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Target intelligence / Profile preview
Norepinephrine Alpha2 Receptor (α2-AR)
- Target
- α2-AR
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The norepinephrine alpha 2 adrenergic receptors are key regulators within both peripheral sympathetic nerves and central neural circuits. Their pharmacological modulation underpins several therapeutic strategies for cardiovascular disease management (e.g., hypertension), pain control without opioids (analgesia), sedation during medical procedures or intensive care settings—and even cognitive enhancement therapies for disorders like ADHD through selective subtype targeting.
- Other names
- Alpha-2 adrenergic receptorAdrenergic receptor alpha 2Alpha2 adrenoceptor
02
Mechanism of action
Gi/o protein activation → ↓ Adenylyl cyclase → ↓ cAMP → Inhibition of neurotransmitter release
03
Biological functions
Signal transductionNeurotransmitter release modulationVascular tone regulationBlood pressure regulationSedationAnalgesiaNegative feedback control of norepinephrine release
04
Disease associations
HypertensionADHDAnxiety disordersPainCardiovascular disease
05
Safety considerations
HypotensionSedationBradycardia
06
Interacting drugs
Clonidine
3 more in the full profile.
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