히스타민 수용체, Histamine Receptor에 따른 특징

항히스타민제는 알레르기비염, 아토피피부염, 두드러기 등의 알레르기 질환에서 상기도염의 증상까지 다양하게 사용된다.

 

히스타민 수용체에 따른 기능

 

 

	H1	H2	H3	H4
발현 위치	Many tissues and cells, including nerves, respiratory epithelium, endothelial cells, hepatic cells, vascular smooth muscle cells, dendritic cells, and lymphocytes (다양한 세포)	Various cells and tissues, such as B cells, T cells, dendritic cells, gastricparietal cells, smooth muscle cells, and the brain and cardiac tissues  (다양한 세포)	neurone	variety of immune cells as well as on other cells such as spleen, intestinal epithelia, lung, synovial tissue, central nervous system, sensory neurons, and cancer cells (주로 면역세포)
활성화 결과	① contraction of smooth muscle of the respiratory tract ② increases vascular permeability ③ induces the production of prostacyclin and platelet activating factor by activating H1R ⇨ 호흡기관의 수축, 혈관 투과성 증가 등 염증반응 증가 ⇨ immediate hypersensitivity 반응(홍반, 간지러움, 부종)	① induce airway mucus production ② vascular permeability ③ secretion of gastric acid ⇨ 기도 점액 생성, 위산 분비 유도	① homeostatic regulation of energy levels ② sleep-wake cycle ③ cognition ④ inflammation ⇨ 항상성 유지, 인지능, 염증 반응에 관여; 신경전달물질의 분비 조절에 관여 * 결핍 mice에서 비만, 인슐린 수치 증가가 특징인 대사 증후군을 보임	enhances adhesion molecule expression, cell shape change, and cytoskeletal rearrangement via H4R, leading to the increased migration of eosinophils ⇨ 염증 반응 및 골수모세포 등의 분화에 관여
임상적 사용	O	O	X	NEW TARGET (allergy & inflammation)
예	azatadine, cetirizine	famotidine, nizatidine	thioperamide, clobenpropit	JNJ 7777120

 

reference:

1) Thangam, Elden Berla, et al. "The role of histamine and histamine receptors in mast cell-mediated allergy and inflammation: the hunt for new therapeutic targets." Frontiers in immunology 9 (2018): 1873.