The histamine H receptor as a new therapeutic target for inflammation

The role of histamine in human mammary carcinogenesis: H3 and H4 receptors as potential therapeutic targets for breast cancer treatment.

“…Histamine exerts its functions through binding to G-protein-associated histamine H1, H2, H3, H4 receptors (H1R, H2R, H3R, H4R), resulting in activation of different signal transduction pathways. [9][10][11][12] High histamine biosynthesis and content has been reported in different human neoplasias including breast cancer, as well as in experimental tumors induced in rodents. 5,[13][14][15] We have previously reported that H1R and H2R are present in different normal and malignant cell lines and benign lesions and tumors derived from human mammary gland.…”

“…[23][24][25][26][27] On the other hand, H4R is predominantly expressed in bone marrow, eosinophils and mast cells. [10][11][12]28,29 Recently, we have demonstrated that H3R and H4R are expressed in cell lines derived from human mammary gland. In addition, histamine is capable of modulating cell proliferation exclusively in malignant cells while no effect is observed in non-tumorigenic cells.…”

Histamine reverses IL-5-afforded human eosinophil survival by inducing apoptosis: Pharmacological evidence for a novel mechanism of action of histamine

“…Moreover, during receptor. [19,37] Moreover, at least some antagonism by thioperamide, JNJ7777120 and MMPCI would have been expected at the H 4 receptor [19,35] even though histamine was used with a much higher concentration than its affinity for the H 4 receptor subtype [19]. In previous studies evaluating the H 4 receptor-mediated effects of histamine on eosinophils, the A c c e p t e d m a n u s c r i p t effects of similar histamine concentrations were antagonized with similar thioperamide and JNJ7777120 concentrations and agonized with similar clobenpropit concentrations as used in the present study.…”

“…subtype [12,13,16,17,20,21,37,47]. Moreover, human eosinophils have recently been shown not to express the histamine H 3 receptor.…”

“…5B). To exclude the possibility that the high concentration of histamine (100 µM) used in these experiments would, by competition, limit the degree of antagonism produced by JNJ7777120, we also tested the effect of 10 µM JNJ7777120 on eosinophil apoptosis induced by 10 µM nM [37]; clobenpropit = 8 nM [19]). …”