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adenosine receptor agonist, CNS stimulant

An adenosine receptor ligand and a major metabolite of caffeine

Paraxanthine is an inhibitor of phosphodiesterase 9 (PDE9) and an antagonist of adenosine receptors A₁ and A₂ (K_is = 35 and 22 μM, respectively in equine forebrain tissues). It is the main metabolite of caffeine (Item No. 14118) in humans, making up 80% of the three dimethylxanthine metabolites produced by caffeine demethylation. Paraxanthine increases locomotor activity and counteracts adenosine receptor agonist-induced motor depression in rats not habituated to caffeine. At a dose of 30 mg/kg, paraxanthine induces a significant increase in striatal cGMP and extracellular striatal dopamine concentrations in vivo. It also promotes wakefulness and increases locomotor activity and core temperature in narcoleptic transgenic mice without increasing behavioral anxiety.

ChEBI: 1,7-dimethylxanthine is a dimethylxanthine having the two methyl groups located at positions 1 and 7. It is a metabolite of caffeine and theobromine in animals. It has a role as a central nervous system stimulant, a human xenobiotic metabolite, a human blood serum metabolite and a mouse metabolite.

Adenosine receptor ligand; major metabolite of caffeine

An experimental teratogen. Mutation data reported. Whenheated to decomposition it emits toxic fumes of NOx.