Adenosine reuptake inhibitor
Adenosine reuptake inhibitor (equilibrative nucleoside transporter blocker)
- Adenosine stays extracellular
- ↑ adenosine → vasodilation and reduced platelet aggregation
- Adenosine boluses must be reduced
- A1 receptors are the brain’s own brake on seizures
- ↓ glutamate release, K⁺ hyperpolarization — proposed for cannabidiol
- A2A carries the anti-inflammatory arm (↓ TNF-α)
- Inhibits Equilibrative Nucleoside Transporter (ENT)
- Blocks adenosine reuptake into red blood cells and endothelial cells → vasodilation and antiplatelet effects
- ➔ for stroke prevention
- ➔ used in cardiac stress testing
- ➔ adenosine-mediated side effects ◇ dyspnea, bradyarrhythmias
- A1 receptors are the brain’s own brake on seizures
- ➔ ↓ presynaptic glutamate release; postsynaptic K⁺ efflux hyperpolarizes the neuron
- ➔ proposed contributor to cannabidiol’s antiseizure effect
Drugs with this mechanism (3)
- Cannabidiol — Purified, nonintoxicating cannabinoid for severe developmental epilepsies.
- Dipyridamole — Antiplatelet vasodilator; used with aspirin and for cardiac stress testing.
- Ticagrelor — Reversible P2Y12 antiplatelet; twice-daily, causes dyspnea.
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