An inverse agonist of α5β3γ2 subunit-containing GABAA receptors (Ki = 1.6 nM); 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

TB 21007 – 25 mg

Brand:
Cayman
CAS:
207306-50-1
Storage:
-20
UN-No:
Non-Hazardous - /

TB 21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptors (Ki = 1.6 nM).{48803} 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 (Item No. 16474) in a rat model of fibromyalgia-like pain when administered intrathecally at doses of 1.5, 15, and 150 nmol.{48807}  

 

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Description

An inverse agonist of α5β3γ2 subunit-containing GABAA receptors (Ki = 1.6 nM); 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); 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 at 0.3 mg/kg; reduces reserpine-induced paw tactile allodynia in a rat model of fibromyalgia-like pain at 1.5, 15, and 150 nmol intrathecally

Formal name: 6,7-dihydro-3-[(2-hydroxyethyl)thio]-6,6-dimethyl-1-(2-thiazolyl)-benzo[c]thiophen-4(5H)-one

Synonyms: 

Molecular weight: 339.5

CAS: 207306-50-1

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Pain Research

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