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首页> 外文期刊>Life sciences >Regulation of neurokinin-1 receptor expression by GABA(B) receptor agonists.
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Regulation of neurokinin-1 receptor expression by GABA(B) receptor agonists.

机译：GABA（B）受体激动剂对神经激肽-1受体表达的调节。

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摘要

Activation of GABA(B) receptors produces analgesia in acute and chronic pain models. Data indicate that a possible mechanism for this effect is a GABA(B) receptor-induced blockade of neurokinin-1 (NK-1) receptor gene expression in the spinal cord. While much more potent GABA(B) receptor agonists (CGP 44532) have been developed, there is no information on their antinociceptive properties or their ability to influence NK-1 receptors. To address these issues, rats were treated with baclofen or CGP 44532 and tested for sedation, ataxia, and pain-related behaviors in a chronic pain model (formalin hindpaw injection). In a separate group of experiments the analgesic response to a single dose of CGP 44532 was tested prior, and subsequent to, its chronic administration. The results indicate that CGP 44532 is a substantially more potent analgesic than baclofen. In addition, after chronic administration baclofen was no longer capable of inducing analgesia or of inhibiting the increased expression of NK-1R mRNA and CGP 44532 was still fully effective in both regards. The results suggest that GABA(B) agonists could be clinically useful analgesics.
机译：GABA（B）受体的激活在急性和慢性疼痛模型中产生镇痛作用。数据表明，这种作用的可能机制是脊髓中GABA（B）受体诱导的神经激肽1（NK-1）受体基因表达的阻断。尽管已经开发出了更有效的GABA（B）受体激动剂（CGP 44532），但尚无有关其抗伤害感受特性或影响NK-1受体能力的信息。为了解决这些问题，用巴氯芬或CGP 44532治疗大鼠，并在慢性疼痛模型（福尔马林后爪注射）中测试了镇静，共济失调和疼痛相关行为。在另一组实验中，在慢性给药之前和之后测试了对单剂量CGP 44532的镇痛反应。结果表明，CGP 44532比巴氯芬具有更强的镇痛作用。另外，在长期给药后，巴氯芬不再具有诱导镇痛或抑制NK-1R mRNA表达增加的作用，而CGP 44532在这两个方面仍然完全有效。结果表明，GABA（B）激动剂可能是临床上有用的镇痛药。

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