Cimetidine

Cimetidine is a histamine-2 (H2) receptor antagonist.(In Vitro):Cimetidine (SKF-92334), a partial agonist for H2R, has a pharmacological profile different from ranitidine and famotidine, possibly contributing to its antitumor activity on gastrointestinal cancers . Cimetidine had no effect on the uptake and cytotoxicity of cisplatin in ovarian cancer cells with high OCT2 mRNA levels (IGROV-1 cells).Cimetidine showed no effect on proliferation, survival, migration and invasion of 3LL cells. Cimetidine reversed MDSC-mediated T-cell suppression, and improved IFN-γ production.Cimetidine-mediated down-regulation of NCAM involved suppression of the nuclear translocation of NF-kappaB, a transcriptional activator of NCAM gene expression.(In Vivo):Cimetidine (SKF-92334) reduceS CD11b(+)Gr-1(+) myeloid derived-suppressive cell (MDSC) accumulation in spleen, blood and tumor tissue of tumor-bearing mice.Cimetidine exerts a beneficial effect on periodontal disease in rats, decreasing the RANKL/OPG ratio in gingival connective tissue and reducing alveolar bone resorption.