A GPR52 antagonist
CAY10786 is an antagonist of G protein-coupled receptor 52 (GPR52; IC50 = 0.63 µM).1 It reduces mutant huntingtin (mHTT) protein levels in STHdhQ7/Q111 cells, a heterozygous in vitro model of Huntington’s disease, in a concentration-dependent manner. CAY10786 (3 µM) reduces apoptosis induced by growth factor deprivation in primary striatal neurons isolated from the heterozygous HdhQ7/Q140 mouse model of Huntington’s disease. It decreases striatal levels of soluble and insoluble mHTT, as well as increases the latency to fall in the rotarod test, in the homozygous HdhQ140 mouse model of Huntington’s disease, when administered at a dose of 5 mg/kg.
1.Wang, C., Zhang, Y.-F., Guo, S., et al.GPR52 antagonist reduces huntingtin levels and ameliorates Huntington’s disease-related phenotypesJ. Med. Chem.64(2)941-957(2021)
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