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ADX-71441

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
3D model (JSmol)
  • 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).

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

Addiction

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]

Anxiety

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

Pain

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

Tolerance

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

References

  1. ^ "Addex Reports ADX71441 Reduces Alcohol Intake in a Preclinical Model of Chronic Alcohol Dependence". Addex therapeutics. Retrieved 2024-02-03.
  2. ^ 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.
  3. ^ "Addex ADX71441 Positive Results in Preclinical Model of Nicotine Addiction". Addex therapeutics. Retrieved 2024-02-03.
  4. ^ 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.
This page was last edited on 7 February 2024, at 01:25
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