ADX88178

ADX88178
Identifiers
	IUPAC name 5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)-1,3-thiazol-2-amine;
CAS Number	1235318-89-4;
PubChem CID	46836872;
IUPHAR/BPS	6238;
ChemSpider	28294729;
ChEMBL	ChEMBL3609729;
Chemical and physical data
Formula	C12H12N6S
Molar mass	272.33 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=NC(=NC=C1)NC2=NC(=C(S2)C)C3=CNN=C3;
	InChI 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

↑ 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.
↑ 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.
↑ 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.
↑ Abulwerdi G, Stoica BA, Loane DJ, Faden AI (September 2020). "Putative mGluR4 positive allosteric modulators activate G_i-independent anti-inflammatory mechanisms in microglia". Neurochemistry International. 138 104770. doi:10.1016/j.neuint.2020.104770. PMC 7392812. PMID 32454165.
↑ 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.
↑ 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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[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 G_i-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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References