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Wikipedia

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
  • 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
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


raseglurant, code, name, 10059, negative, allosteric, modulator, mglu5, receptor, derivative, mpep, which, under, development, addex, therapeutics, treatment, migraine, gastroesophageal, reflux, disease, dental, anxiety, reached, phase, clinical, trials, afore. 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 RaseglurantClinical dataATC codeNoneIdentifiersIUPAC name 2 3 Fluorophenyl ethynyl 4 6 dimethyl 3 pyridinamineCAS Number757950 09 7PubChem CID10331863ChemSpider8507323UNII66UCJ8Z8L1CompTox Dashboard EPA DTXSID40226707Chemical and physical dataFormulaC 15H 13F N 2Molar mass240 281 g mol 13D model JSmol Interactive imageSMILES Fc2cccc C Cc1nc cc c1N C C c2InChI 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 2H3Key MEDCLNYIYBERKO UHFFFAOYSA NSee also editBasimglurant Dipraglurant Fenobam MavoglurantReferences edit Celanire 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 Don t Dodge the Dentist Tips for Dealing with Dental Anxiety Retrieved 2017 04 05 a b Stein MB Steckler T 30 July 2010 Behavioral Neurobiology of Anxiety and Its Treatment Springer Science amp Business Media pp 397 ISBN 978 3 642 02912 7 Dominguez C 18 November 2010 Neurodegenerative Diseases Springer Science amp Business Media pp 120 ISBN 978 3 642 16758 4 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 editDevelopment of ADX10059 Ended for Long term Use Addex Therapeutics nbsp This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Raseglurant amp oldid 1188795444, wikipedia, wiki, book, books, library,

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