharmaceutical drug forinsomnia.[1]It is abenzodiazepinederivativeand a partialpositive allosteric modulator of the GABAAreceptor[2]with two- to four-fold higher functionalaffinityfor theα1subunitrelative to theα2,α3,andα5subunits.
Medical use
[edit]Dimdezenil shows effectiveness in the treatment ofinsomnia,but has lessintrinsic activityin comparison to currently-marketed benzodiazepines and theZ-drugs;[3]however, it is thought that the lower efficacy may result in fewerside effects,such asmotor incoordination.[3]In China, dimdezenil is approved for short-term treatment of insomnia.[4]
History
[edit]Dimdezenil was originally developed byRoche,based onpreclinicaldata, as a non-sedatinganxiolytic,but was found to producesedationin humans inphase Iclinical trials.For this reason, it was subsequently licensed toEvotec,which is now developing it for the treatment of insomnia.[3]By 2007, dimdezenil completedphase IIclinical trials for this indication, with positive findings reported.[5]In China, the drug was developed by Zhejiang Jingxin Pharmaceutical.
References
[edit]- ^Huang Z, Zhan S, Chen C, Zhang R, Zhou Y, He J, et al. (February 2024)."Efficacy and safety of Dimdazenil in adults with insomnia disorder: results from a multicenter, randomized, double-blind, placebo-controlled phase III trials".Sleep.47(2).doi:10.1093/sleep/zsad272.PMC10851846.PMID37875349.
- ^Guilleminault C (2010).Sleep Medicine.Elsevier Health Sciences. pp. 574–.ISBN978-1-4377-1836-2.
- ^abcMonti JM, Pandi-Perumal SR, Möhler H (28 September 2010).GABA and Sleep: Molecular, Functional and Clinical Aspects.Springer Science & Business Media. pp. 50–51.ISBN978-3-0346-0226-6.
- ^Syed YY (March 2024)."Dimdazenil: First Approval".Drugs.doi:10.1007/s40265-024-02020-9.PMID38546956.
- ^Plunkett JW (September 2007).Plunkett's Biotech & Genetics Industry Almanac 2008: Biotech & Genetics Industry Market Research, Statistics, Trends & Leading Companies.Plunkett Research, Ltd. pp. 311–.ISBN978-1-59392-087-6.