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瘙痒的药物治疗-抗组胺药和作为 G 蛋白偶联受体的组胺受体。

Pharmacotherapy of Itch-Antihistamines and Histamine Receptors as G Protein-Coupled Receptors.

机构信息

Department of Dermatology, Graduate School of Medicine, The University of Tokyo, Tokyo 113-8655, Japan.

Laboratory of Molecular Radiology, Center for Disease Biology and Integrative Medicine, Graduate School of Medicine, The University of Tokyo, Tokyo 113-8655, Japan.

出版信息

Int J Mol Sci. 2022 Jun 13;23(12):6579. doi: 10.3390/ijms23126579.

DOI:10.3390/ijms23126579
PMID:35743023
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9223628/
Abstract

Itching can decrease quality of life and exacerbate skin symptoms due to scratching. Itching not only contributes to disease progression but also triggers complications such as skin infections and eye symptoms. Therefore, controlling itching is very important in therapeutic management. In addition to the well-known histamine, IL-31, IL-4 and IL-13 have recently been reported as factors that induce itching. Itching may also be caused by factors other than these histamines. However, we do not know the extent to which these factors are involved in each disease. In addition, the degree of involvement is likely to vary among individuals. To date, antihistamines have been widely used to treat itching and are often effective, suggesting that histamine is more or less involved in itchy diseases. This review discusses the ligand-receptor perspective and describes the dynamics of G protein-coupled receptors, their role as biased agonists, their role as inverse agonists, proactive antihistamine therapy, and drug selection with consideration of impaired performance and anti-PAF effects.

摘要

瘙痒可降低生活质量,并因搔抓而使皮肤症状恶化。瘙痒不仅会导致疾病进展,还会引发皮肤感染和眼部症状等并发症。因此,控制瘙痒在治疗管理中非常重要。除了众所周知的组胺外,IL-31、IL-4 和 IL-13 最近也被报道为引起瘙痒的因素。瘙痒也可能由这些组胺以外的因素引起。然而,我们不知道这些因素在每种疾病中的参与程度。此外,参与的程度可能因个体而异。迄今为止,抗组胺药已被广泛用于治疗瘙痒,且通常有效,这表明组胺或多或少参与了瘙痒性疾病。本文综述了配体-受体的角度,并描述了 G 蛋白偶联受体的动力学、作为偏激动剂的作用、作为反向激动剂的作用、主动抗组胺治疗以及考虑到性能受损和抗 PAF 作用的药物选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/36b26db3cefd/ijms-23-06579-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/25edd6a8454e/ijms-23-06579-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/3d452cef82e7/ijms-23-06579-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/1789901534ef/ijms-23-06579-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/c7be4fc216ee/ijms-23-06579-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/36b26db3cefd/ijms-23-06579-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/25edd6a8454e/ijms-23-06579-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/3d452cef82e7/ijms-23-06579-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/1789901534ef/ijms-23-06579-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/c7be4fc216ee/ijms-23-06579-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2456/9223628/36b26db3cefd/ijms-23-06579-g005.jpg

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