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Dimdazenil is a novel, small-molecule, oral partial positive allosteric modulator of the gamma-aminobutyric acid type A (GABA A) receptor. It is structurally classified as a benzodiazepine derivative and was developed to address limitations of full GABA A receptor agonists, such as tolerance, withdrawal symptoms, and adverse effects. Dimdazenil selectively acts on the α1β2γ2 subtype of GABA A receptors with high affinity but moderate maximum activation. This selectivity and partial agonist profile are intended to provide sedative-hypnotic effects for insomnia while minimizing side effects like motor incoordination and dependence risk seen with traditional benzodiazepines or Z-drugs. The drug was originally developed by Roche (as EVT 201), then further developed by Evotec SE in collaboration with Zhejiang Jingxin Pharmaceutical. In November 2023, it received its first approval in China for the short-term treatment of insomnia[1][3][4][7].
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