TrkB Agonist, 7,8-Dihydroxyflavone

A cell permeable flavone based compound with neurotrophic and neuroprotective properties. Mimicks the action of Brain Derived Neurotrophic Factor (BDNF) and acts as a TrkB receptor agonist. Due to its lipophilic nature, it can cross the blood-brain barrier. Binds to the extra cellular domain of TrkB with high affinity and promotes its dimerization and autophosphorylation. Potentiates TrkB, but not TrkA, signaling in mouse brain slices. Its neurotropic effects are abolished in the presence of K252a. Suppresses apoptosis in human and rodent neurons and in stably transfected TrkB murine cell line T48 (EC₅₀ = 35 nM). Selectively reduces the basal GABAergic transmission due to its suppressive effect on presynaptic GABA release. However, it does not affect glutamatergic transmission.

Cell permeable: yes

Primary Target
TrkB

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Ren, Q., et al. 2013. Pharm. Biochem. Behav.106, 124.
Marongiu, D., et al. 2013. Eur. J. Pharmacol.709, 64.
Jang, S., et al. 2010. PNAS107, 2687.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)