Target intelligence / Profile preview

Adrenergic alpha-1B receptor (ADRA1B)

Target
ADRA1B
Molecular classification
G protein-coupled receptor, GPCR
01

Overview

The adrenergic alpha-1B receptor (ADRA1B) is a subtype of the alpha-1 adrenergic receptors, a G protein-coupled receptor (GPCR) encoded by the ADRA1B gene. It plays a critical role in sympathetically mediated vasoconstriction, smooth muscle contraction, and cardiac function. Overexpression of ADRA1B can induce neoplastic transformation, identifying it as a proto-oncogene. It's also involved in baroreceptor-mediated cardiovascular responses and may have implications for treating orthostatic intolerance.

Other names
Alpha-1B adrenergic receptorα1B-adrenoreceptor
02

Mechanism of action

Gq/11 protein activation, leading to activation of phosphatidylinositol-calcium second messenger systems. Activation by norepinephrine leads to smooth muscle contraction primarily via vasoconstriction.

03

Biological functions

VasoconstrictionSmooth muscle contractionCardiac effectsCell growthCell proliferationSignal transduction
04

Disease associations

Cardiovascular diseaseOrthostatic intoleranceCancer
05

Safety considerations

Potential for neoplastic transformation when overexpressed
06

Interacting drugs

Cyclazosin

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