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Target intelligence / Profile preview
Alpha-2 Adrenergic Receptor A Subtype (α2A-AR)
- Target
- α2A-AR
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The alpha-2 adrenergic receptor A subtype (α2A-AR) is a G protein-coupled receptor that plays a key role in regulating sympathetic outflow, neurotransmitter release, and pain. Activation of α2A-AR inhibits adenylyl cyclase activity. It is a therapeutic target for hypertension, sedation, and analgesia. Selective agonists like dexmedetomidine are used clinically, but sedation is a potential side effect. There are species differences in ligand binding profiles between human α2A and rodent α2D.
- Other names
- ADRA2AAlpha2A AdrenoceptorAlpha-2A Adrenergic Receptor
02
Mechanism of action
Gi/o-mediated inhibition of adenylyl cyclase
03
Biological functions
Signal transductionInhibition of sympathetic outflowRegulation of neurotransmitter releaseAnalgesia
04
Disease associations
HypertensionPainAnxietyDepression
05
Safety considerations
SedationHypotension
06
Interacting drugs
Norepinephrine
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