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Raseglurant

Summary

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
  • 2-[(3-Fluorophenyl)ethynyl]-4,6-dimethyl-3-pyridinamine
CAS Number
  • 757950-09-7
PubChem CID
  • 10331863
ChemSpider
  • 8507323
UNII
  • 66UCJ8Z8L1
CompTox Dashboard (EPA)
  • DTXSID40226707 Edit this at Wikidata
Chemical and physical data
FormulaC15H13FN2
Molar mass240.281 g·mol−1
3D model (JSmol)
  • Interactive image
  • Fc2cccc(C#Cc1nc(cc(c1N)C)C)c2
  • 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 edit

References edit

  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. ^ a b 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.

External links edit

  • Development of ADX10059 Ended for Long-term Use - Addex Therapeutics