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Target intelligence / Profile preview
Alpha-1 Adrenergic Receptor (α1-AR)
- Target
- α1-AR
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The alpha-1 adrenergic receptor (α1-adrenergic receptor) is a G protein-coupled receptor that is primarily activated by norepinephrine and epinephrine. It mediates physiological responses to sympathetic nervous system activation, including vasoconstriction, smooth muscle contraction, and neurotransmission. There are three subtypes: α1A, α1B, and α1D. Drugs targeting alpha-1 adrenergic receptors include agonists and antagonists, used for conditions such as hypertension and benign prostatic hyperplasia.
- Other names
- Alpha1 adrenergic receptorAdrenergic Receptor Alpha 1alpha-1 adrenoceptorα1 adrenergic receptor
02
Mechanism of action
Activation of Gq/11 proteins leading to phospholipase C activation and increased intracellular calcium levels.
03
Biological functions
Signal transductionVasoconstrictionNeurotransmissionRegulation of neurotransmitter releaseSmooth muscle contractionPupil dilation
04
Disease associations
HypertensionBenign prostatic hyperplasiaCardiovascular diseaseUrinary retentionNeurological disorders
05
Safety considerations
Potential side effects of alpha-blockers (e.g., orthostatic hypotension)Cardiovascular effectsPotential for drug interactions
06
Interacting drugs
Norepinephrine
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