最近的进步分子药理学的组胺系统:组胺H1受体调节信号通过改变其表达水平。
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公司总裁堀尾三好K Das AK,藤本K,年代,福井H
最近的进步分子药理学的组胺系统:组胺H1受体调节信号通过改变其表达水平。
101年5月,J Sci杂志》2006 (1):3 - 6。Epub 2006年4月28日。
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16648669 (在PubMed]
- 文摘
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组胺H1受体(H1R)信号是由改变其表达水平。这两种机制参与监管。一个是通过受体脱敏下调。受体磷酸化是至关重要的,因为刺激的突变H1R缺乏五个公认的磷酸化网站没有显示下调。磷酸化水平的突变体受体是远小于野生型的几个蛋白激酶。另一种是通过激活受体基因表达的上调。蛋白激酶C (PKC)信号被认为是参与这个老年病。监管H1R表达水平是介导不仅通过H1R还自主神经受体。刺激M3毒蕈碱的受体(M3R) H1R诱导上调和下调。下调的M3R-mediated H1R似乎不受PKC介导的激活,尽管PKC激活诱导H1R磷酸化。 Elevation of H1R expression was induced by the stimulation of M3Rs. PKC was suggested to be involved in this up-regulation. Stimulation of beta2-adrenergic receptors induced H1R down-regulation through several mechanisms. One of them is enhanced receptor degradation after desensitization and another is suppression of receptor synthesis that includes the suppression of receptor gene expression and enhanced degradation of the receptor mRNA. Protein kinase A was suggested to be involved in enhanced degradation and the activation of the receptor gene expression. Elevation of both H1R expression and its mRNA was observed in nasal mucosa of nasal hypersensitivity allergy model rat after toluene diisocyanate provocation. These results suggest that activation of H1R gene expression plays an important patho-physiological role in allergy. Elevation of the mRNA was partially but significantly suppressed by antihistamines.