ABP 688

ABP 688 is a non-competitive antagonist of metabotropic glutamate receptor 5 (mGluR5; K_i = 3.5 nM in a radioligand binding assay using L(tk-) cell membranes expressing human receptors).¹ It is selective for mGluR5 receptors over a panel of CNS G protein-coupled receptors, ion channels, and transporters at 10 μM. ABP 688 inhibits quisqualate-induced phosphoinositol accumulation in and glutamate-induced calcium release from L(tk-) cells expressing human mGluR5 (IC₅₀s = 2.4 and 2.3 nM, respectively). Radiolabeled forms of ABP 688 have been used as PET tracers for in vivo imaging of mGluR5 receptors in rodents.^1,2

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1. Hintermann, S., Vranesic, I., Allgeier, H., et al. ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: Identification, in vitro pharmacology, pharmacokinetic and biodistribution studies. Bioorg. Med. Chem. 15(2), 903-914 (2007).

2. Elmenhorst, D., Minuzzi, L., Aliaga, A., et al. In vivo and in vitro validation of reference tissue models for the mGluR5 ligand [¹¹C]ABP688. J. Cereb. Blood Flow Metab. 30(8), 1538-1549 (2010).