TrkB receptor antagonist. Binds to two distinct receptor sites preventing activation by BDNF non-competitively, IC50 = 45.6 nM and 41.1 µM for the high and low affinity sites respectively. Systemic administration to adult mice decreased TrkB activity in the brain without affecting neuronal survival or altering TrkA and TrkC functions. Displays antidepressant and anxiolytic properties in mouse models after systemic administration1. Shows antidepressant effects on LPS-induced depression-like behavior in mice2. Has been used to elucidate the role of BDNF in improvement of cognitive decline during calorie restriction3 and in the discovery of new neurotrophic agents4.
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