Cao B J, Li W P
Department of Pharmacology, Hunan Institute of Pharmaceutical Industry, Changsha, People's Republic of China.
Eur J Pharmacol. 1994 Jun 23;259(1):75-8. doi: 10.1016/0014-2999(94)90160-0.
The effects of pretreatment with buspirone and its major metabolite 1-(2-pyrimidinyl)-piperazine (1-PP) on antinociception produced by clonidine were investigated in mice. Buspirone and 1-PP dose dependently attenuated the antinociceptive action of s.c. administered clonidine in the writhing and tail-flick assays. In both assays, 1-PP was more potent than buspirone in antagonizing clonidine-induced antinociception. After s.c. pretreatment with buspirone (8 mg/kg) and 1-PP (4 mg/kg), the antinociceptive ED50 values of s.c. clonidine were significantly increased. The antagonistic effects of buspirone and 1-PP on clonidine-induced antinociception may be due to their alpha 2-adrenoceptor antagonist activity.
在小鼠中研究了丁螺环酮及其主要代谢产物1-(2-嘧啶基)-哌嗪(1-PP)预处理对可乐定产生的抗伤害感受的影响。在扭体和甩尾试验中，丁螺环酮和1-PP剂量依赖性地减弱了皮下注射可乐定的抗伤害感受作用。在这两种试验中，1-PP在拮抗可乐定诱导的抗伤害感受方面比丁螺环酮更有效。皮下预先给予丁螺环酮(8mg/kg)和1-PP(4mg/kg)后，皮下注射可乐定的抗伤害感受ED50值显著增加。丁螺环酮和1-PP对可乐定诱导的抗伤害感受的拮抗作用可能归因于它们的α2-肾上腺素能受体拮抗活性。
