Chemical Name: 3,7-Dihydro-1,3,7-trimethyl-1H-purine-2,6-dione
Biological ActivityCaffeine is a central nervous system stimulant. Antagonist at A1 and A2A adenosine receptors and inhibitor of cyclic nucleotide phosphodiesterases. Mobilizes calcium from intracellular stores and inhibits benzodiazepine binding to GABA receptors.
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Caffeine and the central nervous system: mechanisms of action, biochemical, metabolic and psychostimulant effects.
Nehlig et al.
Brain Res.Brain Res.Rev., 1992;17:139
Caffeine as a psychomotor stimulant: mechanism of action.
Fisone et al.
Cell.Mol.Life Sci., 2004;61:857
Caffeine blocks disruption of blood brain barrier in a rabbit model of Alzheimer's disease.
Chen et al.
Citations for Caffeine
The citations listed below are publications that use Tocris products. Selected citations for Caffeine include:
2 Citations: Showing 1 - 2
Contrasting Effects of the Cytotoxic Anticancer Drug gemcit. and the EGFR Tyrosine Kinase Inhibitor gefi. on NK Cell-Mediated Cytotoxicity via Regulation of NKG2D Ligand in Non-Small-Cell Lung Cancer Cells.
Authors: Okita Et al.
PLoS One 2015;10:e0139809
Acute SimV. inhibits K ATP channels of porcine coronary artery myocytes.
Authors: Seto Et al.
J Cell Sci 2013;8:e66404
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Rats had free access to untreated water or water containing 0.2 mg/ml of caffeine every other day of a 14-day experiment. This dose is relevant to human caffeine intake. Rats were tested on alternated days in an open-field arena for discrete movements (horizontal and vertical) and ambulatory distance. Results showed that although caffeine intake decreased significantly across test sessions, the number of discrete horizontal movements increased significantly, that is, showed sensitization.
HL-1 cells were loaded with cytosolic Ca2+ sensitive dye, Fura-2AM (1 µM)+F127 (0.01%) in normal tyrode solution for 40 min and excited alternately at 340 and 380 nm and fluorescence was captured at 510 nm. When the cells are perfused with 10 mM caffeine in nominally Ca2+ free tyrode solution, caffeine acts on RyR2 to release ER Ca2+, resulting in transient cytosolic peak (shown in the figure).
Control or saxagliptin treated primary guinea pig cardiomyocytes were loaded with FURA-2AM (1 µM) and Pluronic F 127 (1%). Ca2+ transient decay tau evoked by caffeine (30 µM) is shown in the Image. Caffeine acts as a ryanodine receptor agonist and releases Ca2+ from sarcoplasmic reticulum into the cytosol.