Caffeine

stimulant · nervous · Oral

Caffeine, a stimulant. Non-selective adenosine receptor signaling A1/A2A antagonist; PDE inhibition at high doses. Oral half-life 5 h.

Non-selective Adenosine receptor signaling A1/A2A antagonist; PDE inhibition at high doses.

Tolerance develops within 1-2 weeks of daily use. Orexin / wakefulness arousal axis — A2A is the higher-affinity arousal receptor (lower ec50) — caffeine occupies it well below the typical 100 mg dose's Cmax.

Pharmacokinetics

• Oral — t½ 5 h · F 100% · ka 5 h⁻¹ · Vd 36 L

Related compounds

• L-Theanine — synergistic
• Adenosine — caution
• EGCG — synergistic
• Theobromine — synergistic
• Theophylline — caution
• Yohimbine — caution
• Dipyridamole — caution

Sources: PMID:20164566, PMID:6832208, PMID:6886969, PMID:10049999, PMID:7153897