Cimetidine (SKF-92334) hydrochloride is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride shows anti-cancer and anti-inflammatory activity. Cimetidine hydrochloride is a gastric acid reducer that can be used in the research of duodenal and gastric ulcers[1] [2] [5].

H2 receptor:.6 μM (Kd)

Cimetidine (SKF-92334) hydrochloride, a partial agonist for H2R, has a pharmacological profile different from ranitidine and famotidine, possibly contributing to its antitumor activity on gastrointestinal cancers [1]. Cimetidine hydrochloride has no effect on the uptake and cytotoxicity of cisplatin in ovarian cancer cells with high OCT2 mRNA levels (IGROV-1 cells) [3]. Cimetidine hydrochloride shows no effect on proliferation, survival, migration and invasion of 3LL cells. Cimetidine hydrochloride reverses MDSC-mediated T-cell suppression, and improves IFN-γ production [4]. Cimetidine-mediated down-regulation of NCAM involved suppression of the nuclear translocation of NF-kappaB, a transcriptional activator of NCAM gene expression [5].

Cimetidine (SKF-92334) hydrochloride reduces CD11b(+)Gr-1(+) myeloid derived-suppressive cell (MDSC) accumulation in spleen, blood and tumor tissue of tumor-bearing mice [4]. Cimetidine hydrochloride exerts a beneficial effect on periodontal disease in rats, decreasing the RANKL/OPG ratio in gingival connective tissue and reducing alveolar bone resorption [6].