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首页> 外文期刊>Life sciences >Intrathecal endomorphin-1 produces antinociceptive activities modulated by alpha 2-adrenoceptors in the rat tail flick, tail pressure and formalin tests.
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Intrathecal endomorphin-1 produces antinociceptive activities modulated by alpha 2-adrenoceptors in the rat tail flick, tail pressure and formalin tests.

机译：鞘内内啡肽1在大鼠甩尾，尾压和福尔马林测试中产生由α2肾上腺素能受体调节的镇痛活性。

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摘要

It is known that spinal morphine produces antinociception that is modulated by alpha 2-adrenoceptors. Endomorphin-1, a newly-isolated endogenous opioid ligand, shows the greatest selectivity and affinity for the mu-opiate receptor of any endogenous substance found to date and may serve as a natural ligand for the mu-opiate receptor. We examined the antinociceptive effects of endomorphin-1 administered intrathecally (i.t.) in the rat tail flick, tail pressure and formalin tests. Intrathecal endomorphin-1 produced dose-dependent antinociceptive effects in the three tests. ED50 (CI95) values for antinociception of i.t. endomorphin-1 in the tail flick test and tail pressure test were 1.9 (0.96-3.76) nmol and 1.8 (0.8-4.2) nmol, respectively. ED50 (CI95) values for phase 1 and phase 2 in the formalin test were 12.5 (7.9-19.8) nmol and 17.5 (10.2-30) nmol, respectively. Pretreatment with i.t. beta-funaltrexamine (a mu-opioid receptor selective antagonist) significantly antagonized the antinociceptive effects of endomorphin-1 in the three tests. Beta-funaltrexamine alone had not effects on the three tests. The antinociceptive effects of endomorphin-1 were also antagonized by i.t. yohimbine (an alpha 2-adrenoceptor selective antagonist). The combination of ineffective doses of i.t. clonidine (an alpha 2-adrenoceptor agonist) and endomorphin-1 produced a significant antinociception in the three tests. The results showed that intrathecal endomorphin-1 produced antinociception in a dose-dependent manner in the rat tail flick, tail pressure and formalin tests, which was mediated by spinal mu-opioid receptors and modulated by alpha 2-adrenoceptors.
机译：已知脊髓吗啡会产生由α2肾上腺素受体调节的镇痛作用。 Endomorphin-1是一种新近分离的内源性阿片样物质配体，对迄今发现的任何内源性物质均具有对mu-鸦片受体的最大选择性和亲和力，并可作为mu-鸦片受体的天然配体。我们在大鼠尾部甩动，尾压和福尔马林测试中检查了鞘内（i.t.）施用内啡肽1的抗伤害感受作用。鞘内endomorphin-1在这三个测试中产生剂量依赖性的镇痛作用。镇痛作用的ED50（CI95）值甩尾试验和尾压试验中的endomorphin-1分别为1.9（0.96-3.76）nmol和1.8（0.8-4.2）nmol。在福尔马林测试中，阶段1和阶段2的ED50（CI95）值分别为12.5（7.9-19.8）nmol和17.5（10.2-30）nmol。 i.t.预处理在这三项测试中，β-funaltrexamine（一种μ阿片受体选择性拮抗剂）显着拮抗了endomorphin-1的抗伤害感受作用。单独的β-去氨曲明对这三个试验没有影响。内啡肽1的抗伤害感受作用也被i.t.育亨宾（一种α2肾上腺素受体选择性拮抗剂）。无效剂量的i.t.可乐定（一种α2肾上腺素受体激动剂）和内啡肽-1在这三个试验中产生了显着的抗伤害感受。结果表明鞘内endomorphin-1在大鼠甩尾，尾巴压力和福尔马林试验中以剂量依赖性方式产生抗伤害感受，这是由脊髓μ阿片受体介导并受α2肾上腺素受体调节的。

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