Target intelligence / Profile preview

Adrenergic Beta-3 Receptor (ADRB3)

Target
ADRB3
Molecular classification
G protein-coupled receptor, GPCR, Class A rhodopsin-type GPCR, Receptor
01

Overview

The Adrenergic Beta-3 Receptor (ADRB3) is a G protein-coupled receptor primarily expressed in adipose tissue, gallbladder, and urinary bladder. It plays a key role in regulating lipolysis, thermogenesis, and bladder relaxation. ADRB3 variants have been associated with increased risk for obesity and diabetes. Agonists like mirabegron are used to treat overactive bladder.

Other names
Beta-3 adrenergic receptorβ₃-adrenoceptor
02

Mechanism of action

Catecholamine-induced activation leading to stimulation of adenylate cyclase through Gs proteins, increasing cyclic AMP levels.

03

Biological functions

Regulation of lipolysisThermogenesisBladder relaxationSignal transduction
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Disease associations

ObesityNon-insulin-dependent diabetes mellitusOveractive bladderMetabolic disorders
05

Safety considerations

Potential cardiovascular effects (though less pronounced than with other beta-adrenergic receptors)Off-target effects of some ligands (e.g., SR59230A also blocks α₁ receptors)
06

Interacting drugs

Mirabegron

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