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研究一种新型的N型电压敏感性钙通道阻断剂虎纹蜘蛛毒素 Ⅰ (HWTX Ⅰ ) ,硬脊膜外腔用药对福尔马林结肠壁粘膜下注射诱导的大鼠急性炎性内脏疼痛的抑制性效应 .5 %福尔马林溶液15 0 μl快速注入SD大鼠乙状结肠壁粘膜下层 ,可产生几种可评估的反映内脏疼痛的固定性行为 .在此伤害性刺激反应前 30min ,经留置的导管向大鼠硬脊膜外腔分别注入各待测药品和试剂 ,观察其对该模型疼痛行为的影响 .与生理盐水阴性对照组 ,美国同类镇痛新药ω 芋螺毒素 (ω CTX MVIIA)和吗啡两个阳性对照组比较 ,HWTX Ⅰ五个剂量组 ,进行大鼠硬脊膜外腔注药 ,均能以剂量依赖方式明显抑制福尔马林结肠壁注射诱导的伤害性行为反应 .HWTX Ⅰ和ω CTX MVIIA在 2 0μg kg体重剂量时 ,其抑制效果是稳定和明显的 ;在 5 0 70 μg kg体重剂量下 ,抑制效果更为显著 .HWTX Ⅰ量 效实验发现 ,在等剂量下 ,ω CTX MVIIA镇痛效果略高于HWTX Ⅰ .但在 5 0～ 75 μg kg较高剂量下 ,ω CTX MVIIA可能引起大鼠产生明显的运动能力障碍 ,而HWTX Ⅰ在该剂量范围内则未见类似的毒副作用 .盐酸吗啡镇痛作用起效快于HWTX Ⅰ和ω CTX MVIIA ,但维持时间较后二者短 .实验结果表明 :同为多肽类N型电压敏感性钙通道拮抗剂 ,HWTX Ⅰ和ω CTX MVIIA大鼠硬脊?
A new type of N-type voltage-sensitive calcium channel blocker, tiger spider toxin I (HWTX Ⅰ), was used to study the acute inflammatory visceral pain induced by submucosal injection of formalin into the colon wall of rats Of the inhibitory effect of 5% formalin solution 15 0 μl rapid injection of SD rat sigmoid colon submucosa, can produce several evaluable visceral pain reflect the fixed behavior 30 minutes before the nociceptive response, the Indwelling catheters were injected into the epidural space of each rat to be tested drugs and reagents, to observe its impact on the pain behavior of the model.Compared with saline negative control group, the same type of analgesic drug conotoxin (ω CTX MVIIA ) And morphine, the two doses of HWTX Ⅰ were injected into the epidural space of rats in a dose-dependent manner, and all of the five doses of HWTX Ⅰ significantly inhibited the nociceptive responses induced by injection of formalin into the colon wall. The inhibitory effect of HWTX Ⅰ and ω CTX MVIIA was stable and obvious at the dose of 20 μg kg body weight, and the inhibitory effect was more significant at the dose of 50 70 μg kg body weight.HWTX Ⅰ dose-effect test found that at the same dose , ωCTX MVIIA analgesic effect was slightly higher than that of HWTX Ⅰ, but ω CTX MVIIA could cause significant motor dysfunction in rats at higher doses of 50 ~ 75 μg kg, while no HWTX Ⅰ was found in this dose range Similar toxicities and side effects of morphine hydrochloride analgesic effect onset faster than HWTX Ⅰ and ω CTX MVIIA, but the maintenance time is short.The results show that: with peptide N-type voltage-sensitive calcium channel antagonist, HWTX Ⅰ And ω CTX MVIIA rat spinal?