Alpha 1-Adrenoreceptor Overview
The alpha 1-adrenoreceptor (α1-adrenergic receptor) is a G-protein coupled receptor that binds catecholamines like norepinephrine and epinephrine. It has three subtypes (α1A, α1B, α1D) and mediates sympathetic "fight-or-flight" effects via smooth muscle contraction, primarily vasoconstriction. It also plays roles in neural signaling related to cognition and synaptic plasticity. Dysregulation can lead to conditions such as hypertension, hypotension, and cognitive dysfunction.
Mechanism of Action
Alpha 1-adrenoreceptors are coupled to Gq/11 proteins. Upon activation by agonists, they stimulate phospholipase C, leading to increased production of inositol trisphosphate (IP3) and diacylglycerol (DAG). This cascade results in elevated intracellular calcium levels and subsequent cellular responses.
Biological Functions
Disease Associations
Safety Considerations
- Side effects associated with vasoconstriction (e.g., increased blood pressure)
- Potential for drug interactions