Cayman TB 21007

TB 21007 is an inverse agonist of α₅β₃γ₂ subunit-containing GABA_A receptors (K_i = 1.6 nM).¹ It selectively inhibits α₅β₃γ₂ subunit-containing GABA_A receptors over α_1-4 and α₆ subunit-containing GABA_A receptors that also contain β₃ and γ₂ subunits (K_is = 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 (Item No. 16474) in a rat model of fibromyalgia-like pain when administered intrathecally at doses of 1.5, 15, and 150 nmol.²

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