Cayman GPR52 Comp-43

GPR52 comp-43 is an antagonist of g protein-coupled receptor 52 (GPR52; IC₅₀ = 0.63 µM).¹ It reduces mutant huntingtin (mHTT) protein levels in STHdh^Q7/Q111 cells, a heterozygous in vitro model of Huntingtons disease, in a concentration-dependent manner. GPR52 comp-43 (3 µM) reduces apoptosis induced by growth factor deprivation in primary striatal neurons isolated from the heterozygous Hdh^Q7/Q140 mouse model of Huntingtons 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 Hdh^Q140 mouse model of Huntingtons disease, when administered at a dose of 5 mg/kg.

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