三氟拉嗪的抗伤害作用及其作用机理

应用小鼠热板法和醋酸扭体法伤害实验 ,评价三氟拉嗪的抗伤害作用 ,并对其作用机理进行探讨 .结果表明 :在热板法伤害实验中 ,三氟拉嗪 (2～ 2 0mg·kg- 1)剂量依赖性地延长热板伤害反应的潜伏期 ,三氟拉嗪 (2mg·kg- 1)和吗啡 (1,3和 6mg·kg- 1)合并使用 ,增加吗啡抗伤害的作用和效率(2 9.4 %～ 5 4 .4 % ) ;在醋酸扭体法伤害实验中 ,三氟拉嗪 (0 .1～ 3mg·kg- 1)非常显著地抑制醋酸伤害刺激所致小鼠扭体反应的次数 ,增加扭体反应的潜伏期 ,呈剂量依赖性 .进一步研究结果表明 :μ受体拮抗剂纳洛酮 (1～ 9mg·kg- 1)和多巴胺 1(DA1) /多巴胺 2 (DA2 )受体激动剂阿扑吗啡 (1～ 9mg·kg- 1)对三氟拉嗪的抗伤害作用无翻转作用 .这些结果提示 :三氟拉嗪具有一定的抗伤害刺激的药理作用 ,但是中枢神经系统中的 μ受体和DA2 受体不参与三氟拉嗪的抗伤害作用

Antinociception of trifluoperazine and its mechanisms

Antinociception of trifluoperazine (TFP) and its mechanisms were investigated by hot-plate nociceptive test and acetic acid-induced writhing test in mice. The results indicated that TFP (2－20 mg·kg^-1) produced a dose-dependent increase in the latency to hotplate nociception. Co-administration of TFP (2 mg·kg^-1) and morphine (1, 3 and 6 mg·kg^-1) markedly increased antinociceptive action and their antinociceptive rates (29.4%－54.4%). TFP (0.1－3.0 mg·kg^-1) dose-dependently inhibited the number of acetic acid- induced writhes in mice and increased their latency significantly. Neither naloxone (1－9 mg·kg^-1), a μ receptor antagonist, nor apomorphine (1－9 mg·kg^-1), a mixed DA₁/DA₂ receptor agonist, had any reverse effect on TFP antinociception. These findings suggest that TFP have some antagonism against the nociceptive stimulation in mice and the antinociception of TFP be not involved in μ and DA₂ receptors in central nervous system.