Biological Activity
ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively.
In Vitro
ANA-12 (10 nM) prevents BDNF-induced neurite outgrowth in the TrkB-expressing cells, and completely abolishes the effects of BDNF at concentrations up to 10-100 μM[1].
In Vivo
ANA-12 (0.5 mg/kg, i.p.) partially inhibits the total endogenous TrkB activity in the whole brain of mice. ANA-12, injected in mice, demonstrates anxiolytic and antidepressive activities at 0.5 mg/kg. ANA-12 (0.5, 1.0, and 2.0 mg/kg) does not affect neuron survival[1]. ANA-12 (0.5 mg/kg) shows antidepressant effects in lipopolysaccharide (LPS)-induced depression-like behavior. ANA-12 (0.5 mg/kg) significantly attenuates an increased immobility time in depressed mice. In the TST, FST, and SPT, ANA-12 (0.5 mg/kg) does not show antidepressant-like effects in the control mice[2]. ANA-12 (0.5 mg/kg, i.p.) reverses the diminished self-administration of cocaine in CocSired rats[3].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.
