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  2. The Role of Histamine and Histamine Receptors in Mast Cell-Mediated Allergy and Inflammation: The Hunt for New Therapeutic Targets

The Role of Histamine and Histamine Receptors in Mast Cell-Mediated Allergy and Inflammation: The Hunt for New Therapeutic Targets

  • Front Immunol. 2018 Aug 13:9:1873. doi: 10.3389/fimmu.2018.01873.
Elden Berla Thangam 1 Ebenezer Angel Jemima 1 Himadri Singh 2 Mirza Saqib Baig 3 Mahejibin Khan 4 Clinton B Mathias 5 Martin K Church 6 Rohit Saluja 2 7
Affiliations

Affiliations

  • 1 Department of Biotechnology, School of Bioengineering, SRM Institute of Science and Technology, Kattankulathur, Tamil Nadu, India.
  • 2 Department of Biochemistry, All India Institute of Medical Sciences, Bhopal, Madhya Pradesh, India.
  • 3 Discipline of Biosciences and Biomedical Engineering (BSBE), Indian Institute of Technology Indore (IITI), Indore, Madhya Pradesh, India.
  • 4 Central Food Technological Research Institute-Resource Centre, Lucknow, India.
  • 5 Department of Pharmaceutical and Administrative Sciences, Western New England University, Springfield, MA, United States.
  • 6 Department of Dermatology and Allergy, Charité - Universitätsmedizin Berlin, Berlin, Germany.
  • 7 Department of Biotechnology, Government of India, New Delhi, India.
Abstract

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.

Keywords

allergy; antihistamines; histamine; histamine receptors; inflammation; mast cells.

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