Beta-3 adrenergic receptor: Difference between revisions
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==Antagonists== |
==Antagonists== |
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* [[SR 59230A]] <ref name="pmid8569714">{{cite journal | author = Nisoli E, Tonello C, Landi M, Carruba MO | title = Functional studies of the first selective β<sub>3</sub>-adrenergic receptor antagonist SR 59230A in rat brown adipocytes | journal = Mol. Pharmacol. | volume = 49 | issue = 1 | pages = 7–14 | year = 1996 | pmid = 8569714 | doi = | issn = }}</ref> |
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==See also== |
==See also== |
Revision as of 22:17, 19 August 2008
Template:PBB The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is an beta-adrenergic receptor, and also denotes the human gene encoding it.[1]
Receptor
Functions
Actions of the β3 receptor include:
- Enhancement of lipolysis in adipose tissue.
- Thermogenesis in skeletal muscle[2]
It is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis. Some β3 agonists have demonstrated antidepressant effects in animal studies, suggesting it also has a role in the CNS.
Mechanism
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 Gs.[1]
Agonists
- Amibegron (SR-58611A)[3][4]
- Solabegron (GW-427,353)[5]
- L-796,568[6]
- CL-316,243[7]
- LY-368,842
- Ro40-2148
Antagonists
See also
- Other adrenergic receptors
References
- ^ a b "Entrez Gene: ADRB1 adrenergic, beta-1-, receptor". Cite error: The named reference "entrez" was defined multiple times with different content (see the help page).
- ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 163
- ^ Consoli D, Leggio GM, Mazzola C, Micale V, Drago F. Behavioral effects of the beta3 adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs? European Journal of Pharmacology. 2007 Nov 14;573(1-3):139-47. PMID 17669397
- ^ Overstreet DH, Stemmelin J, Griebel G. Confirmation of antidepressant potential of the selective beta3 adrenoceptor agonist amibegron in an animal model of depression. Pharmacology, Biochemistry and Behaviour. 2008 Jun;89(4):623-6. PMID 18358519
- ^ Hicks A, McCafferty GP, Riedel E, Aiyar N, Pullen M, Evans C, Luce TD, Coatney RW, Rivera GC, Westfall TD, Hieble JP. GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. Journal of Pharmacology and Experimental Therapeutics. 2007 Oct;323(1):202-9. PMID 17626794
- ^ Larsen TM, Toubro S, van Baak MA, Gottesdiener KM, Larson P, Saris WH, Astrup A (2002). "Effect of a 28-d treatment with L-796568, a novel β3-adrenergic receptor agonist, on energy expenditure and body composition in obese men". Am. J. Clin. Nutr. 76 (4): 780–8. PMID 12324291.
{{cite journal}}
: CS1 maint: multiple names: authors list (link) - ^ Fu L, Isobe K, Zeng Q, Suzukawa K, Takekoshi K, Kawakami Y. The effects of beta(3)-adrenoceptor agonist CL-316,243 on adiponectin, adiponectin receptors and tumor necrosis factor-alpha expressions in adipose tissues of obese diabetic KKAy mice. European Journal of Pharmacology. 2008 Apr 14;584(1):202-6. PMID 18304529
- ^ Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Mol. Pharmacol. 49 (1): 7–14. PMID 8569714.
{{cite journal}}
: CS1 maint: multiple names: authors list (link)