Chemistry:Dimdazenil
Dimdazenil, sold under the brand name Junoenil, is a medication used in the treatment of insomnia in China.[1] It is a benzodiazepine derivative and a partial positive allosteric modulator of the GABAA receptor[2] with two- to four-fold higher functional affinity for the α1 subunit relative to the α2, α3, and α5 subunits.
Medical use
Dimdazenil shows effectiveness in the treatment of insomnia, but has less intrinsic activity in comparison to currently-marketed benzodiazepines and the Z-drugs;[3] however, it is thought that the lower efficacy may result in fewer side effects, such as motor incoordination.[3] In China, dimdazenil is approved for short-term treatment of insomnia.[4]
History
Dimdazenil was originally developed by Roche, based on preclinical data, as a non-sedating anxiolytic, but was found to produce sedation in humans in phase I clinical trials. For this reason, it was subsequently licensed to Evotec, which is now developing it for the treatment of insomnia.[3] By 2007, dimdazenil completed phase II clinical trials for this indication, with positive findings reported.[5] In China, the drug was developed by Zhejiang Jingxin Pharmaceutical.
References
- ↑ "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). February 2024. doi:10.1093/sleep/zsad272. PMID 37875349.
- ↑ Sleep Medicine. Elsevier Health Sciences. 2010. pp. 574–. ISBN 978-1-4377-1836-2. https://books.google.com/books?id=np1NaFTF_CQC&pg=PA574.
- ↑ 3.0 3.1 3.2 GABA and Sleep: Molecular, Functional and Clinical Aspects. Springer Science & Business Media. 28 September 2010. pp. 50–51. ISBN 978-3-0346-0226-6. https://books.google.com/books?id=u54tqIOP8RUC&pg=PA50.
- ↑ "Dimdazenil: First Approval". Drugs. March 2024. doi:10.1007/s40265-024-02020-9. PMID 38546956. https://figshare.com/articles/online_resource/Dimdazenil_First_Approval/25355965.
- ↑ Plunkett's Biotech & Genetics Industry Almanac 2008: Biotech & Genetics Industry Market Research, Statistics, Trends & Leading Companies. Plunkett Research, Ltd.. September 2007. pp. 311–. ISBN 978-1-59392-087-6. https://books.google.com/books?id=3BGBibHJ1FYC&pg=PT311.
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