Target intelligence / Profile preview

Alpha₁A adrenergic receptor

Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The Alpha₁A adrenergic receptor (α1A adrenoreceptor), encoded by the ADRA1A gene, is a subtype of the alpha-1 adrenergic receptors and belongs to the G protein-coupled receptor (GPCR) superfamily. Activation leads to stimulation of phospholipase C (PLC), generating second messengers inositol trisphosphate (IP3) and diacylglycerol (DAG), resulting in increased intracellular calcium levels. It is highly expressed in smooth muscle cells throughout blood vessels and other tissues, mediating vasoconstriction. It also plays roles in neurotransmission within the CNS and participates in the development/growth/functioning of heart tissue. Alpha₁-adrenoceptors are targets for drugs treating hypertension or benign prostatic hyperplasia.

Other names
ADRA1Aalpha-1A adrenoreceptoralpha-1C adrenergic receptor (historical)
02

Mechanism of action

Agonist or antagonist binding to the Alpha₁A adrenergic receptor modulating downstream signaling via Gq/11 proteins and phospholipase C activation.

03

Biological functions

Signal transductionVasoconstrictionSmooth muscle contractionNeurotransmissionCardiac growthCardiac protection
04

Disease associations

HypertensionBenign prostatic hyperplasiaCognition disordersNeurotransmission disorders
05

Interacting drugs

Norepinephrine

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