丁螺环酮和1-(2-嘧啶基)-哌嗪可减弱小鼠中赛拉嗪诱导的抗伤害感受作用。
Buspirone and 1-(2-pyrimidinyl)-piperazine attenuate xylazine-induced antinociception in the mouse.
作者信息
Cao B J, Li W P
机构信息
Department of Pharmacology, Hunan Institute of Pharmaceutical Industry, Changsha, People's Republic of China.
出版信息
J Pharm Pharmacol. 1994 Nov;46(11):931-2. doi: 10.1111/j.2042-7158.1994.tb05720.x.
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.
使用小鼠醋酸试验检测了丁螺环酮及其主要代谢产物1-(2-嘧啶基)-哌嗪(1-PP)皮下预处理对赛拉嗪镇痛作用的影响。丁螺环酮和1-PP均剂量依赖性地减弱皮下注射赛拉嗪(0.8mg/kg)的镇痛作用，丁螺环酮的ED50值为7.3mg/kg，1-PP的ED50值为3.4mg/kg。用丁螺环酮(8mg/kg)或1-PP(4mg/kg)预处理可使赛拉嗪的镇痛ED50增加3至4倍。这些数据支持α2-肾上腺素能受体和1-PP参与丁螺环酮的药理活性。
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