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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Antinociceptive effects of intragastric dl-tetrahydropalmatine on visceral and somatic persistent nociception and pain hypersensitivity in rats.
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Antinociceptive effects of intragastric dl-tetrahydropalmatine on visceral and somatic persistent nociception and pain hypersensitivity in rats.

机译：胃内dl-四氢巴马汀对大鼠内脏和躯体持续伤害感受和疼痛超敏反应的镇痛作用。

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Although tetrahydropalmatine (THP), an alkaloid constituent of plants from the genera Stephania and Corydalis, is known to have analgesic property, the antinociceptive effects of THP have not been well evaluated experimentally and the appropriate indications for treatment of clinical pain remain unclear. In the present study, nociceptive and inflammatory models of both somatic and visceral origins were used to assess the antinociceptive and antihyperalgesic effects of intragastric (i.g.) pretreatment of dl-THP in rats. In the bee venom (BV) test that has been well established experimentally, i.g. pretreatment of three doses of dl-THP (20, 40, 60 mg/kg, body weight) resulted in less stably antinociceptive effect on the BV-induced persistent paw flinches that are known to be processed by spinal nociceptive circuit, however the drug of the two higher doses produced distinct suppression of the BV-induced persistent nociception rated by nociceptive score that reflects both spinal and supraspinal mediation. Similarly, the antinociception of dl-THP (60 mg/kg) was only significant for phase 1 but not for phase 2 of the formalin-induced persistent paw flinches, however, the inhibition was distinct for both phase 1 and phase 2 of the formalin nociceptive score. For the antihyperalgesic effect, in contrast, pretreatment of dl-THP (60 mg/kg) produced significant inhibition of both primary hyperalgesia to either thermal or mechanical stimuli and the mirror-image thermal hyperalgesia identified in the BV test. In the acetic acid writhing test, the number of writhes was completely blocked at the first 5-min interval followed by a sustained suppression in the remaining period of the whole time course comparing to the vehicle control. These data suggest that i.g. pre-administration of dl-THP could more effectively inhibit visceral nociception as well as thermal and mechanical inflammatory pain hypersensitivity (hyperalgesia) than persistent nociception. Moreover, the drug is likely to produce more effectiveness on supraspinally processed nociceptive behaviors than spinally mediated nociceptive behaviors, implicating an action of THP at the supraspinal level.
机译：尽管已知四氢帕马汀（THP）是Stephania和Corydalis属植物的生物碱成分，具有镇痛作用，但尚未通过实验很好地评估THP的镇痛作用，并且尚不清楚治疗临床疼痛的适当适应症。在本研究中，体细胞和内脏起源的伤害性和炎症性模型被用于评估大鼠dl-THP胃内（例如）预处理的抗伤害性和抗痛觉过敏作用。在通过实验确定的蜂毒（BV）测试中，例如预处理三剂dl-THP（20、40、60 mg / kg体重）对BV引起的持续性爪状退缩作用的镇痛作用较差，已知该退行性缩痛是由脊髓伤害性回路处理的，但是两种高剂量产生的BV诱导的持续伤害感受明显受到抑制，伤害感受评分反映了脊髓和脊髓上调解。同样，dl-THP（60 mg / kg）的镇痛作用仅对福尔马林诱导的持续性爪退缩的1期有效，对2期无效，但是，对福尔马林的1期和2期抑制作用明显伤害评分。相反，对于抗痛觉过敏作用，dl-THP（60 mg / kg）的预处理对热刺激或机械刺激产生的原发性痛觉过敏和BV测试中确定的镜像热痛觉过敏均产生了明显的抑制作用。在醋酸扭体试验中，与车辆对照相比，在最初的5分钟间隔内完全遮住了写数，然后在整个时间过程的其余时间内持续抑制了写数。这些数据表明预先给予dl-THP可以比持续伤害更有效地抑制内脏伤害感受以及热和机械性炎性疼痛超敏反应（痛觉过敏）。此外，与脊柱介导的伤害感受行为相比，该药物可能对脊髓上处理的伤害感受行为产生更大的有效性，这暗示了THP在脊髓上水平的作用。

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