Beta-3 adrenergic receptor
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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.
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
- L-796568[3]
- CL 316,243
- LY 368842
- Ro 40-2148
Antagonists
See also
- Other adrenergic receptors
References
- ↑ 1.0 1.1 Entrez Gene: ADRB1 adrenergic, beta-1-, receptor.
- ↑ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 163
- ↑ 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.
- ↑ 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.
Further reading
- Granneman JG, Lahners KN, Rao DD (1993). "Rodent and human beta 3-adrenergic receptor genes contain an intron within the protein-coding block.". Mol. Pharmacol. 42 (6): 964-70. PMID 1336117.
- Nahmias C, Blin N, Elalouf JM, et al. (1991). "Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes.". EMBO J. 10 (12): 3721-7. PMID 1718744.
- Emorine LJ, Marullo S, Briend-Sutren MM, et al. (1989). "Molecular characterization of the human beta 3-adrenergic receptor.". Science 245 (4922): 1118-21. PMID 2570461.
- Guan XM, Amend A, Strader CD (1995). "Determination of structural domains for G protein coupling and ligand binding in beta 3-adrenergic receptor.". Mol. Pharmacol. 48 (3): 492-8. PMID 7565630.
- Rodriguez M, Carillon C, Coquerel A, et al. (1995). "Evidence for the presence of beta 3-adrenergic receptor mRNA in the human brain.". Brain Res. Mol. Brain Res. 29 (2): 369-75. PMID 7609625.
- Clément K, Vaisse C, Manning BS, et al. (1995). "Genetic variation in the beta 3-adrenergic receptor and an increased capacity to gain weight in patients with morbid obesity.". N. Engl. J. Med. 333 (6): 352-4. PMID 7609752.
- Dib A, Adélaïde J, Chaffanet M, et al. (1995). "Characterization of the region of the short arm of chromosome 8 amplified in breast carcinoma.". Oncogene 10 (5): 995-1001. PMID 7898940.
- Mahmoudian M (1994). "The complex of human Gs protein with the beta 3 adrenergic receptor: a computer-aided molecular modeling study.". Journal of molecular graphics 12 (1): 22-8, 34. PMID 8011597.
- Wilkie TM, Chen Y, Gilbert DJ, et al. (1994). "Identification, chromosomal location, and genome organization of mammalian G-protein-coupled receptors.". Genomics 18 (2): 175-84. doi:10.1006/geno.1993.1452. PMID 8288218.
- Krief S, Lönnqvist F, Raimbault S, et al. (1993). "Tissue distribution of beta 3-adrenergic receptor mRNA in man.". J. Clin. Invest. 91 (1): 344-9. PMID 8380813.
- van Spronsen A, Nahmias C, Krief S, et al. (1993). "The promoter and intron/exon structure of the human and mouse beta 3-adrenergic-receptor genes.". Eur. J. Biochem. 213 (3): 1117-24. PMID 8389293.
- Lelias JM, Kaghad M, Rodriguez M, et al. (1993). "Molecular cloning of a human beta 3-adrenergic receptor cDNA.". FEBS Lett. 324 (2): 127-30. PMID 8389717.
- Candelore MR, Deng L, Tota LM, et al. (1996). "Pharmacological characterization of a recently described human beta 3-adrenergic receptor mutant.". Endocrinology 137 (6): 2638-41. PMID 8641219.
- Fujisawa T, Ikegami H, Yamato E, et al. (1996). "Association of Trp64Arg mutation of the beta3-adrenergic-receptor with NIDDM and body weight gain.". Diabetologia 39 (3): 349-52. PMID 8721782.
- Higashi K, Ishikawa T, Ito T, et al. (1997). "Association of a genetic variation in the beta 3-adrenergic receptor gene with coronary heart disease among Japanese.". Biochem. Biophys. Res. Commun. 232 (3): 728-30. doi:10.1006/bbrc.1997.6339. PMID 9126344.
- Hoffstedt J, Poirier O, Thörne A, et al. (1999). "Polymorphism of the human beta3-adrenoceptor gene forms a well-conserved haplotype that is associated with moderate obesity and altered receptor function.". Diabetes 48 (1): 203-5. PMID 9892244.
- Halushka MK, Fan JB, Bentley K, et al. (1999). "Patterns of single-nucleotide polymorphisms in candidate genes for blood-pressure homeostasis.". Nat. Genet. 22 (3): 239-47. doi:10.1038/10297. PMID 10391210.
- Kimura K, Sasaki N, Asano A, et al. (2000). "Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 preadipocytes.". Horm. Metab. Res. 32 (3): 91-6. PMID 10786926.
- Cao W, Luttrell LM, Medvedev AV, et al. (2001). "Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation.". J. Biol. Chem. 275 (49): 38131-4. doi:10.1074/jbc.C000592200. PMID 11013230.
- Russell ST, Hirai K, Tisdale MJ (2002). "Role of beta3-adrenergic receptors in the action of a tumour lipid mobilizing factor.". Br. J. Cancer 86 (3): 424-8. doi:10.1038/sj.bjc.6600086. PMID 11875710.
Transmembrane receptor: G protein-coupled receptors | |
|---|---|
| Class A: Rhodopsin like | Acetylcholine (M1, M2, M3, M4, M5) - Adrenergic (α1 (A, B, D), α2 (A, B, C), β1, β2, β3) - Adrenomedullin - Anaphylatoxin (C3a, C5a) - Angiotensin (1, 2) - Apelin - Bile acid - Bombesin (BRS3, GRPR, NMBR) - Bradykinin (B1, B2) - Cannabinoid (CB1, CB2) - Chemokine - Cholecystokinin (A, B) - Dopamine (D1, D2, D3, D4, D5) - Eicosanoid (CysLT (1, 2), LTB4 (1, 2), FPRL1, OXE, Prostaglandin ((DP (1, 2), EP (1, 2, 3, 4), PGF, Prostacyclin, Thromboxane) - EBI2 - Endothelin (A, B) - Estrogen - Formyl peptide (1, L1, L2) - Free fatty acid (1, 2, 3, 4) - FSH - Galanin (1, 2, 3) - Gonadotropin-releasing hormone (1, 2) - GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 182) - Ghrelin - Histamine (H1, H2, H3, H4) - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) - MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) - Melanocortin (1, 2, 3, 4, 5) - MCHR (1, 2) - Melatonin (1A, 1B)- Motilin - Neuromedin (B, U (1, 2)) - Neuropeptide (B/W (1, 2), FF (1, 2), S, Y (1, 2, 4, 5)) - Neurotensin (1, 2) - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory - Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) - Orexin (1, 2) - Oxytocin - Oxoglutarate - PAF - Prokineticin (1, 2) - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Purinergics (Adenosine (A1, A2a, A2b, A3), P2Y, (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)) - Relaxin (1, 2, 3, 4) - Somatostatin (1, 2, 3, 4, 5) - Serotonin, all but 5-HT3 (5-HT1 (A, B, D, E, F), 5-HT2 (A, B, C), 5-HT (4, 5A, 6, 7)) - SREB - Succinate - TAAR (1, 2, 3, 5, 6, 8, 9) - Tachykinin (1, 2, 3) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2) |
| Class B: Secretin like | Brain-specific angiogenesis inhibitor (1, 2, 3) - Cadherin (1, 2, 3) - Calcitonin - CD97 - Corticotropin-releasing hormone (1, 2) - EMR (1, 2, 3) - Glucagon (GR, GIPR, GLP1R, GLP2R) - Growth hormone releasing hormone - PACAPR1- GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157) - Latrophilin (1, 2, 3, ELTD1) - Parathyroid hormone (1, 2) - Secretin - Vasoactive intestinal peptide (1, 2) |
| Class C: Metabotropic glutamate / pheromone | Calcium-sensing receptor - GABA B (1, 2) - Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) - GPRC6A - GPR (156, 158, 179) - RAIG (1, 2, 3, 4) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50)) |
| Frizzled / Smoothened | Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened |
| ||||
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .

