Drug intelligence / Profile preview

caffeine + methylliberine

Development stage
Unknown
Lead developer
Compound Solutions
Modality
Small Molecules
Administration
Oral
01

Overview

Caffeine + methylliberine is a combination of two purine alkaloids used primarily as dietary supplements for their stimulant effects. Caffeine is a methylxanthine acting as a central nervous system stimulant, largely through antagonist activity at adenosine receptors, resulting in increased alertness and reduced drowsiness. Methylliberine is a methoxiuric acid derivative and a metabolite of caffeine, naturally present in Coffea species at low levels; it modulates adenosine receptors with a similar but somewhat milder stimulant profile, and is hypothesized to have less anxiety-inducing potential than caffeine. When co-administered, methylliberine increases the half-life and area under the curve (AUC) of caffeine via inhibition of CYP1A2 metabolism, potentially prolonging its stimulant effects. The combination produces synergistic and prolonged actions on alertness, focus, and mood, and is frequently encountered in functional food products and dietary supplements targeting energy and cognitive performance. Human studies show no significant adverse cardiovascular effects for methylliberine, but caffeine remains associated with classic increases in blood pressure and heart rate[1][3][4][2].

Other names
2-methoxy-1,7,9-trimethylpurine-6,8-dioneO(2),1,7,9-tetramethyluratepurine alkaloidmethylxanthine derivativemethoxiuric acid
02

Targets

ADOR (Adenosine receptors)CYP1A2 (Cytochrome P450 1A2)

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