ADX88178

Last updated

ADX88178
ADX88178.svg
Identifiers
  • 5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)-1,3-thiazol-2-amine
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
Formula C12H12N6S
Molar mass 272.33 g·mol−1
3D model (JSmol)
  • CC1=NC(=NC=C1)NC2=NC(=C(S2)C)C3=CNN=C3
  • InChI=1S/C12H12N6S/c1-7-3-4-13-11(16-7)18-12-17-10(8(2)19-12)9-5-14-15-6-9/h3-6H,1-2H3,(H,14,15)(H,13,16,17,18)
  • Key:MIQNXKWDQRNHAU-UHFFFAOYSA-N

ADX88178 is an experimental drug that acts as a positive allosteric modulator for the glutamate receptor mGluR4. It was developed as a potential medication for the treatment of Parkinson's disease but had mixed results in animal studies, improving dyskinesia but worsening psychosis-like symptoms. However it has antiinflammatory effects in brain tissue which may make it useful for other indications. [1] [2] [3] [4] [5] [6]

References

  1. ↑ Le Poul E, Boléa C, Girard F, Poli S, Charvin D, Campo B, et al. (October 2012). "A potent and selective metabotropic glutamate receptor 4 positive allosteric modulator improves movement in rodent models of Parkinson's disease". The Journal of Pharmacology and Experimental Therapeutics. 343 (1): 167–177. doi:10.1124/jpet.112.196063. PMID   22787118.
  2. ↑ Kalinichev M, Le Poul E, Boléa C, Girard F, Campo B, Fonsi M, et al. (September 2014). "Characterization of the novel positive allosteric modulator of the metabotropic glutamate receptor 4 ADX88178 in rodent models of neuropsychiatric disorders". The Journal of Pharmacology and Experimental Therapeutics. 350 (3): 495–505. doi:10.1124/jpet.114.214437. PMC   4152882 . PMID   24947466.
  3. ↑ Ponnazhagan R, Harms AS, Thome AD, Jurkuvenaite A, Gogliotti R, Niswender CM, et al. (June 2016). "The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia". Journal of Neuroimmune Pharmacology. 11 (2): 231–237. doi:10.1007/s11481-016-9655-z. PMC   4848139 . PMID   26872456.
  4. ↑ Abulwerdi G, Stoica BA, Loane DJ, Faden AI (September 2020). "Putative mGluR4 positive allosteric modulators activate Gi-independent anti-inflammatory mechanisms in microglia". Neurochemistry International. 138 104770. doi:10.1016/j.neuint.2020.104770. PMC   7392812 . PMID   32454165.
  5. ↑ Frouni I, Kwan C, Bédard D, Kang W, Hamadjida A, Nuara SG, et al. (October 2023). "Effect of the mGlu4 positive allosteric modulator ADX-88178 on parkinsonism, psychosis-like behaviours and dyskinesia in the MPTP-lesioned marmoset". Psychopharmacology. 240 (10): 2093–2099. doi:10.1007/s00213-023-06428-1. PMID   37516708.
  6. ↑ Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, et al. (October 2023). "Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers". Cell Research. 33 (10): 762–774. doi:10.1038/s41422-023-00830-2. PMC   10543438 . PMID   37286794.
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