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Target intelligence / Profile preview
Adrenergic Alpha1 Receptor (α1-AR)
- Target
- α1-AR
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The adrenergic alpha1 receptor (α1-AR) is a G protein-coupled receptor that mediates various physiological responses, most notably smooth muscle contraction and vasoconstriction. It is primarily activated by norepinephrine and epinephrine. There are three subtypes: α1A, α1B, and α1D, each with distinct tissue distributions and functions. Activation leads to stimulation of phospholipase C (PLC) via Gq/11 proteins, resulting in increased intracellular calcium and activation of protein kinase C. Alpha‐blockers targeting these receptors are used therapeutically for hypertension and benign prostatic hyperplasia.
- Other names
- Alpha1-adrenergic receptorα1-adrenergic receptorAlpha-1 adrenergic receptor
02
Mechanism of action
Gq/11 → PLC → IP3/DAG → ↑Ca²⁺/PKC, leading to smooth muscle contraction and other cellular effects.
03
Biological functions
Signal transductionSmooth muscle contractionVasoconstrictionNeurotransmissionRegulation of blood pressureCardiac contractility regulationEjaculationPupil dilationCell growth
04
Disease associations
HypertensionBenign prostatic hyperplasiaCardiovascular diseasesAutonomic dysfunction
05
Safety considerations
Hypotension (due to excessive vasodilation)DizzinessNasal congestion
06
Interacting drugs
Norepinephrine
2 more in the full profile.
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