We investigated the activation of transient receptor potential cation channel (TRP) subfamily V, member 1 (TRPV1) and TRP subfamily A, member 1 (TRPA1) by 1'-acetoxychavicol acetate (ACA), the main pungent component in galangal. ACA did not activate TRPV1-expressing human embryonic kidney (HEK) cells, but strongly activated TRPA1-expressing HEK cells. ACA was more potent than allyl isothiocyana...

Because of the importance of intracellular unbound drug concentrations in the prediction of in vivo concentrations that are determinants of drug efficacy and toxicity, a number of assays have been developed to assess in vitro unbound concentrations of drugs. Here we present a rapid method to determine the intracellular unbound drug concentrations in cultured cells, and we apply the method along...

BACKGROUND Xenograft rejection of pigs organs with an engineered mutation in the GGTA-1 gene (GTKO) remains a predominantly antibody mediated process which is directed to a variety of non-Gal protein and carbohydrate antigens. We previously used an expression library screening strategy to identify six porcine endothelial cell cDNAs which encode pig antigens that bind to IgG induced after pig-to...

The effect of endocytosis inhibitors on 5-hydroxytryptamine(2A) (5-HT(2A)) receptor desensitization and resensitization was examined in transiently transfected human embryonic kidney (HEK) 293 cells and in C6 glioma cells that endogenously express 5-HT(2A) receptors. In HEK-293 cells, 5-HT(2A) receptor desensitization was unaffected by cotransfection with a dominant-negative mutant of dynamin (...

The strategy of the nucleophilic substitution hydrogen (SNH) was first applied for metal-free C-H/C-H coupling reactions 4H-imidazole 3-oxides with indoles. As a result, series novel bifunctional azaheterocyclic derivatives were obtained in yields up to 95%. In silico experiments on molecular docking performed evaluate binding possibility synthesized small molecules selected biotargets (BACE1, ...

Aim: Dexmedetomidine; it is widely used in anesthesia and intensive care. We aimed to examine compare the cytotoxic, reactive oxygen species (ROS) apoptotic effects of dexmedetomidine on kidney cells (Hek-293) vitro at two different high cumulative doses. Material Methods: The half-maximum inhibitory concentration (IC50) dose Hek-293 was determined using 3-[4,5-dimethylthiazol-2yl]-2,5-diphenyl...