1235318-89-4
Chemical Structure
ADX88178
- CAS No.: 1235318-89-4
- Formula:C12H12N6S
- Molecular Weight:272.33
IUPAC Name: 5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine
InChIKey: MIQNXKWDQRNHAU-UHFFFAOYSA-N
SMILES: CC1=C(C2=CNN=C2)N=C(NC3=NC=CC(C)=N3)S1
Biological Activity: ADX88178 is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC50 of 3.5 nM against hmGluR4. ADX88178 modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease[1][2].
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ADX88178 | 99.50% | ADX88178 is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC50 of 3.5 nM against hmGluR4. ADX88178 modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease. | ||||||||||||||||||||
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- [1]. Finlay CJ, et al. Metabotropic Glutamate Receptor 4 (mGlu4) Positive Allosteric Modulators Lack Efficacy in Rat and Marmoset Models of L-DOPA-Induced Dyskinesia. J Parkinsons Dis. 2024;14(2):245-259. [Content Brief]
- [2]. Le Poul E, et al. A potent and selective metabotropic glutamate receptor 4 positive allosteric modulator improves movement in rodent models of Parkinson's disease. J Pharmacol Exp Ther. 2012;343(1):167-177. [Content Brief]
Keywords