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Contents

(Top) 1 Therapeutic potential 1.1 Addiction 1.2 Anxiety 1.3 Pain 2 Tolerance 3 References

ADX-71441

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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
CAS Number	1207440-88-7
3D model (JSmol)	Interactive image
PubChem CID	25106292
InChI 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)
SMILES CC(=O)NC1=C(C=CC(=C1)N2C(=O)N(C(=O)C(=N2)OC)CC3=CC(=C(C=C3)Cl)F)F
Properties
Chemical formula	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). Infobox references

ADX-71441 is a GABA_B receptor positive allosteric modulator currently being investigated as a potential treatment for anxiety, epilepsy, pain and other conditions.

Therapeutic potential

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Addiction

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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 symptomsofnicotine withdrawal.^[3]

Anxiety

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This compound has also been shown to reduce anxiety in people with PTSD.^[4]

Pain

[edit]

Experiments have shown that this compound was able to decrease hypersensitivity to pain in mice, Guinea pigs and rats.^[4]

Tolerance

[edit]

ADX-71441 has been shown to have less tolerance and side effects than direct GABA_B agonists, such as baclofen.^[2]

References

[edit]

^ "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 GABA_B 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.

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GABA receptor modulators

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: 5α-Dihydroprogesterone
Bilobalide
Loreclezole
Picrotoxin (picrotin, picrotoxinin)
Pregnanolone
ROD-188
THDOC
Zinc

Negative modulators: Compound 14

See also: Receptor/signaling modulators; GABA_A receptor positive modulators; GABA metabolism/transport modulators

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