Revision as of 17:58, 17 July 2022 by imported>WikiGary
(diff) ← Older revision | Latest revision (diff) | Newer revision → (diff)
Short description: Chemical compound
EVT-201 |
Clinical data |
---|
ATC code | |
---|
Identifiers |
---|
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
|
CAS Number | |
---|
PubChem CID | |
---|
ChemSpider | |
---|
UNII | |
---|
Chemical and physical data |
---|
Formula | C17H17ClN6O2 |
---|
Molar mass | 372.81 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
|
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), EVT-201 has completed phase II clinical trials for this indication, with positive findings reported.[3] (As of August 2015), Phase II development is ongoing in China .[4]
See also
References
External links
|
---|
GABAAR PAMs |
- Benzodiazepines: Brotizolam
- Cinolazepam
- Climazolam
- Clorazepate
- Doxefazepam
- Estazolam
- Etizolam
- Flunitrazepam
- Flurazepam
- Flutoprazepam
- Haloxazolam
- Loprazolam
- Lormetazepam
- Midazolam
- Nimetazepam
- Nitrazepam
- Quazepam
- Temazepam
- Triazolam; Nonbenzodiazepines/[[Chemistry:Z-drug|]] Eszopiclone
- Zaleplon
- Zolpidem
- Zopiclone; 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
- Paraldehyde
- Piperidinediones (e.g., glutethimide)
- Quinazolinones (e.g., methaqualone)
- Sulfonmethane
- Valerian
|
---|
Antihistamines (H1R inverse agonists) | |
---|
OXR antagonists | |
---|
MTR agonists | |
---|
Miscellaneous |
- Antipsychotics (e.g., quetiapine, olanzapine, 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-HTP)
- Sodium oxybate (GHB)
- Sympatholytics (e.g., clonidine, guanfacine)
- TCAs (e.g., amitriptyline, doxepin, trimipramine)
- TeCAs (e.g., mirtazapine)
- Theanine
- Trazodone
- Valnoctamide
|
---|
|
---|
Alcohols | |
---|
Barbiturates | |
---|
Benzodiazepines | |
---|
Carbamates | |
---|
Flavonoids | |
---|
Imidazoles | |
---|
Kava constituents | |
---|
Monoureides | |
---|
Neuroactive steroids | |
---|
Nonbenzodiazepines | |
---|
Phenols | |
---|
Piperidinediones | |
---|
Pyrazolopyridines | |
---|
Quinazolinones | |
---|
Volatiles/gases | |
---|
Others/unsorted |
- 3-Hydroxybutanal
- α-EMTBL
- AA-29504
- Avermectins (e.g., ivermectin)
- Bromide compounds (e.g., lithium bromide, potassium bromide, sodium bromide)
- Carbamazepine
- Chloralose
- Chlormezanone
- Clomethiazole
- DEABL
- 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
- Lanthanum
- Lavender oil
- Lignans (e.g., 4-O-methylhonokiol, honokiol, magnolol, obovatol)
- Loreclezole
- Menthyl isovalerate (validolum)
- Monastrol
- Niacin
- Nicotinamide (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)
|
---|
|
| Original source: https://en.wikipedia.org/wiki/EVT-201. Read more |