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Adrenergic alpha 2A receptor (α2A adrenoceptor)
- Target
- α2A adrenoceptor
- Molecular classification
- G protein-coupled receptor (GPCR)
01
Overview
The Adrenergic alpha 2A receptor (α2A adrenoceptor or ADRA2A) is a subtype of the alpha-2 adrenergic receptors, which are G protein-coupled receptors (GPCRs) involved in mediating physiological responses to catecholamines such as norepinephrine and epinephrine. It plays a key role in inhibiting neurotransmitter release, regulating vascular tone, and influencing cognitive functions. Agonists are used for hypertension, sedation, and ADHD treatment, while antagonists have been explored for reversing sedation and treating sexual dysfunction. Recent structural studies have provided insights into ligand binding and drug design.
- Other names
- ADRA2Aalpha-2A adrenergic receptor
02
Mechanism of action
Agonists activate the receptor, inhibiting adenylate cyclase and decreasing cAMP levels. Antagonists block the receptor, preventing activation by agonists.
03
Biological functions
Inhibition of adenylate cyclaseNeurotransmitter release inhibitionRegulation of vascular toneCognitive function enhancementGlucose homeostasisFear response modulationNegative regulation of insulin secretionIntestinal absorptionDNA replication control
04
Disease associations
HypertensionADHD
05
Interacting drugs
Norepinephrine
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