Adenosine A1 antagonist
Adenosine A1 receptor antagonist
- Little of caffeine’s wakefulness — that runs through A2A (A2A-knockout mice do not wake with caffeine; A1-knockouts do)
- ↑ heart rate/AV conduction
- Promotes diuresis
- Lowers seizure threshold
- Minor part of caffeine’s effect — its arousal is A2A-mediated (Huang 2005: A2A-knockout mice do not wake with caffeine; A1-knockouts do)
- ↑ HR and AV conduction
- Afferent arteriolar vasoconstriction → ↑ glomerular filtration rate (GFR)
- Diuretic effect
- Lipolysis
- ↓ seizure threshold
Drugs with this mechanism (3)
- Aminophylline — Soluble theophylline; a bronchodilator with a narrow therapeutic index.
- Caffeine — The world's most-used stimulant; adenosine antagonist, OTC.
- Theophylline — Old methylxanthine bronchodilator; narrow index, largely supplanted.
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