ANA-12 is a selective, small-molecule non-competitive antagonist of TrkB (Kd = 10 nM and 12 μM for the high- and low-affinity sites, respectively), the main receptor of brain-derived neurotrophic factor (BDNF). The compound crosses the blood-brain-barrier and exerts central TrkB blockade, producing effects as early as 30 minutes (~400 nM) and as long as 6 hours (~10 nM) following intraperitoneal injection in mice. It blocks the neurotrophic actions of BDNF without compromising neuron survival.