CTEP

An inverse agonist of mGluR5 (Kis = 16.4, 12.6, and 9.5 nM for the human, rat, and mouse receptors, respectively, in a radioligand binding assay); selective for mGluR5 over mGluR1, -2, -3, -4, -6, -7, and -8 (IC50s = >10 µM for all) and the histamine H1 and α5β3γ2 subunit-containing GABAA receptors (Kis = >4 and >3.2 µM, respectively), but does inhibit adenosine A1, A3, muscarinic, and kainate receptors (Kis = 6.2, 2.3, 5.3, and 7.9 µM, respectively), as well as L-type calcium and sodium channels (Kis = 2.7 and 5 µM, respectively) in a panel of 103 receptors, enzymes, and ion channels at 10 µM; inhibits inositol phosphate accumulation and quisqualate-induced calcium mobilization in HEK293 cells expressing human recombinant mGluR5 (IC50s = 6.4 and 11.4 nM, respectively); reduces stress-induced hyperthermia in mice and increases drinking in the Vogel conflict test in rats, indicating anxiolytic-like activity, at 0.3 mg/kg