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Dimdazenil
Dimdazenil
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Dimdazenil
Dimdazenil
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Dimdazenil

Dimdazenil
200px
Clinical data
Trade namesJunoenil
Other namesEVT-201; EVT201
Legal status
Legal status
  • Rx in China
Identifiers
  • 7-Chloro-3-[5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl]-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H17ClN6O2
Molar mass372.81 g·mol−1
3D model (JSmol)
  • Clc4cccc3n2cnc(c1nc(on1)CN(C)C)c2CN(C(=O)c34)C
  • InChI=1S/C17H17ClN6O2/c1-22(2)8-13-20-16(21-26-13)15-12-7-23(3)17(25)14-10(18)5-4-6-11(14)24(12)9-19-15/h4-6,9H,7-8H2,1-3H3
  • Key:JCYLWUVDHLVGER-UHFFFAOYSA-N

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

[edit]

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

[edit]

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

[edit]
  1. ^ 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. PMC 10851846. PMID 37875349.
  2. ^ Guilleminault C (2010). Sleep Medicine. Elsevier Health Sciences. pp. 574–. ISBN 978-1-4377-1836-2.
  3. ^ a b c Monti JM, Pandi-Perumal SR, Möhler H (28 September 2010). GABA and Sleep: Molecular, Functional and Clinical Aspects. Springer Science & Business Media. pp. 50–51. ISBN 978-3-0346-0226-6.
  4. ^ Syed YY (March 2024). "Dimdazenil: First Approval". Drugs. doi:10.1007/s40265-024-02020-9. PMID 38546956.
  5. ^ 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–. ISBN 978-1-59392-087-6.
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