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Foliglurax

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Foliglurax
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
PubChemCID
ChemSpider
UNII
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 namesPXT-002331,DT2331) is apositive allosteric modulator of themetabotropic glutamate receptor 4 (mGluR4),[1] which is under development by Prexton Therapeutics for the treatment ofParkinson's disease.[2][3][4] It reachedphase IIclinical 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 othertautomeric 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. ^ab"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.
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


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