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Beta-3 adrenergic receptor
A beta-3 adrenergic receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P13945]
Synonyms
Beta-3 adrenoreceptor;
Beta-3 adrenoceptor
Research
Bioassay Publications (62)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 7 (11.29) | 18.7374 |
| 1990's | 11 (17.74) | 18.2507 |
| 2000's | 26 (41.94) | 29.6817 |
| 2010's | 17 (27.42) | 24.3611 |
| 2020's | 1 (1.61) | 2.80 |
Compounds (79)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Synthesis and biological evaluation of βEuropean journal of medicinal chemistry, , May-25, Volume: 152, 2018
[no title available]Journal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Discovery of Novel Indazole Derivatives as Highly Potent and Selective Human β3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and evaluation of physical properties as potential overactive bladder therapies: part 5.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and molecular modeling based on the solved X-ray structure of the beta2-adrenergic receptor: part 6.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists.Bioorganic & medicinal chemistry, , May-01, Volume: 17, Issue:9, 2009
Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 17, Issue:15, 2009
Discovery of novel series of benzoic acid derivatives containing biphenyl ether moiety as potent and selective human beta(3)-adrenergic receptor agonists: Part IV.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Discovery of a novel series of benzoic acid derivatives as potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Discovery of a novel series of biphenyl benzoic acid derivatives as highly potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. Part II.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Stereospecific synthesis and bio-activity of novel beta(3)-adrenoceptor agonists and inverse agonists.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human beta3-adrenergic receptor agonists with good oral bioavailability. Part I.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.Journal of medicinal chemistry, , May-04, Volume: 49, Issue:9, 2006
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Relationship between stereochemistry and the beta3-adrenoceptor agonistic activity of 4'-hydroxynorephedrine derivative as an agent for treatment of frequent urination and urinary incontinence.Journal of medicinal chemistry, , Jan-02, Volume: 46, Issue:1, 2003
Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.Journal of medicinal chemistry, , Jan-31, Volume: 45, Issue:3, 2002
2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: novel selective beta3-adrenoceptor agonists.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.Journal of medicinal chemistry, , Volume: 27, Issue:8, 1984
Conformational effects on the activity of drugs. 10. Synthesis, conformation, and pharmacological properties of 1-(2,5-dimethoxyphenyl)-2-aminoethanols and their morpholine analogues.Journal of medicinal chemistry, , Volume: 26, Issue:2, 1983
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[omega-[4-[(alkylsulfonyl)amino]phenyl]-omega- hydroxyalkyl]-1H-imidazolium salts and related compounds.Journal of medicinal chemistry, , Volume: 30, Issue:4, 1987
[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.Journal of medicinal chemistry, , Volume: 27, Issue:8, 1984
Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds.Journal of medicinal chemistry, , Volume: 27, Issue:9, 1984
[no title available],
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 19, Issue:9, 2010
2,4-Thiazolidinediones as potent and selective human beta3 agonists.Bioorganic & medicinal chemistry letters, , Mar-26, Volume: 11, Issue:6, 2001
Beta 3 agonists. Part 1: evolution from inception to BMS-194449.Bioorganic & medicinal chemistry letters, , Dec-03, Volume: 11, Issue:23, 2001
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.Journal of medicinal chemistry, , Apr-26, Volume: 44, Issue:9, 2001
Pharmacological treatment of obesity: therapeutic strategies.Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 8, Issue:16, 1998
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.Bioorganic & medicinal chemistry letters, , May-05, Volume: 8, Issue:9, 1998
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 8, Issue:21, 1998
Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 19, Issue:9, 2010
Stereospecific synthesis and bio-activity of novel beta(3)-adrenoceptor agonists and inverse agonists.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Relationship between stereochemistry and the beta3-adrenoceptor agonistic activity of 4'-hydroxynorephedrine derivative as an agent for treatment of frequent urination and urinary incontinence.Journal of medicinal chemistry, , Jan-02, Volume: 46, Issue:1, 2003
Beta 3 agonists. Part 1: evolution from inception to BMS-194449.Bioorganic & medicinal chemistry letters, , Dec-03, Volume: 11, Issue:23, 2001
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 8, Issue:21, 1998
Development of 3D-QSAR models in cyclic ureidobenzenesulfonamides: human beta3-adrenergic receptor agonist.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 13, Issue:15, 2003
Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.Bioorganic & medicinal chemistry letters, , Sep-18, Volume: 10, Issue:18, 2000
Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 9, Issue:5, 1999
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 9, Issue:5, 1999
L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| beta-adrenergic receptor activity | molecular function | Combining with epinephrine or norepinephrine to initiate a change in cell activity via activation of a G protein, with pharmacological characteristics of beta-adrenergic receptors; the activity involves transmitting the signal to the Gs alpha subunit of a heterotrimeric G protein. [GOC:cb, GOC:mah, IUPHAR_GPCR:1274] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| beta3-adrenergic receptor activity | molecular function | Combining with epinephrine or norepinephrine to initiate a change in cell activity via activation of a G protein, with pharmacological characteristics of beta3-adrenergic receptors. [GOC:mah, IUPHAR_GPCR:1274] |
| beta-3 adrenergic receptor binding | molecular function | Binding to a beta-3 adrenergic receptor. [GOC:mah, GOC:nln] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| epinephrine binding | molecular function | Binding to epinephrine, a hormone produced by the medulla of the adrenal glands that increases heart activity, improves the power and prolongs the action of muscles, and increases the rate and depth of breathing. It is synthesized by the methylation of norepinephrine. [GOC:ai] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 15 target(s):
| Target | Category | Definition |
|---|
| diet induced thermogenesis | biological process | The process that results in increased metabolic rate in tissues of an organism. It is triggered by the detection of dietary excess. This process is achieved via signaling in the sympathetic nervous system. [PMID:12161655] |
| carbohydrate metabolic process | biological process | The chemical reactions and pathways involving carbohydrates, any of a group of organic compounds based of the general formula Cx(H2O)y. [GOC:mah, ISBN:0198506732] |
| generation of precursor metabolites and energy | biological process | The chemical reactions and pathways resulting in the formation of precursor metabolites, substances from which energy is derived, and any process involved in the liberation of energy from these substances. [GOC:jl] |
| energy reserve metabolic process | biological process | The chemical reactions and pathways by which a cell derives energy from stored compounds such as fats or glycogen. [GOC:mah] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194] |
| response to cold | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cold stimulus, a temperature stimulus below the optimal temperature for that organism. [GOC:lr] |
| heat generation | biological process | Any homeostatic process in which an organism produces heat, thereby raising its internal temperature. [GOC:mah] |
| negative regulation of multicellular organism growth | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of growth of an organism to reach its usual body size. [GOC:dph, GOC:ems, GOC:tb] |
| eating behavior | biological process | The specific behavior of an organism relating to the intake of food, any substance (usually solid) that can be metabolized by an organism to give energy and build tissue. [GOC:jl, GOC:pr, PMID:19361967] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| brown fat cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a brown adipocyte, an animal connective tissue cell involved in adaptive thermogenesis. Brown adipocytes contain multiple small droplets of triglycerides and a high number of mitochondria. [PMID:12588810] |
| adenylate cyclase-activating adrenergic receptor signaling pathway | biological process | An adenylate cyclase-activating G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process. [GOC:BHF, GOC:mah, GOC:signaling] |
| positive regulation of cold-induced thermogenesis | biological process | Any process that activates or increases the frequency, rate or extent of cold-induced thermogenesis. [PMID:27876809] |
| norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure | biological process | A process that results in an increase in the diameter of an artery during the norepinephrine-epinephrine response to blood pressure change. [GOC:mtg_cardio, PMID:10358008] |