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Foliglurax

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Chemical compound Pharmaceutical compound
Foliglurax
Clinical data
Other namesDT2331; PXT-002331; PXT-2331
Identifiers
IUPAC name
  • 4-pyridin-6-ylidene)chromen-6-yl]propyl]morpholine
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC23H23N3O3S
Molar mass421.52 g·mol
3D model (JSmol)
SMILES
  • C1COCCN1CCCC2=CC3=C(C=C2)OC(=C4C=C5C(=CN4)C=CS5)C=C3N=O
InChI
  • 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), which is under development by Prexton Therapeutics for the treatment of Parkinson's disease. It reached phase II clinical trials, 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.

The other tautomeric form of foliglurax.

References

  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. ^ "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.
Metabotropic glutamate receptor modulators
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
mGluR6Tooltip Metabotropic glutamate receptor 6
mGluR7Tooltip Metabotropic glutamate receptor 7
mGluR8Tooltip Metabotropic glutamate receptor 8
See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators


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