TB 21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptors (Ki = 1.6 nM). It 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). TB 21007 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 when administered at a dose of 0.3 mg/kg. It reduces paw tactile allodynia induced by reserpine in a rat model of fibromyalgia-like pain when administered intrathecally at doses of 1.5, 15, and 150 nmol.