TB 21007

An inverse agonist of α5β3γ2 subunit-containing GABAA receptors (Ki = 1.6 nM); selectively inhibits α5β3γ2 subunit-containing GABAA receptors over α1-4 and α6 subunit-containing GABAA receptors that also contain β3 and γ2 subunits (Kis = 20, 16, 20, 106, and 1,800 nM, respectively); reduces the latency to find the hidden platform in a matching-to-place variant of the Morris water maze, indicating enhanced spatial memory, in rats at 0.3 mg/kg; reduces reserpine-induced paw tactile allodynia in a rat model of fibromyalgia-like pain at 1.5, 15, and 150 nmol intrathecally