Buspirone and 1-(2-pyrimidinyl)-piperazine attenuate xylazine-induced antinociception in the mouse

The effects of subcutaneous pretreatment with buspirone and its major metabolite 1-(2-pyrimidinyl)-piperazine (1-PP) on the antinociceptive effect of xylazine were examined using the mouse acetic acid assay. Both buspirone and 1-PP dose-dependently attenuated the antinociceptive action of subcutaneously administered xylazine (0.8 mg kg-1), with ED50 values of 7.3 mg kg-1 for buspirone and 3.4 mg kg-1 for 1-PP. Pretreatment with either buspirone (8 mg kg-1) or 1-PP (4 mg kg-1) increased the antinociceptive ED50 of xylazine 3-4-fold. These data support the involvement of alpha 2-adrenoceptor and 1-PP in the pharmacological activity of buspirone.