924298-51-1

ABP 688 is a high affinity and selective of metabotropic glutamate receptor (mGluR5). Also, it inhibits glutamate induced calcium release from L(tk-) cells expressing human mGlu5 receptors.

This high-affinity mGluR antagonist (FW = 240.31 g/mol; CAS 924298- 51-1; Soluble to 100 mM in DMSO; 50 mM in 1 eq. HCl), also named 3- [2-(6-methyl-2-pyridinyl)ethynyl]-2-cyclohexene-1-one O-methyloxime, targets the human metabolotrophic glutamate receptor-5 (mGluR5) (Ki = 1.7 nM) and inhibits glutamate-induced calcium release from Ltk-cells expressing human mGlu5 receptors (IC50 = 2.3 nM). Indeed, [11C]- ABP688 is a useful PET tracer for in vivo imaging of the mGluR5 in rodents.

human mGluR5: 1.7 nM (Ki)

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