Histamine H4 receptor (H4R) (H4R)

The Histamine H4 receptor (H4R) is a G protein-coupled receptor (GPCR) primarily expressed on hematopoietic and immune cells, including mast cells, eosinophils, dendritic cells, and T cells [1, 4, 7]. It plays a critical role in the immune system by mediating histamine-induced chemotaxis and regulating the production of various cytokines and chemokines [1, 4]. In mice, the H4R is encoded by the Hrh4 gene and is involved in the pathogenesis of several inflammatory and allergic conditions, such as asthma, allergic rhinitis, and dermatitis [3, 7, 14]. Beyond its peripheral immune functions, recent studies have identified H4R expression in the central nervous system, where it may modulate pain perception, anxiety, and locomotor activity [8, 10]. Pharmacologically, H4R is a significant therapeutic target; antagonists like JNJ 7777120 have shown efficacy in reducing inflammation and pruritus in animal models [11, 13, 14]. Additionally, H4R agonists are being explored for their potential anti-nociceptive effects in neuropathic pain models [10]. However, translating these findings to the clinic has been challenging due to significant interspecies differences in receptor affinity and pharmacological profiles between mice and humans [4, 13]. Despite these challenges, the H4R remains a promising target for treating chronic inflammatory diseases and autoimmune disorders like multiple sclerosis and rheumatoid arthritis [6, 11].

Other names

H4RHH4RGPCR105GPRv53AXOR35BG26Histamine receptor H4Hrh4

Antagonist, Inverse agonist, Agonist