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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >Substitution of a mutant α_2a-adrenergic receptor via 'hit and run' gene targeting reveals the role of this subtype in sedative, analgesic, and anesthetic-sparing responses in vivo
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Substitution of a mutant α_2a-adrenergic receptor via 'hit and run' gene targeting reveals the role of this subtype in sedative, analgesic, and anesthetic-sparing responses in vivo

机译:通过“命中和奔跑”基因靶向替代突变体α_2a-肾上腺素受体揭示了该亚型在体内的镇静,镇痛和麻醉剂缓解反应中的作用

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摘要

Norepinephrine contributes to antinocicep- tive, sedative, and sympatholytic responses in vivo, and α2 adrenergic receptor (α_2AR) agonists are used clinically to mimic these effects. Lack of subtype-specific agonists has prevented elucidation of the role that each α_2AR subtype (α_2A, α2B, and α_2C) plays in these central effects. Here we demon- strate that α_2AR agonist-elicited sedative, anesthetic-sparing, and analgesic responses are lost in a mouse line expressing a subtly mutated α_2A AR, D79N α_2A AR, created by two-step homologous recombination.
机译:去甲肾上腺素有助于体内的抗伤害性,镇静性和交感神经反应,临床上使用α2肾上腺素能受体(α_2AR)激动剂来模拟这些作用。缺乏亚型特异性激动剂无法阐明每种α_2AR亚型(α_2A,α2B和α_2C)在这些中心作用中的作用。在这里,我们证明了通过两步同源重组产生的α_2AR激动剂引起的镇静,麻醉保留和镇痛反应在表达微妙突变的α_2AAR,D79Nα_2AAR的小鼠品系中消失了。

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