Target intelligence / Profile preview

Adrenergic alpha2 receptor (None)

Target
None
Molecular classification
G protein-coupled receptor (GPCR)
01

Overview

The adrenergic alpha2 receptor (α2-adrenergic receptor) is a G protein-coupled receptor (GPCR) that primarily couples to the Gi/o class of G proteins. It is activated by endogenous catecholamines, mainly norepinephrine and epinephrine, and plays a key role in modulating neurotransmitter release, vascular tone, and central nervous system functions. There are three main subtypes: α2A, α2B, and α2C, each with distinct tissue distributions and physiological roles.

Other names
α2-adrenergic receptorAlpha-2 adrenergic receptorAdrenoceptor alpha 2
02

Mechanism of action

Gi/o protein activation leading to decreased cAMP levels, potassium channel opening, and reduced calcium influx, ultimately inhibiting neurotransmitter release and sympathetic outflow.

03

Biological functions

Signal transductionRegulation of neurotransmitter releaseRegulation of vascular toneModulation of sympathetic tone
04

Disease associations

HypertensionADHDGlaucoma
05

Safety considerations

HypotensionBradycardiaSedationRebound hypertension upon withdrawal
06

Interacting drugs

Clonidine

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