LY2428703

LY2428703 is a small molecule antagonist developed as a radioligand for positron emission tomography (PET) imaging of the metabotropic glutamate receptor subtype 1 (mGluR1). It acts as a full antagonist at mGluR1 with high affinity (IC50 ≈ 8.9 nM) and as a partial antagonist at mGluR5 with lower affinity (IC50 ≈ 118 nM). LY2428703 shows high specificity for mGluR1 over other metabotropic glutamate receptors and demonstrates favorable in vitro and in vivo characteristics for quantifying mGluR1 in rodent brains. The compound has been labeled with carbon-11 ([11C]) to create [11C]LY2428703 for use as a PET radiotracer. However, it was found unsuitable for imaging in monkey and human brains due to pharmacokinetic limitations[1][2][5][9].

Other names

(1R,2R)-N-[3-(4-methoxyphenyl)-4-methyl-isothiazol-5-yl]-2-methyl-cyclopropanecarboxamide