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≥98% (HPLC)
DMSO: 2 mg/mL, clear
TB21007 is a gamma-aminobutyric acid type A receptor (GABAA) alpha 5 (α5) subtype-selective (αβ3γ2 Ki in nM = 1.6/α5, 20/α1, 16/α2, 20/α3) negative allosteric modulator (NAM)/inverse agonist (% inhibition at 100 nM = 51/α5, 21/α1, 1/α2, 3/α3, using L(tk-) fibroblast expressing β3γ2 with respective α subunit). TB21007 enhances cognitive performance in a hippocampal-dependent memory task in vivo (0.3 mg/kg i.p. in rats; delayed ‘matching-to-place′ Morris water maze test) without the convulsant or proconvulsant activity (3 mg/kg i.p. in mice) observed with nonselective inverse agonists.
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