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β1-adrenoceptor

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Target not currently curated in GtoImmuPdb

Target id: 28

Nomenclature: β1-adrenoceptor

Family: Adrenoceptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 477 10q25.3 ADRB1 adrenoceptor beta 1 14
Mouse 7 466 19 51.96 cM Adrb1 adrenergic receptor, beta 1 20
Rat 7 466 1q55 Adrb1 adrenoceptor beta 1 31
Previous and Unofficial Names Click here for help
ADRB1R | Adrenergic receptor beta 1 | B1AR | beta-1 adrenergic receptor | beta-1 adrenoreceptor | Adrb-1 | beta 1-AR | adrenergic receptor
Database Links Click here for help
Specialist databases
GPCRdb adrb1_human (Hs), adrb1_mouse (Mm), adrb1_rat (Rn)
Other databases
Alphafold P08588 (Hs), P34971 (Mm), P18090 (Rn)
ChEMBL Target CHEMBL213 (Hs), CHEMBL3440 (Mm), CHEMBL3252 (Rn)
DrugBank Target P08588 (Hs)
Ensembl Gene ENSG00000043591 (Hs), ENSMUSG00000035283 (Mm), ENSRNOG00000017002 (Rn)
Entrez Gene 153 (Hs), 11554 (Mm), 24925 (Rn)
Human Protein Atlas ENSG00000043591 (Hs)
KEGG Gene hsa:153 (Hs), mmu:11554 (Mm), rno:24925 (Rn)
OMIM 109630 (Hs)
Pharos P08588 (Hs)
RefSeq Nucleotide NM_000684 (Hs), NM_007419 (Mm), NM_012701 (Rn)
RefSeq Protein NP_000675 (Hs), NP_031445 (Mm), NP_036833 (Rn)
UniProtKB P08588 (Hs), P34971 (Mm), P18090 (Rn)
Wikipedia ADRB1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the β1-Adrenergic G Protein-Coupled Receptor
PDB Id:  2VT4
Ligand:  cyanopindolol
Resolution:  2.7Å
Species:  Turkey
References:  56
Image of receptor 3D structure from RCSB PDB
Description:  Turkey β1-adrenergic receptor with stabilising mutations and partial bound agonist Dobutamine
PDB Id:  2Y01
Ligand:  dobutamine
Resolution:  2.6Å
Species:  Turkey
References:  55
Image of receptor 3D structure from RCSB PDB
Description:  Turkey β1-adrenergic receptor with stabilising mutations and bound agonist Isoprenaline
PDB Id:  2Y03
Ligand:  isoprenaline
Resolution:  2.85Å
Species:  Turkey
References:  55
Image of receptor 3D structure from RCSB PDB
Description:  Turkey β1-adrenergic receptor with stabilising mutations and partial bound agonist Salbutamol
PDB Id:  2Y04
Ligand:  salbutamol
Resolution:  3.05Å
Species:  Turkey
References:  55
Image of receptor 3D structure from RCSB PDB
Description:  Turkey β1-adrenergic receptor with stabilising mutations and bound agonist Carazolol
PDB Id:  2YCW
Ligand:  carazolol
Resolution:  3.0Å
Species:  Turkey
References:  38
Image of receptor 3D structure from RCSB PDB
Description:  Turkey β1-Adrenergic receptor with stabilising mutations and bound antagonist Cyanopindolol
PDB Id:  2YCX
Ligand:  cyanopindolol
Resolution:  3.25Å
Species:  Turkey
References:  38
Image of receptor 3D structure from RCSB PDB
Description:  Turkey β1-adrenergic receptor with stabilising mutations and partial bound agonist Dobutamine
PDB Id:  2Y00
Ligand:  dobutamine
Resolution:  2.5Å
Species:  Turkey
References:  55
Image of receptor 3D structure from RCSB PDB
Description:  Turkey β1-adrenergic receptor with stabilising mutations and bound antagonist Cyanopindolol
PDB Id:  2YCY
Ligand:  cyanopindolol
Resolution:  3.15Å
Species:  Turkey
References:  38
Image of receptor 3D structure from RCSB PDB
Description:  NMR and circular dichroism studies of synthetic peptides derived from the third intracellular loop of the beta-adrenoceptor
PDB Id:  1DEP
Resolution:  0.0Å
Species:  Turkey
References:  24
Image of receptor 3D structure from RCSB PDB
Description:  Turkey β1-adrenergic receptor with stabilising mutations and bound agonist Carmoterol
PDB Id:  2Y02
Ligand:  carmoterol
Resolution:  2.6Å
Species:  Turkey
References:  55
Image of receptor 3D structure from RCSB PDB
Description:  Turkey β1-adrenergic receptor with stabilising mutations and bound antagonist Iodocyanopindolol
PDB Id:  2YCZ
Ligand:  iodocyanopindolol
Resolution:  3.65Å
Species:  Turkey
References:  38
Associated Proteins Click here for help
Interacting Proteins
Name Effect References
β1-adrenoceptor 34
β2-adrenoceptor 26-27,34,60
α2A-adrenoceptor 58
Natural/Endogenous Ligands Click here for help
(-)-adrenaline
noradrenaline
(-)-noradrenaline
Comments: Noradrenaline exhibits greater potency than adrenaline
Potency order of endogenous ligands (Human)
(-)-noradrenaline > (-)-adrenaline

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H](-)CGP 12177 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Partial agonist 6.6 – 9.9 pKd 21
⤷ pKd 6.6 – 9.9 [21]
CGP 12177 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 9.4 pKi 30
⤷ pKi 9.4 [30]
pindolol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 9.3 pKi 25
⤷ pKi 9.3 (Ki 5.2x10-10 M) [25]
(-)-Ro 363 Small molecule or natural product Hs Agonist 8.0 pKi 37
⤷ pKi 8.0 [37]
xamoterol Small molecule or natural product Hs Partial agonist 7.0 pKi 19
⤷ pKi 7.0 (Ki 1x10-7 M) [19]
isoprenaline Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 6.6 – 7.0 pKi 15,48
⤷ pKi 6.6 – 7.0 [15,48]
indacaterol Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Agonist 6.7 pKi 8
⤷ pKi 6.7 (Ki 1.8x10-7 M) [8]
T-0509 Small molecule or natural product Hs Full agonist 6.6 pKi 48
⤷ pKi 6.6 [48]
prenalterol Small molecule or natural product Hs Partial agonist 6.6 pKi 11,19
⤷ pKi 6.6 [11,19]
arformoterol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Agonist 6.5 pKi 9
⤷ pKi 6.5 (Ki 3.19x10-7 M) [9]
noradrenaline Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 6.0 pKi 15
⤷ pKi 6.0 [15]
(±)-adrenaline Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.0 pKi 15
⤷ pKi 6.0 [15]
denopamine Small molecule or natural product Hs Partial agonist 5.8 pKi 19,52
⤷ pKi 5.8 (Ki 1.584x10-6 M) [19,52]
(-)-noradrenaline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 5.5 – 6.0 pKi 15,18
⤷ pKi 5.5 – 6.0 [15,18]
(-)-adrenaline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Immunopharmacology Ligand Hs Agonist 5.4 – 6.0 pKi 15,18
⤷ pKi 5.4 – 6.0 [15,18]
dobutamine Small molecule or natural product Approved drug Primary target of this compound Hs Partial agonist 5.5 pKi 19
⤷ pKi 5.5 [19]
BI-167107 Small molecule or natural product Click here for species-specific activity table Hs Agonist 9.2 pEC50 17
⤷ pEC50 9.2 (EC50 6x10-10 M) [17]
Description: Determined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ1-AR
solabegron Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.4 pEC50 54
⤷ pEC50 5.4 [54]
mirabegron Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Agonist <5.0 pEC50 53
⤷ pEC50 <5.0 (EC50 >1x10-5 M) [53]
abediterol Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Agonist 7.4 pIC50 2
⤷ pIC50 7.4 (IC50 3.62x10-8 M) [2]
Description: Membrane radioligand displacement assay using [3H]CGP12177 as tracer.
fenoterol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist - - 5
⤷ [5]
cimaterol Small molecule or natural product Click here for species-specific activity table Hs Agonist - - 5
⤷ [5]
Agonist Comments
CGP 12177 is listed as a selective partial agonist at the β1 -adrenoceptor. It has now been established that the agonist action of this ligand is a result of action at a non-catecholamine activated site on the β1-adrenoceptor. This site is resistant to propranolol but is eliminated in β1-adrenoceptor knockout mice, confirming the site of action as the β1-adrenoceptor. This site was previously referred to as the β4-adrenoceptor. See reference [21] for additional information.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]ICYP Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 10.4 – 11.3 pKd 19,30,48
⤷ pKd 10.4 – 11.3 (Kd 3.9x10-11 – 4.99x10-12 M) It is necessary to use an excess of a β2-AR-selective ligand such as ICI 118551 in combination with this radioligand in order to allow visualisation of β1-AR binding in native tissue. [19,30,48]
[125I](-)ICYP Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 10.0 – 11.3 pKd 22,30,48
⤷ pKd 10.0 – 11.3 [22,30,48]
[3H](-)CGP 12177 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 6.6 – 9.2 pKd 4,21
⤷ pKd 6.6 – 9.2 3H-CGP12177 (high affinity non-selective antagonist of orthosteric site) is excellent for membrane and whole cell binding with little non-specific binding. [4,21]
nebivolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 9.2 pKi 5,13
⤷ pKi 9.2 [5,13]
Description: Radioligand binding
carvedilol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.8 – 9.5 pKi 4,12
⤷ pKi 8.8 – 9.5 [4,12]
CGP 12177 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 – 9.3 pKi 4,21
⤷ pKi 8.8 – 9.3 [4,21]
betaxolol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.8 pKi 30
⤷ pKi 8.8 [30]
ICI-89406 Small molecule or natural product Hs Partial agonist 8.8 pKi 36
⤷ pKi 8.8 [36]
levobetaxolol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.2 – 9.1 pKi 49
⤷ pKi 8.2 – 9.1 [49]
NDD-825 Small molecule or natural product Hs Antagonist 8.3 – 9.0 pKi 6
⤷ pKi 8.3 – 9.0 [6]
CGP 20712A Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.9 – 9.2 pKi 4,12,30,47,50
⤷ pKi 7.9 – 9.2 [4,12,30,47,50]
LK 204-545 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 30
⤷ pKi 8.5 [30]
(-)-propranolol Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.9 – 8.9 pKi 4,21,30,50
⤷ pKi 7.9 – 8.9 [4,21,30,50]
NIP Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 pKi 30
⤷ pKi 8.4 [30]
levobunolol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.4 pKi 3
⤷ pKi 8.4 (Ki 3.99x10-9 M) [3]
bupranolol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.3 – 9.0 pKi 4,12,30
⤷ pKi 7.3 – 9.0 [4,12,30]
NDD-713 Small molecule or natural product Hs Antagonist 7.8 – 8.5 pKi 6
⤷ pKi 7.8 – 8.5 [6]
SR59230A Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 – 8.6 pKi 4,12
⤷ pKi 7.5 – 8.6 [4,12]
cicloprolol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 pKi 30
⤷ pKi 8.0 [30]
bisoprolol Small molecule or natural product Approved drug Hs Antagonist 8.0 pKi 6
⤷ pKi 8.0 (Ki 1x10-8 M) [6]
labetalol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 7.6 – 8.2 pKi 3-4,7
⤷ pKi 7.6 – 8.2 [3-4,7]
metoprolol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.0 – 7.9 pKi 4,7,12,18,30
⤷ pKi 7.0 – 7.9 [4,7,12,18,30]
atenolol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.7 – 7.6 pKi 4,21,30
⤷ pKi 6.7 – 7.6 [4,21,30]
NIHP Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.1 pKi 30
⤷ pKi 7.1 [30]
H87/07 Small molecule or natural product Hs Antagonist 7.0 pKi 30
⤷ pKi 7.0 [30]
nadolol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.9 pKi 12
⤷ pKi 6.9 [12]
esmolol Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 6.7 – 6.9 pKi 3,39
⤷ pKi 6.7 – 6.9 [3,39]
propafenone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.7 pKi 3
⤷ pKi 6.7 (Ki 2.05x10-7 M) [3]
practolol Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 6.1 – 6.8 pKi 4,30
⤷ pKi 6.1 – 6.8 [4,30]
acebutolol Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 6.4 pKi 3
⤷ pKi 6.4 (Ki 4.22x10-7 M) [3]
sotalol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.1 pKi 3
⤷ pKi 6.1 (Ki 8.33x10-7 M) [3]
nebivolol Small molecule or natural product Approved drug Oc Antagonist 8.1 – 8.7 pIC50 41
⤷ pIC50 8.1 – 8.7 [41]
View species-specific antagonist tables
Antagonist Comments
CGP 12177 acts as an antagonist at the catecholamine site of the β1-adrenoceptor, in addition to acting as a partial agonist at the second site on the β1-adrenoceptor. For more information see references [21].
Propafenone may also act to block α-subunits of sodium ion channels (see the Voltage-gated sodium channels family in the Ion Channels section of this website for further details).
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family Adenylyl cyclase stimulation
Comments:  Stimulation of adenylate cyclase (AC) causes the conversion of ATP into cAMP. This activates protein kinase A, which in turn phosphorylates several substrates, for example L-type Ca2+ channels.
References:  51,57
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Guanylate cyclase stimulation
Comments:  Stimulation of guanylate cyclase (GC) causes an increase in cGMP levels, and subsequent activation of protein kinase G.
References:  29
Tissue Distribution Click here for help
Lung > brain > spleen > heart, kidney > liver > muscle.
Species:  Mouse
Technique:  Radioligand binding.
References:  1
Brain: Pineal gland, thalamus, amygdala, septum, hippocampus, anterior basal ganglia.
Species:  Rat
Technique:  Northern blotting.
References:  31
Heart.
Species:  Rat
Technique:  Northern blotting.
References:  31
Heart > lung.
Species:  Rat
Technique:  Radioligand binding.
References:  35
Brain: Caudate, cortex, cerebellum, hippocampus, diencephalon.
Species:  Rat
Technique:  Radioligand binding.
References:  35
Myocardium.
Species:  Rat
Technique:  Radioligand binding.
References:  16
Internal anal sphincter (IAS) smooth muscle.
Species:  Rat
Technique:  Western blotting.
References:  29
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of cAMP levels in rat heart and lung tissue.
Species:  Rat
Tissue:  Heart and lung.
Response measured:  cAMP accumulation.
References:  35
Measurement of cAMP levels in CHO-K1 cells transfected with the human β1 receptor.
Species:  Human
Tissue:  CHO-K1 cells
Response measured:  cAMP accumulation.
References:  23,48
Force generation of isolated atrial trabeculae electrically stimulated at 1Hz.
Species:  Human
Tissue:  Atrial trabeculae.
Response measured:  Contraction.
References:  23
Measurement of cAMP and Ca2+ levels in CHW fibroblast cells endogenously expressing Gs, AC and PKA and transfected with both the β1-adrenoceptor and the L-type Ca2+ channel.
Species:  Human
Tissue:  CHW-1102 fibroblasts.
Response measured:  PTX-insensitive cAMP and Ca2+ accumulation.
References:  59
Physiological Functions Click here for help
All the β-adrenoceptors mediate relaxation of the internal anal sphincter (IAS) smooth muscle, the β1 subtype achieving this via the Gi/o/cGMP pathway.
Species:  Rat
Tissue:  Internal anal sphincter (IAS).
References:  29
Relaxation of colon and oesophagus.
Species:  Mouse
Tissue:  Colon, oesophagus.
References:  40
Apoptosis.
Species:  Rat
Tissue:  Ventricular cardiomyocytes.
References:  42
Tachycardia.
Species:  Mouse
Tissue:  Atrium.
References:  45
Increase in contractile force, positive inotropy.
Species:  Mouse
Tissue:  Right cardiac ventricle.
References:  45
Renin release.
Species:  Human
Tissue:  Kidney.
References:  10
Physiological Consequences of Altering Gene Expression Click here for help
Most homozygous β1 knockout mice die prenatally, but those that reach adulthood show reduced chronotropic and inotropic responses to β-adrenoceptor agonists and reduced stimulation of adenylyl cyclase in cardiac membrane.
These demonstrate the functional differences between the receptor subtypes, and the importance of the β1-adrenoceptor in mouse development and cardiac function.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  45
β1-adrenoceptor knockout mice exhibit a normal heart rate and blood pressure except during exercise where they have a significantly reduced heart rate but no reduction in maximum exercise capacity or matabolic index.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  46
β1- and β2-adrenoceptor double knockout mice appear to have unaltered basal heart rate, blood pressure and meatabolic rate. Stimulation of these receptors by agonists or exercise reveals they exhibit a normal exercise capacity but at a submaximal heart rate.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  44
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Adrb1tm1Bkk|Adrb2tm1Bkk|Adrb3tm1Lowl Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk,Adrb3tm1Lowl/Adrb3tm1Lowl
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MGI:87939  MP:0001777 abnormal body temperature regulation PMID: 12161655 
Adrb1tm1Bkk|Adrb2tm1Bkk|Adrb3tm1Lowl Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk,Adrb3tm1Lowl/Adrb3tm1Lowl
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MGI:87939  MP:0002971 abnormal brown adipose tissue morphology PMID: 12161655 
Adrb1tm1Bkk Adrb1tm1Bkk/Adrb1tm1Bkk
either: (involves: 129/Sv) or (involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2)		 MGI:87937  MP:0001544 abnormal cardiovascular system physiology PMID: 8693001 
Adrb1tm1Bkk|Adrb2tm1Bkk Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MP:0001544 abnormal cardiovascular system physiology PMID: 10358009 
Adrb1tm1Bkk Adrb1tm1Bkk/Adrb1tm1Bkk
either: (involves: 129/Sv) or (involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2)		 MGI:87937  MP:0008872 abnormal physiological response to xenobiotic PMID: 8693001 
Adrb1tm1Bkk|Adrb2tm1Bkk Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MP:0008872 abnormal physiological response to xenobiotic PMID: 10358009 
Adrb1tm1Bkk|Adrb2tm1Bkk Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MP:0003638 abnormal response/metabolism to endogenous compounds PMID: 10358009 
Adrb1tm1Bkk|Adrb2tm1Bkk Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MP:0005140 decreased cardiac muscle contractility PMID: 10358009 
Adrb1tm1Bkk|Adrb2tm1Bkk Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MP:0005333 decreased heart rate PMID: 10358009 
Adrb1tm1Bkk|Adrb2tm1Bkk Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MP:0005290 decreased oxygen consumption PMID: 10358009 
Adrb1tm1Bkk|Adrb2tm1Bkk|Adrb3tm1Lowl Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk,Adrb3tm1Lowl/Adrb3tm1Lowl
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MGI:87939  MP:0005290 decreased oxygen consumption PMID: 12161655 
Adrb1tm1Bkk|Adrb2tm1Bkk|Adrb3tm1Lowl Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk,Adrb3tm1Lowl/Adrb3tm1Lowl
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MGI:87939  MP:0001260 increased body weight PMID: 12161655 
Adrb1tm1Bkk|Adrb2tm1Bkk|Adrb3tm1Lowl Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk,Adrb3tm1Lowl/Adrb3tm1Lowl
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MGI:87939  MP:0009119 increased brown fat cell size PMID: 12161655 
Adrb1tm1Bkk|Adrb2tm1Bkk|Adrb3tm1Lowl Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk,Adrb3tm1Lowl/Adrb3tm1Lowl
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MGI:87939  MP:0005669 increased circulating leptin level PMID: 12161655 
Adrb1tm1Bkk|Adrb2tm1Bkk|Adrb3tm1Lowl Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk,Adrb3tm1Lowl/Adrb3tm1Lowl
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MGI:87939  MP:0009294 increased interscapular fat pad weight PMID: 12161655 
Adrb1tm1Bkk|Adrb2tm1Bkk|Adrb3tm1Lowl Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk,Adrb3tm1Lowl/Adrb3tm1Lowl
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MGI:87939  MP:0010024 increased total body fat amount PMID: 12161655 
Adrb1tm1Bkk|Adrb2tm1Bkk|Adrb3tm1Lowl Adrb1tm1Bkk/Adrb1tm1Bkk,Adrb2tm1Bkk/Adrb2tm1Bkk,Adrb3tm1Lowl/Adrb3tm1Lowl
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2 * FVB/N		 MGI:87937  MGI:87938  MGI:87939  MP:0001261 obese PMID: 12161655 
Adrb1tm1Bkk Adrb1tm1Bkk/Adrb1tm1Bkk
either: (involves: 129/Sv) or (involves: 129S1/Sv * 129X1/SvJ * C57BL/6J * DBA/2)		 MGI:87937  MP:0002080 prenatal lethality PMID: 8693001 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Variation in resting heart rate
OMIM: 607276
Role:  Cardiovascular morbidity and moratilty risk increased progressively with increasing heart rate
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Missense Human S49G Highest mean resting heart rates were seen in individuals with the Ser49Gly polymorphism in ADRB1 43
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Description:  A common Gly389 -> Arg polymorphism has been identified in humans.
Although originally thought that Gly389 was the wild-type, both Gly389 and Arg389 are considered to be common.
This polymorphism is located in the intracellular cytoplasmic tail, resulting in differing Gs binding properties.
The Arg398 polymorphism enhances Gs binding and consequently an increase in adenylyl cyclase activity.
Due to their prevalence, the polymorphisms are not thought to be the primary cause of disease, although may be a small risk factor in common, multi-factorial diseases such as hypertension. They also may result in differing responses to β-blocker therapy.
Amino acid change:  G389R
References:  33
Type:  Single nucleotide polymorphism
Species:  Human
Description:  A Ser49 -> Gly polymorphism has been identified.
It is associated with a higher resting heart rate in individuals of chinese/japanese descent. Ser homozygotes have a more rapid heart rate than Ser/Gly heterozygotes, who have a more rapid heart rate than Gly homozygotes.
Amino acid change:  S49G
References:  32,43
General Comments
For a review on the β-adrenoceptor polymorphisms see reference [28].

References

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