Raseglurant

Raseglurant (INN) (code name ADX-10059) is a negative allosteric modulator of the mGlu5 receptor and derivative of MPEP which was under development by Addex Therapeutics for the treatment of migraine, gastroesophageal reflux disease, and dental anxiety.[1][2][3] It reached phase II clinical trials for all of the aforementioned indications before being discontinued due to the observation of possible predictive signs of hepatotoxicity in patients with long-term use.[3][4][5]

Raseglurant
Clinical data
ATC code
  • None
Identifiers
IUPAC name
  • 2-[(3-Fluorophenyl)ethynyl]-4,6-dimethyl-3-pyridinamine
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H13FN2
Molar mass240.281 g·mol−1
3D model (JSmol)
SMILES
  • Fc2cccc(C#Cc1nc(cc(c1N)C)C)c2
InChI
  • InChI=1S/C15H13FN2/c1-10-8-11(2)18-14(15(10)17)7-6-12-4-3-5-13(16)9-12/h3-5,8-9H,17H2,1-2H3
  • Key:MEDCLNYIYBERKO-UHFFFAOYSA-N

See also

References

  1. Célanire S, Duvey G, Poli S, Rocher JP (January 2012). "mGluR2 activators and mGluR5 blockers advancing in the clinic for major CNS disorders.". Annual Reports in Medicinal Chemistry. Vol. 47. Academic Press. pp. 71–88. ISBN 978-0-12-397214-9.
  2. "Don't Dodge the Dentist – Tips for Dealing with Dental Anxiety". Retrieved 2017-04-05.
  3. Stein MB, Steckler T (30 July 2010). Behavioral Neurobiology of Anxiety and Its Treatment. Springer Science & Business Media. pp. 397–. ISBN 978-3-642-02912-7.
  4. Dominguez C (18 November 2010). Neurodegenerative Diseases. Springer Science & Business Media. pp. 120–. ISBN 978-3-642-16758-4.
  5. Shaheen NJ (25 March 2013). Benign and Neoplastic Conditions of the Esophagus, An Issue of Gastroenterology Clinics. Elsevier Health Sciences. pp. 119–. ISBN 978-1-4557-7175-2.


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