Department of Biotechnology, School of Bioengineering, SRM Institute of Science and Technology, Kattankulathur, Tamil Nadu, India.
Department of Biochemistry, All India Institute of Medical Sciences, Bhopal, Madhya Pradesh, India.
Front Immunol. 2018 Aug 13;9:1873. doi: 10.3389/fimmu.2018.01873. eCollection 2018.
Histamine and its receptors (H1R-H4R) play a crucial and significant role in the development of various allergic diseases. Mast cells are multifunctional bone marrow-derived tissue-dwelling cells that are the major producer of histamine in the body. H1R are expressed in many cells, including mast cells, and are involved in Type 1 hypersensitivity reactions. H2R are involved in Th1 lymphocyte cytokine production. H3R are mainly involved in blood-brain barrier function. H4R are highly expressed on mast cells where their stimulation exacerbates histamine and cytokine generation. Both H1R and H4R have important roles in the progression and modulation of histamine-mediated allergic diseases. Antihistamines that target H1R alone are not entirely effective in the treatment of acute pruritus, atopic dermatitis, allergic asthma, and other allergic diseases. However, antagonists that target H4R have shown promising effects in preclinical and clinical studies in the treatment of several allergic diseases. In the present review, we examine the accumulating evidence suggesting novel therapeutic approaches that explore both H1R and H4R as therapeutic targets for histamine-mediated allergic diseases.
组胺及其受体（H1R-H4R）在各种过敏性疾病的发展中起着至关重要和显著的作用。肥大细胞是多功能的骨髓来源的组织驻留细胞，是体内组胺的主要产生细胞。H1R 在许多细胞中表达，包括肥大细胞，并参与 1 型超敏反应。H2R 参与 Th1 淋巴细胞细胞因子的产生。H3R 主要参与血脑屏障功能。H4R 在肥大细胞上高度表达，其刺激可加剧组胺和细胞因子的产生。H1R 和 H4R 在组胺介导的过敏性疾病的进展和调节中都具有重要作用。仅针对 H1R 的抗组胺药在治疗急性瘙痒、特应性皮炎、过敏性哮喘和其他过敏性疾病方面并非完全有效。然而，针对 H4R 的拮抗剂在治疗几种过敏性疾病的临床前和临床研究中显示出了有希望的效果。在本综述中，我们检查了积累的证据，这些证据表明了新的治疗方法，探索了 H1R 和 H4R 作为组胺介导的过敏性疾病的治疗靶点。
