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Objective: To study the effect of α-cypermethrin (α-CP) on some neuropharmacological paradigms like motor coordination, pentobarbitone-induced sleeping time and pentylenetetrazole-induced (PTZ) convulsion as well as γ-aminobutyric acid (GABA) level in rat brain. Materials and Methods: Albino Wistar rats were the experimental animals. Different neuropharmacological paradigms like motor coordination (determined by rotarod), pentobarbitone-induced sleeping time and PTZ-induced convulsion were carried out following oral administration of α-CP at two dose levels i.e., 145 mg/kg (LD50) and 14.5 mg/kg (1/10LD50), while the level of GABA in the brain of rats was estimated by HPLC after single-dose oral administration of α-CP at 145 mg/kg. Results: α-CP induced significant motor incoordination, decreased the time of onset and increased the duration of sleeping time induced by pentobarbitone; and also decreased the time of onset and increased the duration of convulsion induced by PTZ at the dose levels of 145 mg/kg (LD50) and 14.5 mg/kg (1/10 LD50) respectively. Further α-CP decreased brain GABA levels in the cerebellum and in whole brain (except cerebellum) significantly at LD50 dose level. Conclusion: A correlation between the effect of α-CP on central GABA levels and its neuropharmacological effects can be hypothesized. [ABSTRACT FROM AUTHOR]