Molecular Classification
G-protein coupled receptor (GPCR), Receptor
Other Names
Alpha 1-Adrenergic Receptor, α1-Adrenergic Receptor, Alpha1-Adrenoceptor
Disease Roles
HypertensionHypotensionShock

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

Signal transduction
Vasoconstriction
Smooth muscle contraction
Neurotransmission
Synaptic plasticity
Regulation of blood pressure
Redistribution of blood flow

Disease Associations

Hypertension
Hypotension
Shock
Benign Prostatic Hyperplasia (BPH)
Cognitive dysfunction

Safety Considerations

  • Side effects associated with vasoconstriction (e.g., increased blood pressure)
  • Potential for drug interactions

Interacting Drugs

Norepinephrine
Epinephrine
Alpha 1-receptor agonists
Alpha 1-receptor antagonists