The structure of cyclocreatine is fairly flat (planar), which aids in passive diffusion across membranes. It has been used with success in an animal study, where mice suffered from a SLC6A8 (creatine transporter at the blood brain barrier) deficiency, which is not responsive to standard creatine supplementation.  This study failed to report increases in creatine stores in the brain, but noted a reduction of mental retardation associated with increased cyclocreatine and phosphorylated cyclocreatine storages.  As demonstrated by this animal study and previous ones, cyclocreatine is bioactive after oral ingestion   and may merely be a creatine mimetic, able to phosphorylate ADP via the creatine kinase system. 
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