Gosset Molecular Classification
G protein-coupled receptor, Receptor
Other Names
Alpha1-adrenergic receptor, α1-adrenergic receptor, ADRA1
Disease Roles
Alpha1-Adrenoceptor 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.
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.
Biological Functions
Signal transduction
Vasoconstriction
Smooth muscle contraction
Neurotransmission modulation
Synaptic plasticity
Disease Associations
Hypertension
Heart failure
Benign prostatic hyperplasia
Glaucoma
Sexual dysfunction
Cancer
Safety Considerations
- Hypotension (with antagonists)
- Reflex tachycardia (with antagonists)
Interacting Drugs
Norepinephrine