Foliglurax

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Foliglurax
Foliglurax tautomer skeletal.svg
Clinical data
Other namesDT2331; PXT-002331; PXT-2331
Identifiers
  • 4-[3-[4-nitroso-2-(5H-thieno[3,2-c]pyridin-6-ylidene)chromen-6-yl]propyl]morpholine
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC23H23N3O3S
Molar mass421.52 g·mol−1
3D model (JSmol)
  • C1COCCN1CCCC2=CC3=C(C=C2)OC(=C4C=C5C(=CN4)C=CS5)C=C3N=O
  • InChI=1S/C23H23N3O3S/c27-25-19-13-22(20-14-23-17(15-24-20)5-11-30-23)29-21-4-3-16(12-18(19)21)2-1-6-26-7-9-28-10-8-26/h3-5,11-15,24H,1-2,6-10H2
  • Key:XHRLGFLGWZIPEE-UHFFFAOYSA-N

Foliglurax (developmental code names PXT-002331, DT2331) is a positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4),[1] which is under development by Prexton Therapeutics for the treatment of Parkinson's disease.[2][3][4] It reached phase II clinical trials,[2] but while it was found to be safe and showed some signs of clinical improvement, it failed to sufficiently distinguish itself from placebo to meet the study endpoints.[5][6]

The other tautomeric form of foliglurax.

References[edit]

  1. ^ Charvin D, Pomel V, Ortiz M, Frauli M, Scheffler S, Steinberg E, et al. (October 2017). "Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4". Journal of Medicinal Chemistry. 60 (20): 8515–8537. doi:10.1021/acs.jmedchem.7b00991. PMID 28902994.
  2. ^ a b "Foliglurax - Lundbeck". Adis Insight. Springer Nature Switzerland AG.
  3. ^ Jankovic J, Aguilar LG (August 2008). "Current approaches to the treatment of Parkinson's disease". Neuropsychiatric Disease and Treatment. 4 (4): 743–57. doi:10.1016/j.bmcl.2017.07.075. PMC 2536542. PMID 19043519.
  4. ^ Volpi C, Fallarino F, Mondanelli G, Macchiarulo A, Grohmann U (May 2018). "Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4". Expert Opinion on Drug Discovery. 13 (5): 411–423. doi:10.1080/17460441.2018.1443076. PMID 29486616. S2CID 4572251.
  5. ^ Gonzalez-Latapi P, Bhowmick SS, Saranza G, Fox SH (October 2020). "Non-Dopaminergic Treatments for Motor Control in Parkinson's Disease: An Update". CNS Drugs. 34 (10): 1025–1044. doi:10.1007/s40263-020-00754-0. PMID 32785890. S2CID 221111043.
  6. ^ Rascol O, Medori R, Baayen C, Such P, Meulien D (February 2022). "A Randomized, Double-Blind, Controlled Phase II Study of Foliglurax in Parkinson's Disease". Movement Disorders. 37 (5): 1088–1093. doi:10.1002/mds.28970. PMC 9303267. PMID 35218231. S2CID 247129161.