Page last updated: 2024-08-07 15:47:29
Beta-1 adrenergic receptor
A beta-1 adrenergic receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P08588]
Synonyms
Beta-1 adrenoreceptor;
Beta-1 adrenoceptor
Research
Bioassay Publications (98)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 8 (8.16) | 18.7374 |
| 1990's | 13 (13.27) | 18.2507 |
| 2000's | 33 (33.67) | 29.6817 |
| 2010's | 40 (40.82) | 24.3611 |
| 2020's | 4 (4.08) | 2.80 |
Compounds (104)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| 1-(2-methoxyphenyl)piperazine | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| 1-(3-chlorophenyl)piperazine | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| acebutolol | Homo sapiens (human) | IC50 | 0.7310 | 1 | 0 |
| acebutolol | Homo sapiens (human) | Ki | 0.4220 | 1 | 0 |
| alprenolol | Homo sapiens (human) | IC50 | 0.0070 | 3 | 3 |
| alprenolol | Homo sapiens (human) | Ki | 0.0028 | 1 | 1 |
| amiodarone | Homo sapiens (human) | IC50 | 43.6430 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 25.2020 | 1 | 0 |
| astemizole | Homo sapiens (human) | IC50 | 17.3820 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 10.0370 | 1 | 0 |
| atenolol | Homo sapiens (human) | IC50 | 0.7468 | 8 | 7 |
| atenolol | Homo sapiens (human) | Ki | 0.6043 | 5 | 4 |
| betaxolol | Homo sapiens (human) | IC50 | 0.0371 | 1 | 1 |
| carteolol | Homo sapiens (human) | Ki | 0.0019 | 1 | 1 |
| carvedilol | Homo sapiens (human) | IC50 | 0.0002 | 1 | 0 |
| carvedilol | Homo sapiens (human) | Ki | 0.0001 | 1 | 0 |
| cgp 20712a | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| cisapride | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| clenbuterol | Homo sapiens (human) | IC50 | 0.1200 | 1 | 0 |
| clenbuterol | Homo sapiens (human) | Ki | 0.0690 | 1 | 0 |
| clorprenaline | Homo sapiens (human) | IC50 | 2.5920 | 1 | 0 |
| clorprenaline | Homo sapiens (human) | Ki | 1.4970 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 11.2790 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 6.5130 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 12.8210 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 7.4040 | 1 | 0 |
| formoterol fumarate | Homo sapiens (human) | IC50 | 0.6310 | 2 | 2 |
| formoterol fumarate | Homo sapiens (human) | Ki | 0.8764 | 3 | 3 |
| isoproterenol | Homo sapiens (human) | IC50 | 0.3330 | 1 | 0 |
| isoproterenol | Homo sapiens (human) | Ki | 0.8889 | 2 | 1 |
| labetalol | Homo sapiens (human) | IC50 | 0.0100 | 1 | 0 |
| labetalol | Homo sapiens (human) | Ki | 0.0058 | 1 | 0 |
| metoprolol | Homo sapiens (human) | IC50 | 0.1760 | 1 | 0 |
| metoprolol | Homo sapiens (human) | Ki | 0.0785 | 2 | 1 |
| miconazole | Homo sapiens (human) | IC50 | 12.6350 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 7.2960 | 1 | 0 |
| pindolol | Homo sapiens (human) | IC50 | 0.0009 | 1 | 0 |
| pindolol | Homo sapiens (human) | Ki | 0.0005 | 2 | 1 |
| propafenone | Homo sapiens (human) | IC50 | 0.3540 | 1 | 0 |
| propafenone | Homo sapiens (human) | Ki | 0.2050 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 0.0575 | 5 | 4 |
| propranolol | Homo sapiens (human) | Ki | 0.0042 | 4 | 3 |
| quipazine | Homo sapiens (human) | Ki | 6.3096 | 1 | 1 |
| salmeterol xinafoate | Homo sapiens (human) | IC50 | 0.5012 | 2 | 2 |
| salmeterol xinafoate | Homo sapiens (human) | Ki | 1.5992 | 4 | 4 |
| sotalol | Homo sapiens (human) | IC50 | 7.1087 | 5 | 4 |
| sotalol | Homo sapiens (human) | Ki | 0.8335 | 1 | 0 |
| lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.1400 | 1 | 1 |
| phenylpiperazine | Homo sapiens (human) | IC50 | 19.0000 | 1 | 1 |
| phenylpiperazine | Homo sapiens (human) | Ki | 1.3490 | 1 | 1 |
| ergotamine | Homo sapiens (human) | IC50 | 4.1420 | 1 | 0 |
| ergotamine | Homo sapiens (human) | Ki | 2.3920 | 1 | 0 |
| indopan | Homo sapiens (human) | Ki | 3.7889 | 1 | 2 |
| dexpropranolol | Homo sapiens (human) | IC50 | 0.3700 | 1 | 0 |
| dexpropranolol | Homo sapiens (human) | Ki | 0.2140 | 1 | 0 |
| lisuride | Homo sapiens (human) | IC50 | 0.5590 | 1 | 0 |
| lisuride | Homo sapiens (human) | Ki | 0.3230 | 1 | 0 |
| bromocriptine | Homo sapiens (human) | IC50 | 2.4000 | 1 | 0 |
| bromocriptine | Homo sapiens (human) | Ki | 1.3860 | 1 | 0 |
| 1-(3-chloro-5-benzo[b][1]benzoxepinyl)-4-methylpiperazine | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
| timolol | Homo sapiens (human) | IC50 | 0.0026 | 1 | 0 |
| timolol | Homo sapiens (human) | Ki | 0.0034 | 2 | 1 |
| dobutamine | Homo sapiens (human) | IC50 | 1.9440 | 1 | 0 |
| dobutamine | Homo sapiens (human) | Ki | 1.1230 | 1 | 0 |
| levobunolol | Homo sapiens (human) | IC50 | 0.0069 | 1 | 0 |
| levobunolol | Homo sapiens (human) | Ki | 0.0040 | 1 | 0 |
| bopindolol | Homo sapiens (human) | IC50 | 0.0470 | 1 | 0 |
| bopindolol | Homo sapiens (human) | Ki | 0.0270 | 1 | 0 |
| sematilide | Homo sapiens (human) | IC50 | 7,000.0000 | 1 | 1 |
| esmolol | Homo sapiens (human) | IC50 | 0.1970 | 1 | 0 |
| esmolol | Homo sapiens (human) | Ki | 0.1137 | 1 | 0 |
| sotalol hydrochloride | Homo sapiens (human) | IC50 | 7.2000 | 1 | 1 |
| talinolol | Homo sapiens (human) | Ki | 0.2400 | 1 | 1 |
| 1-(4-nitrophenyl)piperazine | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| 1-(4-chlorophenyl)piperazine | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| sb 204070a | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| ersentilide | Homo sapiens (human) | IC50 | 2.4000 | 1 | 1 |
| sc 53116 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sc 53116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n-demethyllysergic acid diethylamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 8.5650 | 1 | 1 |
| sibenadet | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| sibenadet | Homo sapiens (human) | Ki | 3.9220 | 1 | 1 |
| 1-(4-methoxyphenyl)piperazine | Homo sapiens (human) | IC50 | 38.0000 | 1 | 1 |
| darifenacin | Homo sapiens (human) | IC50 | 0.3162 | 1 | 1 |
| darifenacin | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 22.0880 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 12.7550 | 1 | 0 |
| (S)-(-)-pindolol | Homo sapiens (human) | IC50 | 0.0008 | 1 | 0 |
| (S)-(-)-pindolol | Homo sapiens (human) | Ki | 0.0004 | 1 | 0 |
| 4,4-dicarboxy-5-pyridoxylproline | Homo sapiens (human) | Ki | 0.1072 | 1 | 1 |
| tamoxifen | Homo sapiens (human) | IC50 | 17.2890 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 9.9840 | 1 | 0 |
| sb-224289 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| cl 316243 | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| vx680 | Homo sapiens (human) | IC50 | 0.0550 | 1 | 1 |
| cgp 12177a | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| dihydrexidine | Homo sapiens (human) | Ki | 1.5000 | 1 | 1 |
| indacaterol | Homo sapiens (human) | IC50 | 0.3162 | 1 | 1 |
| indacaterol | Homo sapiens (human) | Ki | 0.0912 | 2 | 2 |
| l 755507 | Homo sapiens (human) | IC50 | 0.2000 | 1 | 1 |
| l 755507 | Homo sapiens (human) | Ki | 0.5700 | 1 | 1 |
| brl 37344 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| solabegron | Homo sapiens (human) | Ki | 0.3981 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 77-lh-28-1 | Homo sapiens (human) | Ki | 47.8630 | 1 | 1 |
| sb-649915 | Homo sapiens (human) | Ki | 2.5119 | 1 | 1 |
| l 764646 | Homo sapiens (human) | IC50 | 18.0000 | 2 | 2 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| acebutolol | Homo sapiens (human) | Kd | 13.3613 | 1 | 3 |
| albuterol | Homo sapiens (human) | EC50 | 0.5858 | 2 | 2 |
| albuterol | Homo sapiens (human) | Kd | 23.1370 | 1 | 3 |
| alprenolol | Homo sapiens (human) | Kd | 0.0544 | 4 | 6 |
| atenolol | Homo sapiens (human) | Kd | 26.2890 | 1 | 3 |
| betaxolol | Homo sapiens (human) | Kd | 0.0016 | 1 | 1 |
| bisoprolol | Homo sapiens (human) | Kd | 0.7843 | 1 | 3 |
| bupranolol | Homo sapiens (human) | Kd | 0.0314 | 1 | 3 |
| carvedilol | Homo sapiens (human) | Kd | 0.0024 | 1 | 3 |
| cgp 20712a | Homo sapiens (human) | Kd | 1.0426 | 5 | 7 |
| cgp 12177 | Homo sapiens (human) | EC50 | 0.0123 | 1 | 1 |
| cgp 12177 | Homo sapiens (human) | Kd | 0.0343 | 1 | 3 |
| cimaterol | Homo sapiens (human) | EC50 | 0.0074 | 1 | 1 |
| formoterol fumarate | Homo sapiens (human) | EC50 | 0.0461 | 6 | 6 |
| ici 118551 | Homo sapiens (human) | Kd | 0.2264 | 2 | 4 |
| isoproterenol | Homo sapiens (human) | EC50 | 0.1000 | 22 | 22 |
| labetalol | Homo sapiens (human) | Kd | 0.2313 | 1 | 3 |
| metoprolol | Homo sapiens (human) | Kd | 1.7790 | 2 | 4 |
| pindolol | Homo sapiens (human) | Kd | 3.3350 | 3 | 3 |
| practolol | Homo sapiens (human) | Kd | 18.8532 | 3 | 6 |
| pronethalol | Homo sapiens (human) | Kd | 0.5650 | 1 | 3 |
| propranolol | Homo sapiens (human) | Kd | 0.0314 | 7 | 11 |
| quipazine | Homo sapiens (human) | Kd | 5.6117 | 1 | 2 |
| salmeterol xinafoate | Homo sapiens (human) | EC50 | 0.8477 | 15 | 15 |
| salmeterol xinafoate | Homo sapiens (human) | Kd | 2.0108 | 1 | 3 |
| sotalol | Homo sapiens (human) | Kd | 3.5840 | 1 | 3 |
| terbutaline | Homo sapiens (human) | Kd | 101.3853 | 1 | 4 |
| isoproterenol hydrochloride | Homo sapiens (human) | EC50 | 0.0015 | 1 | 1 |
| phenylephrine | Homo sapiens (human) | EC50 | 6.0000 | 1 | 1 |
| sq-11725 | Homo sapiens (human) | Kd | 0.2408 | 1 | 3 |
| flestolol | Homo sapiens (human) | Kd | 0.0079 | 1 | 2 |
| (S)-betaxolol | Homo sapiens (human) | Kd | 0.3734 | 1 | 3 |
| propranolol hydrochloride | Homo sapiens (human) | Kd | 0.0013 | 1 | 1 |
| eltoprazine | Homo sapiens (human) | Kd | 15.9244 | 1 | 2 |
| labetalol hydrochloride | Homo sapiens (human) | Kd | 0.0079 | 1 | 1 |
| ici 89406 | Homo sapiens (human) | Kd | 0.7094 | 1 | 3 |
| xamoterol | Homo sapiens (human) | EC50 | 0.0110 | 1 | 1 |
| xamoterol | Homo sapiens (human) | Kd | 0.0495 | 2 | 2 |
| L-isoprenaline | Homo sapiens (human) | EC50 | 0.0359 | 5 | 5 |
| darifenacin | Homo sapiens (human) | EC50 | 0.0398 | 1 | 1 |
| arformoterol | Homo sapiens (human) | EC50 | 0.1090 | 1 | 1 |
| obelin | Homo sapiens (human) | Kd | 0.2239 | 1 | 1 |
| cl 316243 | Homo sapiens (human) | EC50 | 111.0000 | 1 | 1 |
| ici 118551 | Homo sapiens (human) | Kd | 0.1820 | 1 | 1 |
| phentolamine | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| ici 215001 | Homo sapiens (human) | Kd | 0.6803 | 1 | 3 |
| l 755507 | Homo sapiens (human) | EC50 | 0.3300 | 1 | 1 |
| brl 37344 | Homo sapiens (human) | EC50 | 1.7000 | 2 | 2 |
| solabegron | Homo sapiens (human) | EC50 | 3.9811 | 1 | 1 |
| trantinterol | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
| l 748,337 | Homo sapiens (human) | EC50 | 0.8890 | 1 | 1 |
| olodaterol | Homo sapiens (human) | EC50 | 0.1230 | 1 | 1 |
| bi167107 | Homo sapiens (human) | EC50 | 0.0006 | 1 | 1 |
Enables
This protein enables 7 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] |
| beta1-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 beta1-adrenergic receptors. [GOC:mah, IUPHAR_GPCR:1274] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| PDZ domain binding | molecular function | Binding to a PDZ domain of a protein, a domain found in diverse signaling proteins. [GOC:go_curators, Pfam:PF00595] |
| alpha-2A adrenergic receptor binding | molecular function | Binding to an alpha-2A adrenergic receptor. [GOC:mah, GOC:nln] |
| protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
| G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potential | molecular function | A G protein-coupled neurotransmitter receptor activity, occurring in the postsynaptic membrane, involved in regulation of postsynaptic membrane potential. [GOC:dos] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|---|---|
| early endosome | cellular component | A membrane-bounded organelle that receives incoming material from primary endocytic vesicles that have been generated by clathrin-dependent and clathrin-independent endocytosis; vesicles fuse with the early endosome to deliver cargo for sorting into recycling or degradation pathways. [GOC:mah, NIF_Subcellular:nlx_subcell_20090701, PMID:19696797] |
| 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] |
| Schaffer collateral - CA1 synapse | cellular component | A synapse between the Schaffer collateral axon of a CA3 pyramidal cell and a CA1 pyramidal cell. [PMID:16399689] |
| neuronal dense core vesicle | cellular component | A dense core vesicle (granule) that is part of a neuron. These vesicles typically contain neuropeptides. They can be found in all parts of neurons, including the soma, dendrites, axonal swellings (varicosities) and synaptic terminals. [GOC:dos, ISBN:978-0-07-181001-2, Wikipedia:Neuropeptide&oldid=713905176] |
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] |
Involved In
This protein is involved in 14 target(s):
| Target | Category | Definition |
|---|---|---|
| positive regulation of heart rate by epinephrine-norepinephrine | biological process | The process in which the presence of epinephrine or norepinephrine in the bloodstream activates, maintains or increases the rate of heart contraction. [GOC:dph] |
| positive regulation of the force of heart contraction by epinephrine-norepinephrine | biological process | Any process that increases the force with which the cardiac muscles of the heart pump blood through the circulatory system as a result of the presence of epinephrine or norepinephrine in the bloodstream or released from the nerve endings. [GOC:dph, GOC:mtg_cardio] |
| 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] |
| 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] |
| fear response | biological process | The response of an organism to a perceived external threat. [GOC:go_curators] |
| regulation of circadian sleep/wake cycle, sleep | biological process | Any process that modulates the frequency, rate or extent of sleep; a readily reversible state of reduced awareness and metabolic activity that occurs periodically in many animals. [GOC:jl, ISBN:0192800981] |
| 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] |
| regulation of postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |
| 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] |
| 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] |