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Adrenergic alpha-2 receptor (α2-adrenergic receptor)
- Target
- α2-adrenergic receptor
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The adrenergic alpha 2 receptor is a GPCR with three main subtypes that mediate inhibition of adenylyl cyclase via Gi proteins—leading to reduced cAMP levels—and play crucial roles both centrally (sedation/cognition/neurotransmission) and peripherally (vascular tone/blood pressure). Clinically important agonists target these receptors for conditions ranging from hypertension to ADHD or procedural sedation.
- Other names
- Alpha-2 adrenergic receptorα2-adrenoceptorADRA2
02
Mechanism of action
Agonists bind to the α2-adrenergic receptor, activating Gi proteins. This leads to inhibition of adenylyl cyclase, decreased cAMP levels, hyperpolarization of neurons, and reduced neurotransmitter release.
03
Biological functions
Neurotransmitter release modulationVascular tone regulationSignal transductionInhibition of adenylyl cyclaseRegulation of cAMP levels
04
Disease associations
HypertensionADHDSedationAnalgesia
05
Safety considerations
HypotensionBradycardiaSedationSympatholytic effects
06
Interacting drugs
Clonidine
3 more in the full profile.
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