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Target intelligence / Profile preview
Adrenergic Alpha 1 Receptor (α₁)
- Target
- α₁
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The adrenergic alpha 1 (α1) receptor is a G protein-coupled receptor that mediates the effects of norepinephrine and epinephrine. It has three subtypes (α1A, α1B, α1D) and is primarily responsible for vasoconstriction, smooth muscle contraction, and modulation of neurotransmission. Activation of α1 receptors leads to increased intracellular calcium levels through the Gq/11-PLC-IP3/DAG pathway. α1 agonists are used to treat hypotension, while antagonists are used to treat hypertension and benign prostatic hyperplasia.
- Other names
- Alpha 1 Adrenergic Receptorα1-adrenergic receptorAdrenoceptor alpha 1
02
Mechanism of action
Agonists activate the receptor, leading to Gq/11 protein activation, PLC stimulation, IP3/DAG production, and increased intracellular calcium levels. Antagonists block the receptor, preventing catecholamine-induced activation and downstream signaling.
03
Biological functions
VasoconstrictionSmooth muscle contractionModulation of neurotransmissionSignal transduction
04
Disease associations
HypertensionBenign prostatic hyperplasiaCardiovascular disease
05
Safety considerations
Hypotension (with antagonists)Hypertension (with agonists)
06
Interacting drugs
Norepinephrine
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