Pharmacotherapy of generalized anxiety disorders has been depended on benzodiazepines for many decades. However, the use of these compounds is restricted because of their adverse effects. Pregabalin is an anticonvulsant indicated as adjunctive therapy for treating adults' partial seizures. It has shown some efficacy in randomized, placebo-controlled clinical trials aimed to treat generalized anxiety disorder. Mechanism of pharmacologic activity of Pregabalin was extensively studied and it was proven to acquire high-affinity binding to α2δ. The current study employed the dark/light box and the elevated plus maze. Male albino mice were allocated into groups: group i: mice received distilled water (16 ml/kg, p.o.), group ii: mice received diazepam (1 mg/kg, p.o.), group iii-iv: mice received a dose of Pregabalin (25 or 50 mg/kg, p.o.), group v: mice treated with rimonabant (1 mg/kg, i.p.) 30 min before a dose of Pregabalin (50 mg/kg), group vi: mice received rimonabant (1 mg/kg, i.p.) 30 min before a dose of distilled water (16 ml/kg, p.o.). Results indicated that Pregabalin (50 mg/kg) showed anxiolytic effect in the two paradigms, the dark/light transition box and the mouse elevated plus maze. Pretreatment with rimonabant diminished most of the anxiolytic effect of Pregabalin (50 mg/kg) as indicated by shorter time spent in white are in the dark/light box and shorter open arm time (%) compared to mice received Pregabalin.