Dimdazenil

Dimdazenil (trade name Junoenil) is a pharmaceutical drug for insomnia.^[1] It is a benzodiazepine derivative and a partial positive allosteric modulator of the GABA_A receptor^[2] with two- to four-fold higher functional affinity for the α₁ subunit relative to the α₂, α₃, and α₅ subunits.

Dimdazenil

Clinical data
Trade names	Junoenil
Other names	EVT-201
Legal status
Legal status	Rx in China
Identifiers
IUPAC name 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	308239-86-3
PubChem CID	9885841
DrugBank	DB05721
ChemSpider	8061514
UNII	6J8AF7CLE4
ChEMBL	ChEMBL5095096
CompTox Dashboard (EPA)	DTXSID301032055
Chemical and physical data
Formula	C17H17ClN6O2
Molar mass	372.81 g·mol−1
3D model (JSmol)	Interactive image
SMILES Clc4cccc3n2cnc(c1nc(on1)CN(C)C)c2CN(C(=O)c34)C
InChI 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

Medical use

Dimdezenil 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, dimdezenil is approved for short-term treatment of insomnia.^[4]

History

Dimdezenil 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, dimdezenil completed phase II clinical trials for this indication, with positive findings reported.^[5] In China, the drug was developed by Zhejiang Jingxin Pharmaceutical.

References

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. 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.

External links

• Dimdazenil - AdisInsight