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Target intelligence / Profile preview
Alpha1-Adrenoceptor (α1-AR)
- Target
- α1-AR
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The alpha1-adrenoceptor (α1-adrenergic receptor) is a G-protein coupled receptor that mediates responses to norepinephrine and epinephrine. It plays a key role in regulating the sympathetic nervous system, influencing vasoconstriction, smooth muscle contraction, and neurotransmission. There are three main subtypes: α1A, α1B, and α1D. These receptors are therapeutic targets for several conditions including hypertension and benign prostatic hyperplasia.
- Other names
- Alpha1-adrenergic receptorα1-adrenergic receptorADRA1
02
Mechanism of action
Agonists activate the receptor, stimulating phospholipase C via Gq proteins, leading to increased IP3 and DAG levels, and a rise in intracellular calcium. Antagonists block the receptor, preventing activation and downstream signaling.
03
Biological functions
Signal transductionVasoconstrictionSmooth muscle contractionNeurotransmission modulationSynaptic plasticity
04
Disease associations
HypertensionHeart failureBenign prostatic hyperplasiaGlaucomaSexual dysfunctionCancer
05
Safety considerations
Hypotension (with antagonists)Reflex tachycardia (with antagonists)
06
Interacting drugs
Norepinephrine
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