From Wikipedia, the free encyclopedia
ADX71441
|
Names
|
IUPAC name
N-[5-[4-[(4-chloro-3-fluorophenyl)methyl]-6-methoxy-3,5-dioxo-1,2,4-triazin-2-yl]-2-fluorophenyl]acetamide
|
Identifiers
|
|
|
|
|
|
|
Key: BQDMEJYNGXEHSW-UHFFFAOYSA-N InChI=1S/C19H15ClF2N4O4/c1-10(27)23-16-8-12(4-6-14(16)21)26-19(29)25(18(28)17(24-26)30-2)9-11-3-5-13(20)15(22)7-11/h3-8H,9H2,1-2H3,(H,23,27)
|
CC(=O)NC1=C(C=CC(=C1)N2C(=O)N(C(=O)C(=N2)OC)CC3=CC(=C(C=C3)Cl)F)F
|
Properties
|
|
C19H15ClF2N4O4
|
Molar mass
|
436.80 g·mol−1
|
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
|
Chemical compound
ADX-71441 is a GABAB receptor positive allosteric modulator currently being investigated as a potential treatment for anxiety, epilepsy, pain and other conditions.
Therapeutic potential
[edit]
ADX-71441 has been shown to reduce alcohol consumption.[1] This result was observed in both alcohol dependent and non-dependent animals.[2]
There were also trials about nicotine addiction, which showed positive results: ADX-71441 was able to decrease some withdrawal symptoms of nicotine withdrawal.[3]
This compound has also been shown to reduce anxiety in people with PTSD.[4]
Experiments have shown that this compound was able to decrease hypersensitivity to pain in mice, Guinea pigs and rats.[4]
ADX-71441 has been shown to have less tolerance and side effects than direct GABAB agonists, such as baclofen.[2]
- ^ "Addex Reports ADX71441 Reduces Alcohol Intake in a Preclinical Model of Chronic Alcohol Dependence". Addex therapeutics. Retrieved 2024-02-03.
- ^ a b Augier, Eric; Dulman, Russell S.; Damadzic, Ruslan; Pilling, Andrew; Hamilton, J. Paul; Heilig, Markus (August 2017). "The GABAB Positive Allosteric Modulator ADX71441 Attenuates Alcohol Self-Administration and Relapse to Alcohol Seeking in Rats". Neuropsychopharmacology. 42 (9): 1789–1799. doi:10.1038/npp.2017.53. ISSN 1740-634X. PMC 5520784. PMID 28294133.
- ^ "Addex ADX71441 Positive Results in Preclinical Model of Nicotine Addiction". Addex therapeutics. Retrieved 2024-02-03.
- ^ a b Kalinichev, Mikhail; Girard, Françoise; Haddouk, Hasnaà; Rouillier, Mélanie; Riguet, Eric; Royer-Urios, Isabelle; Mutel, Vincent; Lütjens, Robert; Poli, Sonia (2017). "The drug candidate, ADX71441, is a novel, potent and selective positive allosteric modulator of the GABAB receptor with a potential for treatment of anxiety, pain and spasticity". Neuropharmacology. 114: 34–47. doi:10.1016/j.neuropharm.2016.11.016. PMID 27889489. S2CID 36606154.
|
---|
Ionotropic | GABAATooltip γ-Aminobutyric acid A receptor |
- Positive modulators (abridged; see here for a full list): α-EMTBL
- Alcohols (e.g., drinking alcohol, 2M2B)
- Anabolic steroids
- Avermectins (e.g., ivermectin)
- Barbiturates (e.g., phenobarbital)
- Benzodiazepines (e.g., diazepam)
- Bromide compounds (e.g., potassium bromide)
- Carbamates (e.g., meprobamate)
- Carbamazepine
- Chloralose
- Chlormezanone
- Clomethiazole
- Dihydroergolines (e.g., ergoloid (dihydroergotoxine))
- Etazepine
- Etifoxine
- Fenamates (e.g., mefenamic acid)
- Flavonoids (e.g., apigenin, hispidulin)
- Fluoxetine
- Flupirtine
- Imidazoles (e.g., etomidate)
- Kava constituents (e.g., kavain)
- Lanthanum
- Loreclezole
- Monastrol
- Neuroactive steroids (e.g., allopregnanolone, cholesterol, THDOC)
- Niacin
- Niacinamide
- Nonbenzodiazepines (e.g., β-carbolines (e.g., abecarnil), cyclopyrrolones (e.g., zopiclone), imidazopyridines (e.g., zolpidem), pyrazolopyrimidines (e.g., zaleplon))
- Norfluoxetine
- Petrichloral
- Phenols (e.g., propofol)
- Phenytoin
- Piperidinediones (e.g., glutethimide)
- Propanidid
- Pyrazolopyridines (e.g., etazolate)
- Quinazolinones (e.g., methaqualone)
- Retigabine (ezogabine)
- ROD-188
- Skullcap constituents (e.g., baicalin)
- Stiripentol
- Sulfonylalkanes (e.g., sulfonmethane (sulfonal))
- Topiramate
- Valerian constituents (e.g., valerenic acid)
- Volatiles/gases (e.g., chloral hydrate, chloroform, diethyl ether, paraldehyde, sevoflurane)
- Negative modulators: 1,3M1B
- 3M2B
- 11-Ketoprogesterone
- 17-Phenylandrostenol
- α3IA
- α5IA (LS-193,268)
- β-CCB
- β-CCE
- β-CCM
- β-CCP
- β-EMGBL
- Anabolic steroids
- Amiloride
- Anisatin
- β-Lactams (e.g., penicillins, cephalosporins, carbapenems)
- Basmisanil
- Bemegride
- Bicyclic phosphates (TBPS, TBPO, IPTBO)
- BIDN
- Bilobalide
- Bupropion
- CHEB
- Chlorophenylsilatrane
- Cicutoxin
- Cloflubicyne
- Cyclothiazide
- DHEA
- DHEA-S
- Dieldrin
- (+)-DMBB
- DMCM
- DMPC
- EBOB
- Etbicyphat
- FG-7142 (ZK-31906)
- Fiproles (e.g., fipronil)
- Flavonoids (e.g., amentoflavone, oroxylin A)
- Flumazenil
- Fluoroquinolones (e.g., ciprofloxacin)
- Flurothyl
- Furosemide
- Golexanolone
- Iomazenil (123I)
- IPTBO
- Isopregnanolone (sepranolone)
- L-655,708
- Laudanosine
- Lindane
- MaxiPost
- Morphine
- Morphine-3-glucuronide
- MRK-016
- Naloxone
- Naltrexone
- Nicardipine
- Nonsteroidal antiandrogens (e.g., apalutamide, bicalutamide, enzalutamide, flutamide, nilutamide)
- Oenanthotoxin
- Pentylenetetrazol (pentetrazol)
- Phenylsilatrane
- Picrotoxin (i.e., picrotin, picrotoxinin and dihydropicrotoxinin)
- Pregnenolone sulfate
- Propybicyphat
- PWZ-029
- Radequinil
- Ro 15-4513
- Ro 19-4603
- RO4882224
- RO4938581
- Sarmazenil
- SCS
- Suritozole
- TB-21007
- TBOB
- TBPS
- TCS-1105
- Terbequinil
- TETS
- Thujone
- U-93631
- Zinc
- ZK-93426
|
---|
GABAA-ρTooltip γ-Aminobutyric acid A-rho receptor | |
---|
|
---|
Metabotropic | GABABTooltip γ-Aminobutyric acid B receptor | |
---|
|
---|
|