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Chemical compound
EVT-201![](//upload.wikimedia.org/wikipedia/commons/thumb/a/ac/EVT-201.svg/223px-EVT-201.svg.png) |
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7-Chloro-3-{5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl}-5-methyl-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-one
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Formula | C17H17ClN6O2 |
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Molar mass | 372.81 g·mol−1 |
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3D model (JSmol) | |
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Clc4cccc3n2cnc(c1nc(on1)CN(C)C)c2CN(C(=O)c34)C
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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
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EVT-201 is a benzodiazepine derivative drug and partial positive allosteric modulator of the benzodiazepine site of the GABAA receptor.[1] It has 2–4-fold higher functional affinity for the α1 subunit relative to the α2, α3, and α5 subunits and significantly less intrinsic activity in comparison to currently-marketed benzodiazepines and the Z-drugs.[2] Despite the lower efficacy, EVT-201 still shows effectiveness in the treatment of insomnia, and it is thought that the lower efficacy may result in fewer side effects, such as motor incoordination.[2] The drug 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.[2] As of 2007[update], EVT-201 has completed phase II clinical trials for this indication, with positive findings reported.[3] As of August 2015[update], Phase II development is ongoing in China.[4]
See also
References
External links
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GABAA receptor positive modulators |
- Others: Alcohols (e.g., ethchlorvynol, amylene hydrate, ethanol)
- Barbiturates (e.g., amobarbital, pentobarbital, phenobarbital, secobarbital)
- Bromides (e.g., potassium bromide, sodium bromide)
- Carbamates (e.g., meprobamate)
- Chloral hydrate
- Clomethiazole
- Kava
- Neurosteroids (e.g., progesterone, zuranolone†)
- Paraldehyde
- Piperidinediones (e.g., glutethimide)
- Quinazolinones (e.g., methaqualone)
- Sulfonmethane
- Valerian
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Antihistamines (H1 receptor inverse agonists) | |
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Orexin receptor antagonists | |
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Melatonin receptor agonists | |
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Miscellaneous |
- Antipsychotics (e.g., quetiapine, olanzapine, risperidone, chlorpromazine)
- Ashwagandha
- Benzoctamine
- Cannabinoids (e.g., cannabis, dronabinol (THC), nabilone)
- Chamomile
- Fenadiazole
- Gabapentinoids (e.g., gabapentin, pregabalin, phenibut)
- Hops
- Lavender
- Menthyl isovalerate
- Niaprazine
- Opioids (e.g., hydrocodone, oxycodone, morphine)
- Passion flower
- Scopolamine
- Serotonin precursors (tryptophan, 5-HTPTooltip 5-hydroxytryptophan)
- Sodium oxybate (GHB)
- Sympatholytics (e.g., clonidine, guanfacine, prazosin)
- Theanine
- Trazodone
- Tricyclic antidepressants (e.g., amitriptyline, doxepin, trimipramine)
- Tetracyclic antidepressants (e.g., mirtazapine)
- Valnoctamide
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Alcohols | |
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Barbiturates | |
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Benzodiazepines | |
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Carbamates | |
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Flavonoids | |
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Imidazoles | |
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Kava constituents | |
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Monoureides | |
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Neuroactive steroids | |
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Nonbenzodiazepines | |
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Phenols | |
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Piperidinediones | |
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Pyrazolopyridines | |
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Quinazolinones | |
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Volatiles/gases | |
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Others/unsorted |
- 3-Hydroxybutanal
- α-EMTBL
- AA-29504
- Alogabat
- Avermectins (e.g., ivermectin)
- Bromide compounds (e.g., lithium bromide, potassium bromide, sodium bromide)
- Carbamazepine
- Chloralose
- Chlormezanone
- Clomethiazole
- Darigabat
- DEABL
- Deuterated etifoxine
- Dihydroergolines (e.g., dihydroergocryptine, dihydroergosine, dihydroergotamine, ergoloid (dihydroergotoxine))
- DS2
- Efavirenz
- Etazepine
- Etifoxine
- Fenamates (e.g., flufenamic acid, mefenamic acid, niflumic acid, tolfenamic acid)
- Fluoxetine
- Flupirtine
- Hopantenic acid
- KRM-II-81
- Lanthanum
- Lavender oil
- Lignans (e.g., 4-O-methylhonokiol, honokiol, magnolol, obovatol)
- Loreclezole
- Menthyl isovalerate (validolum)
- Monastrol
- Niacin
- Niacinamide
- Org 25,435
- Phenytoin
- Propanidid
- Retigabine (ezogabine)
- Safranal
- Seproxetine
- Stiripentol
- Sulfonylalkanes (e.g., sulfonmethane (sulfonal), tetronal, trional)
- Terpenoids (e.g., borneol)
- Topiramate
- Valerian constituents (e.g., isovaleric acid, isovaleramide, valerenic acid, valerenol)
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