6,7-DIHYDRO-3-[(2-HYDROXYETHYL)THIO]-6,6-DIMETHYL-1-(2-THIAZOLYL)-BENZO[C]THIOPHEN-4(5H)-ONE Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
TB 21007 is an inverse agonist of α
5β
3γ
2 subunit-containing GABA
A receptors (K
i = 1.6 nM). It selectively inhibits α
5β
3γ
2 subunit-containing GABA
A receptors over α
1-4 and α
6 subunit-containing GABA
A receptors that also contain β
3 and γ
2 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.
Verwenden
TB 21007 is a selective GABAA α5 receptor inverse agonist which enhances cognition.
Biologische Aktivit?t
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.
6,7-DIHYDRO-3-[(2-HYDROXYETHYL)THIO]-6,6-DIMETHYL-1-(2-THIAZOLYL)-BENZO[C]THIOPHEN-4(5H)-ONE Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
