The beta-3 adrenergic receptor (β₃-adrenoceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the human

gene In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a b ...

encoding it.

Function

Actions of the β₃ receptor include *Enhancement of

lipolysis Lipolysis is the metabolic pathway through which lipid triglycerides are hydrolyzed into a glycerol and free fatty acids. It is used to mobilize stored energy during fasting or exercise, and usually occurs in fat adipocytes. The most important ...

adipose tissue Adipose tissue, body fat, or simply fat is a loose connective tissue composed mostly of adipocytes. In addition to adipocytes, adipose tissue contains the stromal vascular fraction (SVF) of cells including preadipocytes, fibroblasts, vascular ...

. *

Thermogenesis Thermogenesis is the process of heat production in organisms. It occurs in all warm-blooded animals, and also in a few species of thermogenic plants such as the Eastern skunk cabbage, the Voodoo lily ('' Sauromatum venosum''), and the giant w ...

skeletal muscle Skeletal muscles (commonly referred to as muscles) are organs of the vertebrate muscular system and typically are attached by tendons to bones of a skeleton. The muscle cells of skeletal muscles are much longer than in the other types of m ...

Page 163 It is located mainly in

and is involved in the regulation of lipolysis and

thermogenesis Thermogenesis is the process of heat production in organisms. It occurs in all warm-blooded animals, and also in a few species of thermogenic plants such as the Eastern skunk cabbage, the Voodoo lily ('' Sauromatum venosum''), and the giant w ...

. Some β₃

agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ag ...

s have demonstrated antistress effects in animal studies, suggesting it also has a role in the central nervous system (CNS). 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 Adrenaline, also known as epinephrine, is a hormone and medication which is involved in regulating visceral functions (e.g., respiration). It appears as a white microcrystalline granule. Adrenaline is normally produced by the adrenal glands and ...

- and

norepinephrine Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad ...

-induced activation of adenylate cyclase through the action of the G proteins of the type G_s.

Ligands

Agonists

* Amibegron (SR-58611A) *

BRL-37344 BRL-37344 is a drug which acts as a selective agonist of the β3 adrenergic receptor, which has been investigated for various biomedical research Medical research (or biomedical research), also known as experimental medicine, encompasses a ...

* CL-316,243 * L-742,791 * L-796,568 * LY-368,842 *

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(YM-178), approved for treatment of overactive bladder in Japan, United States, UK, Canada, China and India. *

Nebivolol Nebivolol is a beta blocker used to treat high blood pressure and heart failure. As with other β-blockers, it is generally a less preferred treatment for high blood pressure. It may be used by itself or with other blood pressure medication. I ...

selective beta(1)-blocker and beta(3)-agonist. * Ro40-2148 * Solabegron (GW-427,353) * Vibegron (MK-4618)

Antagonists

* L-748,328 * L-748,337 * SR 59230A was thought to be a selective β₃

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, ri ...

but later found to also be an antagonist of the α₁ receptor.

Interactions

Beta-3 adrenergic receptor has been shown to

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with Src.

References

External links

* * {{Use dmy dates, date=January 2012 Adrenergic receptors