Target intelligence / Profile preview

Adrenergic α₁A Receptor

Molecular classification
G protein-coupled receptor
01

Overview

The Adrenergic α₁A Receptor (ADRA1A) is a G protein-coupled receptor that primarily responds to adrenaline and noradrenaline. It mediates smooth muscle contraction in various tissues, including blood vessels, urethral sphincter, and iris dilator muscle. It also plays a role in cognitive function and neurotransmission within the central nervous system. Drugs targeting this receptor are used to treat hypertension and benign prostatic hyperplasia.

Other names
Alpha-1A adrenergic receptorα1A adrenoreceptorADRA1AAlpha-1C adrenergic receptor (historical; now obsolete)
02

Mechanism of action

Agonist-induced activation of Gq/11 proteins, leading to activation of phospholipase C (PLC) and increased intracellular calcium levels; Antagonist-induced blockade of receptor activation

03

Biological functions

Smooth muscle contractionVasoconstrictionUrethral sphincter contractionIris dilator muscle contractionEjaculationCognitive functionNeurotransmission regulationSignal transduction
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Disease associations

HypertensionBenign prostatic hyperplasia
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Safety considerations

Potential cardiovascular side effects with non-selective alpha-adrenergic antagonistsOrthostatic hypotension
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Interacting drugs

Adrenaline (epinephrine)

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