Target intelligence / Profile preview

Alpha-1B adrenergic receptor (ADRA1B) (ADRA1B)

Target
ADRA1B
Molecular classification
G protein-coupled receptor, Receptor, Adrenergic receptor
01

Overview

The Alpha-1B adrenergic receptor (ADRA1B) is a member of the G protein-coupled receptor (GPCR) superfamily that mediates the physiological actions of the endogenous catecholamines, epinephrine and norepinephrine (UniProt: P35368). Upon activation, ADRA1B primarily couples to Gq/11 proteins, which stimulates phospholipase C activity and increases intracellular calcium concentrations, leading to smooth muscle contraction (NCBI Gene: 147). This receptor is prominently expressed in the vascular system, where it plays a critical role in maintaining vascular tone and regulating systemic blood pressure (PubMed: 1640291). In addition to its cardiovascular functions, ADRA1B is found in the central nervous system and may influence various behavioral and physiological processes (PubMed: 10430521). Clinically, it is a target for alpha-1 adrenergic antagonists like prazosin and doxazosin, which are used to treat hypertension and the urinary symptoms associated with benign prostatic hyperplasia (StatPearls: NBK539830). However, because these drugs often target multiple alpha-1 subtypes, they can cause side effects such as orthostatic hypotension and syncope, particularly during the initiation of therapy (PubChem: CID 4893). Research also suggests that ADRA1B may be involved in cardiac hypertrophy and certain neurological conditions, making it a subject of ongoing pharmacological interest (PubMed: 11752102).

Other names
Alpha-1B adrenoceptorAlpha-1B adrenoreceptorADRA1BAlpha-1B-ARADRA1
02

Mechanism of action

Antagonism of the alpha-1B adrenergic receptor inhibits the Gq-mediated signaling pathway, leading to relaxation of vascular smooth muscle and a decrease in peripheral vascular resistance (StatPearls: NBK539830).

03

Biological functions

Signal transductionSmooth muscle contractionVasoconstrictionRegulation of blood pressure
04

Disease associations

HypertensionCardiovascular diseaseBenign prostatic hyperplasia
05

Safety considerations

Orthostatic hypotensionFirst-dose phenomenonDizzinessReflex tachycardia
06

Interacting drugs

Prazosin

5 more in the full profile.

07

Biomarkers

Blood pressureHeart rate

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