Adenosine A2A antagonist
Adenosine A2A receptor antagonist
- Blocks adenosine sleep pressure → wakefulness — the arousal arm of caffeine (A2A-knockout mice do not wake with caffeine)
- The arousal arm of caffeine — A2A-knockout mice do not wake with caffeine (Huang 2005; nucleus accumbens shell, Lazarus 2011)
- Vasoconstriction
- Striatal A2A blockade → ↓ Parkinson “off” time
- Pro-inflammatory effects
Drugs with this mechanism (3)
- Caffeine — The world's most-used stimulant; adenosine antagonist, OTC.
- Istradefylline — Non-dopaminergic adenosine A2A antagonist adjunct for Parkinson off time.
- Theophylline — Old methylxanthine bronchodilator; narrow index, largely supplanted.
Self-check
- What happens to caffeine-induced arousal in A2A-knockout mice?
They do not wake with caffeine. - What Parkinson disease fluctuation can striatal A2A blockade reduce?
Off time.
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