Emapunil (AC-5216, 0.1-3, 0.003-0.01 and 0.01-0.3 mg/kg, p.o.) produces anti-anxiety effects in the Vogel-type conflict test in rats, and in the light/dark box and social interaction tests in mice. Emapunil (AC-5216, 3-30 mg/kg, p.o.) reduces the immobility time, and this effect was blocked by PK11195. Emapunil (AC-5216, 1-100 mg/kg, p.o.) produces no distinct change in the rat electroencephalogram. Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) causes significant suppression of the enhanced anxiety and contextual fear induced in post-TDS rats. Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) alleviates the enhanced anxiety and fear response in a time-dependent sensitization (TDS) procedure, a rat PTSD animal model. Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) reverses the increased plasma glucose (PG) and decreased insulin (INS) in HFD-STZ rats.