Gosset Alpha-1 Adrenergic Receptor Overview
The alpha-1 adrenergic receptor (α1-AR) is a G protein-coupled receptor activated by norepinephrine and epinephrine. It plays a key role in mediating physiological responses to sympathetic nervous system activation, including vasoconstriction, smooth muscle contraction, and modulation of neurotransmission. There are three subtypes: α1A, α1B, and α1D. The primary signaling pathway involves Gq/11-mediated activation of phospholipase C, leading to increased intracellular calcium levels. Drugs targeting α1-ARs are used to treat conditions like hypertension and benign prostatic hyperplasia. Alterations in these receptors may contribute to various disease states involving cardiovascular and neuropsychiatric function.
Mechanism of Action
Activation of Gq/11 proteins, leading to activation of phospholipase C, production of IP3/DAG, and increased intracellular Ca²⁺ levels.
Biological Functions
Disease Associations
Safety Considerations
- Hypotension (with antagonists)
- Reflex tachycardia (with antagonists)
- Dizziness (with antagonists)
- Potential for drug interactions