Cimetidine (hydrochloride)

Cimetidine (SKF-92334) hydrochloride is an orally active, inverse and BBB-permeable histamine H2 receptor antagonist with a K_i of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity^[1][2][5]. In Vitro: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].
In Vivo: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].