| Identification | Back Directory | [Name]
2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]- | [CAS]
1235318-89-4 | [Synonyms]
ADX88178
ADX-88178
ADX88178, >98%
ADX-88178;ADX 88178;ADX88178
5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine
4-methyl-N-[5-methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]-2-Pyrimidinamine
2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]-
5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)-1,3-thiazol-2-amine | [Molecular Formula]
C12H12N6S | [MDL Number]
MFCD21340285 | [MOL File]
1235318-89-4.mol | [Molecular Weight]
272.33 |
| Hazard Information | Back Directory | [Description]
ADX-88178 is a novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4 receptor in rodent models of anxiety, obsessive compulsive disorder (OCD), fear, depression, and psychosis. ADX88178 dose-dependently reduced the number of buried marbles in the marble burying test and increased open-arm exploration in the elevated plus maze (EPM) test, indicative of anxiolytic-like efficacy. | [Uses]
ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4. | [in vivo]
In mice, ADX88178 (1-30 mg/kg p.o.) dose-dependently increases the number of open-arm entries. Specifically, at 3, 10, and 30 mg/kg ADX88178, there are 5-, 7-, and almost 13-fold increases in the number of open-arm entries, respectively, when compared with the vehicle-treated controls. Also, ADX88178 dose-dependently increases the time spent in the open arms. Specifically, at 3, 10, and 30 mg/kgADX88178, there are 8-, 12-, and 24-fold increases in the time spent in the open arms when compared with the vehicle-treated controls. In rats, ADX88178 (10-100 mg/kg p.o.) dose-dependently increases the number of open-arm entries in the rat EPM test. Specifically, at 10, 30, and 100 mg/kg ADX88178, there are 5-, 8-, and more than 10-fold increases in the number of open-arm entries, respectively, when compared with the vehicle-treated controls. Also, ADX88178 dose-dependently increases the time spent in the open arms. Specifically, at 10, 30, and 100 mg/kg ADX88178, there are 7.5-, 11-, and 13-fold increases in time spent in the open arms when compared with the vehicle-treated controls[3]. | [target]
ADX88178 is a metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4. | [IC 50]
mGluR4: 4 nM (EC50) | [References]
[1] Fujinaga M, et al. Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). Bioorg Med Chem L DOI:10.1016/j.bmcl.2015.12.008
[2] Ponnazhagan R, et al. The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia. J Neuroimmune Pharmacol. 2016 Jun;11(2):231-7. DOI:10.1007/s11481-016-9655-z
[3] Kalinichev M, et al. Characterization of the novel positive allosteric modulator of the metabotropic glutamate receptor 4 ADX88178 in rodent models of neuropsychiatric disorders. J Pharmacol Exp Ther. 2014 Sep;350(3):495-505. DOI:10.1124/jpet.114.214437 |
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