Raseglurant

Chemical compound
  • 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 dataFormulaC15H13FN2Molar mass240.281 g·mol−13D model (JSmol)
  • Interactive image
  • 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

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]

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. ^ 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

  • Development of ADX10059 Ended for Long-term Use - Addex Therapeutics
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Group I
mGluR1Tooltip Metabotropic glutamate receptor 1
mGluR5Tooltip Metabotropic glutamate receptor 5
Group II
mGluR2Tooltip Metabotropic glutamate receptor 2
mGluR3Tooltip Metabotropic glutamate receptor 3
Group III
mGluR4Tooltip Metabotropic glutamate receptor 4
  • Antagonists: CPPG
  • MAP4
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
mGluR6Tooltip Metabotropic glutamate receptor 6
  • Antagonists: CPPG
  • MAP4
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
mGluR7Tooltip Metabotropic glutamate receptor 7
  • Antagonists: CPPG
  • MAP4
  • MMPIP
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
  • XAP044; Negative allosteric modulators: ADX71743
mGluR8Tooltip Metabotropic glutamate receptor 8
  • Antagonists: CPPG
  • MAP4
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators


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