Target intelligence / Profile preview

Alpha1A-Adrenoceptor (ADRA1A)

Target
ADRA1A
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The Alpha1A-adrenoceptor (α1A-adrenoreceptor), also known as ADRA1A, is a subtype of the alpha-1 adrenergic receptor family. This receptor is a G protein-coupled receptor (GPCR) that primarily couples to the Gq/11 family of G proteins, leading to activation of phospholipase C and increases in intracellular calcium. It is involved in vasoconstriction, smooth muscle contraction, and neurotransmission, and is a therapeutic target for conditions like hypertension and benign prostatic hyperplasia. Endogenous ligands include norepinephrine and epinephrine.

Other names
Alpha-1A adrenergic receptoralpha1A-adrenoreceptorADRA1A receptorAlpha-1C adrenergic receptor (obsolete)
02

Mechanism of action

Agonists cause vasoconstriction and smooth muscle contraction by activating Gq/11 signaling, increasing IP3 and DAG, leading to calcium release. Antagonists block this activation, causing vasodilation and smooth muscle relaxation.

03

Biological functions

Signal transductionVasoconstrictionSmooth muscle contractionNeurotransmission
04

Disease associations

HypertensionBenign prostatic hyperplasiaCardiovascular disease
05

Safety considerations

Over-stimulation can lead to excessive vasoconstriction and hypertension.Alpha-blockers can cause hypotension.
06

Interacting drugs

Norepinephrine

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