Target intelligence / Profile preview

Spinal Alpha-2 Adrenergic Receptor (α2-AR)

Target
α2-AR
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

The spinal alpha-2 adrenergic receptor is a G protein-coupled receptor that mediates the effects of catecholamines, primarily norepinephrine and epinephrine, within the spinal cord. It plays a crucial role in modulating neurotransmitter release, neuronal excitability, and pain transmission. There are three main subtypes: α2A, α2B, and α2C, with α2A being the predominant subtype involved in analgesia. Activation of these receptors leads to inhibition of adenylyl cyclase, decreased cAMP production, and reduced neurotransmitter release, ultimately resulting in analgesia and other systemic effects like sedation and hypotension.

Other names
Spinal Adrenergic Receptor Alpha 2Spinal Alpha2 AdrenoceptorSpinal α2 Adrenergic Receptor
02

Mechanism of action

Gi protein activation, inhibition of adenylyl cyclase, decreased cAMP production, reduced PKA activity, hyperpolarization via increased potassium efflux, inhibition of voltage-gated calcium channels, reduced neurotransmitter release.

03

Biological functions

Signal transductionInhibition of neurotransmitter releaseRegulation of neuronal excitabilityModulation of pain transmission
04

Disease associations

Pain (Neuropathic, Inflammatory)HypertensionAnxietySpasticity
05

Safety considerations

HypotensionBradycardiaSedationRespiratory depressionToleranceDependence
06

Interacting drugs

Clonidine

4 more in the full profile.

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