Pain-relieving prospects for adenosine receptors and ectonucleotidases.

Pain-relieving prospects for adenosine receptors and ectonucleotidases.
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腺苷受体和核酸外切酶缓解疼痛的前景。

DOI:
10.1016/j.molmed.2010.12.006
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发表时间:
2011-04
影响因子:
13.6
通讯作者:
Zylka MJ
Zylka MJ
中科院分区:
医学1区
文献类型:
--
作者:
Zylka MJ

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腺苷受体激动剂在多种慢性疼痛的临床前模型中具有有效的抗伤害感受作用。相比之下,腺苷或腺苷受体激动剂在治疗人类疼痛中的功效尚不清楚。最近鉴定了两种在伤害感受神经元中产生腺苷的外核苷酸酶。当脊髓注射时,这些酶在炎症和神经性疼痛模型中具有持久的腺苷A1受体(A1R)依赖性抗伤害作用。此外,最近的研究结果表明,脊髓腺苷A2A受体激活可以有效地抑制神经病理性疼痛症状。总的来说,这些研究表明,通过用激动剂或用产生腺苷的外核苷酸酶靶向解剖学定义的区域中的特定腺苷受体亚型来治疗人类慢性疼痛的可能性。
Adenosine receptor agonists have potent antinociceptive effects in diverse preclinical models of chronic pain. In contrast, the efficacy of adenosine or adenosine receptor agonists at treating pain in humans is unclear. Two ectonucleotidases that generate adenosine in nociceptive neurons were recently identified. When injected spinally, these enzymes have long-lasting adenosine A1 receptor (A1R)-dependent antinociceptive effects in inflammatory and neuropathic pain models. Furthermore, recent findings indicate that spinal adenosine A2A receptor activation can enduringly inhibit neuropathic pain symptoms. Collectively, these studies suggest the possibility of treating chronic pain in humans by targeting specific adenosine receptor subtypes in anatomically defined regions with agonists or with ectonucleotidases that generate adenosine.
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