Beta-3 adrenergic receptor

The beta-3 adrenergic receptor, also known as ADRB3, is a beta-adrenergic receptor, and also denotes the human gene encoding it.

Function

Actions of the β₃ receptor include

Enhancement of lipolysis in adipose tissue.
Thermogenesis in skeletal muscle

It is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis. Some β₃ agonists have demonstrated antistress effects in animal studies, suggesting it also has a role in the central nervous system. β₃ receptors are found in the gallbladder, urinary bladder, and in brown adipose tissue. Their role in gallbladder physiology is unknown, but they are thought to play a role in lipolysis and thermogenesis in brown fat. In the urinary bladder it is thought to cause relaxation of the bladder and prevention of urination.

Mechanism of action

Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase through the action of the G proteins of the type G_s.

Ligands

Agonists

Approved for clinical use

Mirabegron, approved for treatment of overactive bladder in Japan, United States, UK, Canada, China and India.
Nebivolol selective beta-blocker and beta-agonist.
Vibegron

Experimental

Amibegron
BRL-37344
CL-316,243
L-742,791
L-796,568
LY-368,842
Ro40-2148
Solabegron

Antagonists

L-748,328
L-748,337
SR 59230A was thought to be a selective β₃ antagonist but later found to also be an antagonist of the α₁ receptor.

Interactions

Beta-3 adrenergic receptor has been shown to interact with Src.