6,7-DIHYDRO-3-[(2-HYDROXYETHYL)THIO]-6,6-DIMETHYL-1-(2-THIAZOLYL)-BENZO[C]THIOPHEN-4(5H)-ONE

Description

TB 21007 is an inverse agonist of α₅β₃γ₂ subunit-containing GABA_A receptors (K_i = 1.6 nM). 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 in a rat model of fibromyalgia-like pain when administered intrathecally at doses of 1.5, 15, and 150 nmol.

Uses

TB 21007 is a selective GABAA α5 receptor inverse agonist which enhances cognition.

Biological Activity

GABA A receptor inverse agonist selective for the α 5 -subtype (K i values are 1.6, 16, 20 and 20 nM for α 5, α 2, α 1 and α 3 subtypes respectively). Brain penetrant; enhances cognitive performance in rats in the delayed matching-to-place morris water maze test following i.p. administration.

storage

Store at +4°C

Raw materials

Preparation Products