A cell-permeable thiophene carboxymide derived compound that acts as a direct and selective antagonist of TrkB receptor. Binds to the high affinity site on the extracellular domain of TrkB in a dose-dependent manner (Kd = 10 nM) exhibiting much reduced binding to the low affinity site (Kd =12 µM) indicating that it does not compete with BDNF for the same binding site. Does not affect TrkA or TrkC receptors. Shown to permeate the blood-brain barrier, however, its antagonistic effects are not uniform throughout the brain. Does not affect the survivability of neurons. Reduces anxiety and depression related behavior in mice.
Biochem/physiol Actions
Primary Target TrkB
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Cazorla, M., et al. 2011. J. Clin. Invest.121,1846.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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