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α1B-adrenoceptor

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Target not currently curated in GtoImmuPdb

Target id: 23

Nomenclature: α1B-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 7 520 5q33.3 ADRA1B adrenoceptor alpha 1B 70
Mouse 7 514 11 25.81 cM Adra1b adrenergic receptor, alpha 1b 50
Rat 7 515 10q21 Adra1b adrenoceptor alpha 1B 5
Previous and Unofficial Names Click here for help
adrenergic alpha 1B receptor | alpha 1B-adrenoceptor | alpha 1B-adrenoreceptor | alpha1B-adrenergic receptor | adrenergic receptor
Database Links Click here for help
Specialist databases
GPCRdb ada1b_human (Hs), ada1b_rat (Mm), ada1b_mouse (Rn)
Other databases
Alphafold P35368 (Hs), P97717 (Mm), P15823 (Rn)
ChEMBL Target CHEMBL232 (Hs), CHEMBL2486 (Mm), CHEMBL315 (Rn)
DrugBank Target P35368 (Hs), P35368 (Hs), P35368 (Hs)
Ensembl Gene ENSG00000170214 (Hs), ENSMUSG00000050541 (Mm), ENSRNOG00000060087 (Rn)
Entrez Gene 147 (Hs), 11548 (Mm), 24173 (Rn)
Human Protein Atlas ENSG00000170214 (Hs)
KEGG Gene hsa:147 (Hs), mmu:11548 (Mm), rno:24173 (Rn)
OMIM 104220 (Hs)
Pharos P35368 (Hs)
RefSeq Nucleotide NM_000679 (Hs), NM_007416 (Mm), NM_016991 (Rn)
RefSeq Protein NP_000670 (Hs), NP_031442 (Mm), NP_058687 (Rn)
UniProtKB P35368 (Hs), P97717 (Mm), P15823 (Rn)
Wikipedia ADRA1B (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the human α1B-adrenoceptor in complex with inverse agonist (+)-cyclazosin.
PDB Id:  7B6W
Ligand:  (+)-cyclazosin
Resolution:  2.87Å
Species:  Human
References:  24
Natural/Endogenous Ligands Click here for help
(-)-adrenaline
(-)-noradrenaline

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
oxymetazoline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.2 – 6.5 pKi 61,67,77
⤷ pKi 5.2 – 6.5 [61,67,77]
(-)-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 Full agonist 3.9 – 6.5 pKi 67,77
⤷ pKi 3.9 – 6.5 [67,77]
NS-49 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.1 pKi 61
⤷ pKi 5.1 [61]
cirazoline Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.1 pKi 67
⤷ pKi 5.1 [67]
(+)-adrenaline Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.1 pKi 77
⤷ pKi 5.1 [77]
(-)-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 Full agonist 3.8 – 6.2 pKi 67,77
⤷ pKi 3.8 – 6.2 [67,77]
A61603 Small molecule or natural product Click here for species-specific activity table Hs Full agonist <4.0 pKi 67
⤷ pKi <4.0 (Ki >1x10-4 M) [67]
phenylephrine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist 3.9 pKi 67
⤷ pKi 3.9 [67]
methoxamine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 3.0 – 4.0 pKi 67,77
⤷ pKi 3.0 – 4.0 [67,77]
phenylephrine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.1 – 9.0 pEC50 28,55,67
⤷ pEC50 6.1 – 9.0 [67]
pEC50 6.3 – 7.5 [28,55]
(-)-noradrenaline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.9 – 9.2 pEC50 67
⤷ pEC50 5.9 – 9.2 [67]
cirazoline Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.9 – 8.1 pEC50 67
⤷ pEC50 6.9 – 8.1 [67]
(-)-adrenaline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 5.4 – 9.4 pEC50 67
⤷ pEC50 5.4 – 9.4 [67]
oxymetazoline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.7 – 7.4 pEC50 67
⤷ pEC50 6.7 – 7.4 [67]
A61603 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 – 6.5 pEC50 67
⤷ pEC50 5.6 – 6.5 [67]
methoxamine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 4.0 – 6.6 pEC50 67
⤷ pEC50 4.0 – 6.6 [67]
Agonist Comments
Non catecholamine agonists, such as methoxamine and amidephrine, have both low affinity and low intrinsic activity at the α1B- adrenoceptor [55]. Much data has been generated using the hamster α1B-adrenoceptor, since this was the first α1B- homolog to be cloned. More recent data has been obtained utilising the human receptor. There is no evidence for any significant species differences in agonist and antagonist affinity between hamster, rat and human receptors. Methoxamine behaves as a full agonist for some and a partial agonist at other signalling pathways [67]. A61603 is highly selective for α1A-AR- no agonists currently available are selective for α1B-AR.

Note that pEC50 values have been determined in a variety of assay formats measuring intracellular Ca2+ release, ERK1/2 phosphorylation, extracellular acidification rate and cAMP accumulation. Clinical uses: α1B-AR are not specific clinical targets although adrenaline and noradrenaline used for shock will activate α1B-AR in blood vessels.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]HEAT (BE2254) Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Inverse agonist 9.9 – 10.2 pKd 54,75,77
⤷ pKd 9.9 – 10.2 [54,75,77]
[3H]prazosin Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Inverse agonist 9.1 pKd 68
⤷ pKd 9.1 [68]
HEAT (BE2254) Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 8.0 pKd 68
⤷ pKd 8.0 [68]
MT-1207 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 10.1 pKi 87
⤷ pKi 10.1 (Ki 8.6x10-11 M) [87]
compound 12 [PMID: 26238322] Small molecule or natural product Hs Antagonist 9.8 pKi 37
⤷ pKi 9.8 [37]
(+)-cyclazosin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.7 – 9.9 pKi 30,68
⤷ pKi 8.7 – 9.9 [30,68]
prazosin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.7 – 9.9 pKi 28,68,77,90
⤷ pKi 8.7 – 9.9 [28,68,77,90]
NAN 190 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.2 pKi 94
⤷ pKi 9.2 [94]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 9.2 pKi 94
⤷ pKi 9.2 [94]
tamsulosin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.1 – 9.7 pKi 28,68,77,90
⤷ pKi 8.1 – 9.7 [28,68,77,90]
doxazosin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.5 – 9.1 pKi 35,68
⤷ pKi 8.5 – 9.1 (Ki 8.13x10-10 M) [35,68]
Rec 15/2615 Small molecule or natural product Hs Antagonist 7.8 – 9.5 pKi 68,83
⤷ pKi 7.8 – 9.5 [68,83]
rho-TIA Peptide Hs Antagonist 8.4 pKi 19
⤷ pKi 8.4 [19]
A-119637 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 12
⤷ pKi 8.3 [12]
L-765314 Small molecule or natural product Rn Antagonist 8.3 pKi 64
⤷ pKi 8.3 [64]
terazosin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.0 – 8.6 pKi 52,68
⤷ pKi 8.0 – 8.6 [52,68]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.2 pKi 94
⤷ pKi 8.2 [94]
WB 4101 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.4 – 9.0 pKi 28,68,77
⤷ pKi 7.4 – 9.0 [28,68,77]
alfuzosin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.6 – 8.6 pKi 40,68
⤷ pKi 7.6 – 8.6 (Ki 2.8x10-9 M) [40,68]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.0 pKi 94
⤷ pKi 8.0 [94]
A-123189 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 pKi 12
⤷ pKi 8.0 [12]
muscarinic toxin β Peptide Hs Antagonist 8.0 pKi 10
⤷ pKi 8.0 [10]
mamba toxin CM-3 Peptide Hs Antagonist 8.0 pKi 10
⤷ pKi 8.0 [10]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.8 – 8.0 pKi 68,94
⤷ pKi 7.8 – 8.0 [68,94]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.4 – 8.2 pKi 68,94
⤷ pKi 7.4 – 8.2 [68,94]
upidosin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 pKi 28
⤷ pKi 7.8 [28]
L-765314 Small molecule or natural product Hs Antagonist 7.7 pKi 64
⤷ pKi 7.7 [64]
spiroxatrine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.6 pKi 94
⤷ pKi 7.6 [94]
cyproheptadine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.6 pKi 94
⤷ pKi 7.6 [94]
AH 11110 Small molecule or natural product Hs Antagonist 7.5 pKi 74
⤷ pKi 7.5 [74]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.4 pKi 94
⤷ pKi 7.4 [94]
indoramin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.8 – 7.4 pKi 28,68
⤷ pKi 6.8 – 7.4 [28,68]
silodosin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.5 – 7.7 pKi 68,77
⤷ pKi 6.5 – 7.7 [68,77]
Ro-70-0004 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.1 pKi 90
⤷ pKi 7.1 [90]
phentolamine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.6 – 7.5 pKi 68,77
⤷ pKi 6.6 – 7.5 [68,77]
S(+)-niguldipine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 – 7.7 pKi 28,68,77
⤷ pKi 6.3 – 7.7 [28,68,77]
KMUP-1 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.9 pKi 49
⤷ pKi 6.9 [49]
5-methylurapidil Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 – 7.7 pKi 28,68,77,94
⤷ pKi 6.1 – 7.7 [28,68,77,94]
BMY-7378 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 – 7.5 pKi 12,68,94
⤷ pKi 6.2 – 7.5 [12,68,94]
MT-1207 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.8 pIC50 87
⤷ pIC50 9.8 (IC50 1.5x10-10 M) [87]
View species-specific antagonist tables
Antagonist Comments
There are no highly selective α1B-AR antagonists available. (+) Cyclazosin has been shown to have minor α1B- selectivity in early [79] but not more recent [68] radioligand binding assays with recombinant receptors. No functional selectivity is reported in isolated tissue preparations [79]. The 19 amino acid peptide, rho-TIA, produces non-competitive blockade of α1B-AR mediated inositol phosphate formation at concentrations producing competitive blockade of this response in cells expressing α1A or α1D subtypes. There is reported variation in affinities for antagonists related to the assay system used [68,93].
Prazosin, alfuzosin, cyclazosin, doxazosin and terazosin are selective for α1-ARs vs. α2-ARs but show similar affinity for all 3 alpha;1-AR subtypes. Clinical uses: α1B-AR are not specific clinical targets however α1-AR antagonists used for hypertension and benign prostatic hypertrophy will block α1B-AR in blood vessels.
Allosteric Modulators
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Ligand Sp. Action Value Parameter Reference
lorazepam Small molecule or natural product Approved drug Rn Positive 3.8 pKi 88
⤷ pKi 3.8 (Ki 1.7x10-4 M) [88]
midazolam Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Positive 3.7 pKi 88
⤷ pKi 3.7 (Ki 1.83x10-4 M) [88]
rho-TIA Peptide Click here for species-specific activity table Rn Negative 9.1 pIC50 48
⤷ pIC50 9.1 (IC50 8x10-10 M) [48]
Allosteric Modulator Comments
The conopeptide ρ-TIA is a negative allosteric regulator at the hamster α1B-AR (pKi 7.6, [69]).
Additionally, σ-TIA competes for radioligand binding to recombinant α1B-AR in a non-competitive manner [19,33].
Data published by Williams et al. (2018) show that diazepam is not a direct allosteric modulator of α1-ARs [89], but modulates receptor activity by inhibition of phosphodiesterase 4.
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Calcium channel
Other - See Comments
Comments:  The α1B-adrenoceptor is coupled to calcium release and inositol phosphate production (i.e. Gq) less efficiently than the α1A but more efficiently than the α1D.
References:  33,45,54
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Phospholipase D stimulation
Other - See Comments
Comments:  PDK-1 is involved in phosphorylation and desensitization [3].
cAMP accumulation [51,67].
α1-ARs form hetero-oligomeric complexes with the ACKR3:CXCR4 heteromer, and the complex is required for α1B/D-AR function. Phenylephrine-induced inositol trisphosphate production from hVSMCs is abolished after ACKR3 and CXCR4 siRNA knockdown [2].
α1-ARs (all subtypes) also activate protein Kinase C and mitogen activated protein kinases. Like the α1A-AR, α1B-AR can couple to Gs to activate adenylyl cyclase and increase cAMP levels but less efficiently than coupling to Gq.
References:  33,54
Tissue Distribution Click here for help
Prostate cancer cell lines DU145, PC3 and TRAMP.
Species:  Human
Technique:  Radioligand binding.
References:  76
Mesenchymal stromal cells.
Species:  Human
Technique:  RT-PCR, immunocytochemistry.
References:  46
α1B-adrenoceptors are either absent or scarce on human prostatic stromal smooth muscle, proximal urethra or corpus cavernosa, present in the human spleen and kidney, and with other subtypes in human somatic arteries and veins.
Species:  Human
Technique:  RT-PCR, RNase protection assay.
References:  54,66
Lymphocytes & saphenous vein.
Species:  Human
Technique:  In situ hybridisation.
References:  82,92
Osteoblasts & SaM-1 cell line.
Species:  Human
Technique:  RT-PCR, antagonist (chloroethyclonidine) effects.
References:  41,44
Coronary endothelial cells.
Species:  Human
Technique:  PCR, radioligand binding.
References:  42
Uterus, cervix & umbilical vein.
Species:  Human
Technique:  RT-PCR, tissue contraction.
References:  26-27
Ventricular myocytes.
Species:  Mouse
Technique:  RT-qPCR, ERK1/2 responses, contraction, FRET, confocal microscopy.
References:  58,91
Testes & spermatocytes.
Species:  Mouse
Technique:  In situ hybridisation.
References:  53
Atria.
Species:  Mouse
Technique:  RT-PCR, positive inotropic and chronotropic effects.
References:  101
Cerebral cortex, cerebellum, amygdaloid, hypothalamus, midbrain, pontine, spinal cord, olfactory, periaqueductal grey, NG2 oligodendrocytes.
Species:  Mouse
Technique:  In situ hybridisation, GFP-tagged transgenic mouse.
References:  60,62
Spleen.
Species:  Mouse
Technique:  Isometric contractions of spleen from α1A/D–knockout mice.
References:  6
Bone formation and cellular proliferation.
Species:  Mouse
Technique:  Tomography of fluorescently labelled bone in WT and α1B-AR knockout mice.
References:  81
Nucleus accumbens - unmyelinated axons and axon terminals with some labeling in dendrites.
Species:  Rat
Technique:  Immunohistochemistry and electron microscopy.
References:  56
In the rat brain, highest levels of α1B-AR are found in regions involved in stress and neuroendocrine function, including hypothalamic paraventricular nuclei, supraoptic nucleus, median eminence and arcuate nucleus. Also in layer V of the frontal cortex, thalamus, hippocampus, diagonal band of Broca and caudate-putamen. Some midbrain and hindbrain regions important for motor function were also immunoreactive.
Species:  Rat
Technique:  Immunohistochemistry.
References:  1,21
Taste buds.
Species:  Rat
Technique:  RT-PCR
References:  102
Prefrontal cortex, contralateral hind limb, somatosensory cortex, secondary motor cortex, ipsilateral laminae I-III spinal cord.
Species:  Rat
Technique:  In situ hybridisation.
References:  59,73
Liver, hepatocytes, carotid artery.
Species:  Rat
Technique:  Receptor binding 3H prazosin.
References:  93
High expression levels of α1B-AR in the medial layer of the aorta and caudal, femoral, iliac, renal, superior mesenteric and mesenteric resistance arteries.
Species:  Rat
Technique:  Immunohistochemistry.
References:  65
Spleen.
Species:  Rat
Technique:  Isometric contractions of spleen and selective antagonists.
References:  7
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
Isometric contraction of mouse spleen.
Species:  Mouse
Tissue:  Spleen.
Response measured:  Contraction.
References:  6-7
Isolated longitudinal strip of rat spleen.
Species:  Rat
Tissue:  Spleen
Response measured:  Contraction
References:  79
Isolated first order venules.
Species:  Human
Tissue:  Vasculature.
Response measured:  Contraction.
References:  31
Nerve growth factor increases α1B-AR expression and augments neuronal responsiveness to norepinephrine.
Species:  Rat
Tissue:  Primary dorsal root ganglion cells.
Response measured:  Neuronal responsiveness.
References:  100
Sphingosine-1-phosphate or lysophosphatidic acid induced α1B-AR desensitization and phosphorylation.
Species:  Rat
Tissue:  Transfected Rat-1 fibroblasts.
Response measured:  Phosphorylation and desensitization.
References:  14-15
α1B-AR mediated renal vasoconstriction during renal impairment, but not during normal renal function.
Species:  Rat
Tissue:  Kidney.
Response measured:  Vasconstriction.
References:  43
Reduced binding affinity for prazosin and tamsulosin associated with T130A mutation in transmembrane domain III.
Species:  Human
Tissue:  HEK 293 cells transfected with human α1B-AR cDNA.
Response measured:  Receptor binding.
References:  80
Desensitisation of α1B-AR produced by insulin, insulin-like growth factor-1 and estrogen.
Species:  Human
Tissue:  Transfected Rat-1 cells & DDT1MF2 cells.
Response measured:  Desensitization and internalization.
References:  13,29,32,57
Functional changes produced by formation of heterodimers with α1B- or α1D-ARs. Heterodimer formation is observed for human AND rat receptors.
Species:  Human
Tissue:  Transfected HEK 293 & DDT(1)MF-2 cells.
Response measured:  Heterodimer formation.
References:  34,85
Internalisation of α1B-ARs.
Species:  Human
Tissue:  HEK293 cells.
Response measured:  FRET, confocal microscopy, and intracellular calcium quantitation.
References:  4
Functional changes produced by formation of heterodimers with α1B- and α1D-ARs.
Species:  Human
Tissue:  Vascular smooth muscle cells.
Response measured:  Heterodimer formation and function.
References:  2
Phosphorylation and desensitisation of α1B-ARs.
Species:  Human
Tissue:  HEK293 cells.
Response measured:  Mass spectrometry, FRET, Ca2+ signaling.
References:  38-39
The selectivity of α-adrenoceptor agonists for the human α1Aa, α1Ba, and α1D-ARs.
Species:  Human
Tissue:  CHO-K1 cells stably expressing α1B-AR.
Response measured:  Whole cell [3H]prazosin binding, intracellular Ca2++ release, ERK1/2 phosphorylation, cAMP accumulation.
References:  67
Rat primary neonatal cardiomyocytes.
Species:  Rat
Tissue:  Neonatal cardiomyocytes.
Response measured:  Transcriptome analysis of signalling pathways.
References:  51
Signalling, oligomerisation and nuclear localisation of α1B-AR in ventricular myocytes.
Species:  Mouse
Tissue:  Ventricular myocytes.
Response measured:  Receptor knockout mice, adenovirus transfection, confocal microscopy, FRET, ERK1/2 responses.
References:  91
Binding phenotypes of α1B-AR.
Species:  Rat
Tissue:  Liver intact preparations and homogenates, carotid artery.
Response measured:  Receptor binding.
References:  93
Analysis of adrenoceptor subtypes in ventricular myocytes.
Species:  Mouse
Tissue:  Ventricular myocytes.
Response measured:  Receptor knockin and knockout mice, ERK1/2 and phospholamban responses, contraction.
References:  58
Role of α1B-AR in bone formation.
Species:  Mouse
Tissue:  Bone.
Response measured:  Microcomputed tomography and fluorescent labelling of bone.
References:  81
Physiological Functions Click here for help
Contraction of mesenteric resistance arteries.
Species:  Rat
Tissue:  Vasculature.
References:  65
Contraction of umbilical vein.
Species:  Human
Tissue:  Vasculature.
References:  27
α1B-AR roles in the regulation of cardiac growth and contractile function.
Species:  Mouse
Tissue:  Heart.
References:  18,101
Contraction of mammary artery and saphenous vein (with α1A).
Species:  Human
Tissue:  Vasculature
References:  31
Adrenaline induced stimulation of hydroxyl radical formation in isolated hepatocytes.
Species:  Rat
Tissue:  Liver.
References:  17
CNS Stimulation by d-amphetamine, cocaine and morphine.
Species:  Mouse
Tissue:  Brain.
References:  25
Growth of vascular adventitia following balloon injury.
Species:  Rat
Tissue:  Aorta.
References:  99
α1B-AR activation initiates a PLC-dependent biphasic change in pinealocyte membrane potential.
Species:  Rat
Tissue:  Primary pinealocytes.
References: 
Increased replication of human osteoblasts.
Species:  Human
Tissue:  Bone.
References:  41
Diabetes increases α1B-AR mRNA in non-pregnant rats.
Species:  Rat
Tissue:  Uterus.
References:  78
Hetero-oligomer formation with ACKR-3 and CXCR4 required for α1B-AR function.
Species:  Human
Tissue:  Vascular smooth muscle cells.
References:  2
Modulation of α1B-AR translocation to endosomes by PKC and Rab9.
Species:  Human
Tissue:  Transfected HEK293 cells.
References:  4
Contraction of spleen.
Species:  Rat
Tissue:  Spleen.
References:  7
Homologous and heterologous desensitisation direct α1B-AR to different endocytotic vesicles.
Species:  Human
Tissue:  HEK293 cells.
References:  16
Enhanced viability but not proliferation.
Species:  Human
Tissue:  Colonic cancer SW480 cells.
References:  36
α1B-AR activation initiates a PLC-dependent biphasic change in pinealocyte membrane potential.
Species:  Rat
Tissue:  Primary pinealocytes.
References:  97
Bone formation and cellular proliferation.
Species:  Mouse
Tissue:  Osteoblasts.
References:  81
Physiological Consequences of Altering Gene Expression Click here for help
Mice with myocyte-targeted α1B-ARs develop spontaneous ventricular arrhythmias and repolarization defects with age
Species:  Mouse
Tissue:  Heart.
Technique:  Gene over-expression.
References:  71
α1B-AR knockout mice display reduced neointimal growth, adventitial thickening and lumen loss. α1B-AR mediates vascular remodeling trophic effects after injury.
Species:  Mouse
Tissue:  Carotid artery.
Technique:  Gene knockout.
References:  98
Mice with constitutively active mutation (CAM) have decreased inotropic response to phenylephrine (decreased cardiac function).
Species:  Mouse
Tissue:  Heart.
Technique:  Gene over-expression, Langendorff isolated perfused heart assay.
References:  72
α1B-AR knockout mice display reduced fertility and spermatogenesis (hypofertile, low testosterone, high leutinizing hormone).
Species:  Mouse
Tissue:  Testes.
Technique:  Gene knockouts.
References:  53
α1B-AR knockout mice exhibit altered locomoter and rewarding effects of psychostimulants and opiates; mediates dopamine release (hyperactivity and rewarding behavior of cocaine, morphine, amphetamine).
Species:  Mouse
Tissue:  Brain.
Technique:  Gene knockouts.
References:  8,22,86
α1B-AR knockout mice display attenuated pressor and positive inotropic effects after transient bilateral carotid occlusion and denervated aortic baroreceptor surgery. α1B-AR regulates sympathetic neuroeffector junction and baroreceptor activation.
Species:  Mouse
Tissue:  Mesenteric vasculature.
Technique:  Gene knockout.
References:  84
Mice with constitutively active mutation (CAM) have cardiac gene expression profile consistent with maladaptive hypertrophy (a gene expression profile of inflammation, hypertrophy, Src related signaling).
Species:  Mouse
Tissue:  Heart.
Technique:  Gene over-expression and microarray analysis.
References:  96
Mice with constitutively active mutation (CAM) have decreased inotropic response to phenylephrine (decreased cardiac function).
Species:  Mouse
Tissue:  Heart.
Technique:  Gene over-expression, Langendorff isolated perfused heart assay.
References:  72
Mice with constitutively active mutation (CAM) have increased apoptosis, NMDA receptors, but decreased GABA-A receptor (neurodegenerative profile).
Species:  Mouse
Tissue:  Brain.
Technique:  Gene over-expression and microarry analysis.
References:  95
Mice with constitutively active mutation (CAM) have increased spontaneous interictal epileptogenicity and EEG /behavioral seizures (epilepsy).
Species:  Mouse
Tissue:  Brain.
Technique:  Gene over-expression.
References:  47
α1B-AR knockout mice display compensatory changes in α1-AR subtypes; liver from α1B-AR knockout animals displays increased α1A-AR expression.
Species:  Mouse
Tissue:  Liver, hepatocytes.
Technique:  Gene knockout.
References:  23
Mice with constitutively active mutation (CAM) have progressive synucleinopathy that is rescued by long-term terazosin treatment (abnormal aggregated alpha-synuclein inclusion bodies & Purkinje cell loss).
Species:  Mouse
Tissue:  Brain.
Technique:  Gene over-expression.
References:  63
α1B-AR knockout mice display impaired glucose homeostasis (hyperinsulinemia and insulin resistance).
Species:  Mouse
Tissue:  Blood, liver.
Technique:  Gene knockout.
References:  11
Mice with constitutively active mutation (CAM) have hypotension, autonomic failure and cardiac hypertrophy (lower basal and phenylephrine-induced blood pressure, cardiac hypertrophy, cardiac dysfunction, reduced plasma catecholamines and cortisol, weight loss).
Species:  Mouse
Tissue:  Brain & heart.
Technique:  Gene over-expression.
References:  103
α1B-AR knockout mice are protected against methamphetamine induced degeneration (methamphetamine toxicity) of the nigro-striatal neuronal pathway in CNS and show an enhanced reactivity to new situations.
Species:  Mouse
Tissue:  Brain- nigro-striatal projection.
Technique:  Gene knockout.
References:  9
α1B- knockout mice have elevated glycogen stores in both fed and fasted state and are hyperinsulinemic when fasted. They are more sensitive to obesity induced by a high fat diet.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  20
α1B-AR play an important role in bone formation and cellular proliferation.
Species:  Mouse
Tissue:  Bone.
Technique:  Gene knockout, examination of bone microarchitecture by microcomputed tomography and bone formation by fluorescent labelling of bone.
References:  81
Mice with constitutively active mutation (CAM) have progressive apoptotic Parkinsonian-like neurodegeneration with multiple system atrophy (granulovacular apoptotic neurodegeneration, movement disorder, dopaminergic degeneration).
Species:  Mouse
Tissue:  Haert.
Technique:  Gene over-expression.
References:  104
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
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0004184 abnormal baroreceptor physiology PMID: 15466664 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0002972 abnormal cardiac muscle contractility PMID: 14519431 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0000304 abnormal cardiac stroke volume PMID: 12782680 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0001544 abnormal cardiovascular system physiology PMID: 12782680 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0002332 abnormal exercise endurance PMID: 12782680 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0002078 abnormal glucose homeostasis PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0003921 abnormal heart left ventricle morphology PMID: 15466664 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0005406 abnormal heart size PMID: 12782680 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0001449 abnormal learning/ memory PMID: 11222061 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0004215 abnormal myocardial fiber physiology PMID: 14519431 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0003562 abnormal pancreatic beta cell physiology PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0003461 abnormal response to novel object PMID: 11222061 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0002216 abnormal seminiferous tubule morphology PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0002784 abnormal Sertoli cell morphology PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0001463 abnormal spatial learning PMID: 11222061 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0000230 abnormal systemic arterial blood pressure PMID: 9326654 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0002782 abnormal testicular secretion PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0001155 arrest of spermatogenesis PMID: 17951539 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0006138 congestive heart failure PMID: 12782680 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0005140 decreased cardiac muscle contractility PMID: 15466664  9326654 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0003393 decreased cardiac output PMID: 12782680 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0002702 decreased circulating free fatty acid level PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0002780 decreased circulating testosterone level PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0001417 decreased exploration in new environment PMID: 11115730 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0005439 decreased glycogen level PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0005333 decreased heart rate PMID: 15466664 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0005333 decreased heart rate PMID: 12782680 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0002834 decreased heart weight PMID: 12782680 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0001935 decreased litter size PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0004901 decreased male germ cell number PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0002843 decreased systemic arterial blood pressure PMID: 15466664 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0006264 decreased systemic arterial systolic blood pressure PMID: 15466664 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0004852 decreased testis weight PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0003026 decreased vasoconstriction PMID: 15466664 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0003068 enlarged kidney PMID: 12782680 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0001559 hyperglycemia PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0009750 impaired behavioral response to addictive substance PMID: 11923452 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0009712 impaired conditioned place preference behavior PMID: 11923452 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0005293 impaired glucose tolerance PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd		 MGI:104774  MP:0004000 impaired passive avoidance behavior PMID: 11115730 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0005599 increased cardiac muscle contractility PMID: 12782680 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0002079 increased circulating insulin level PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0005669 increased circulating leptin level PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0001751 increased circulating luteinizing hormone level PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0001415 increased exploration in new environment PMID: 11222061 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0005440 increased glycogen level PMID: 14581480 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0003823 increased left ventricular developed pressure PMID: 14519431 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0005458 increased percent body fat PMID: 14581480 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0004485 increased response of heart to induced stress PMID: 12782680 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0009763 increased sensitivity to induced morbidity/mortality PMID: 12782680 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0005658 increased susceptibility to diet-induced obesity PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * C57BL/6J		 MGI:104774  MP:0005331 insulin resistance PMID: 14581480 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0008280 male germ cell apoptosis PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0001925 male infertility PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0001922 reduced male fertility PMID: 17951539 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0002188 small heart PMID: 12782680 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
B6.129-Adra1b Adra1a		 MGI:104773  MGI:104774  MP:0002188 small heart PMID: 12782680 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
involves: 129P2/OlaHsd * 129X1/SvJ * C57BL/6 * FVB/N		 MGI:104773  MGI:104774  MP:0004565 small myocardial fiber PMID: 12782680 
Adra1atm1Pcs|Adra1btm1Cta Adra1atm1Pcs/Adra1atm1Pcs,Adra1btm1Cta/Adra1btm1Cta
B6.129-Adra1b Adra1a		 MGI:104773  MGI:104774  MP:0004565 small myocardial fiber PMID: 12782680 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0001157 small seminal vesicle PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0001153 small seminiferous tubules PMID: 17951539 
Adra1btm1Cta Adra1btm1Cta/Adra1btm1Cta
involves: 129/Sv * C57BL/6J		 MGI:104774  MP:0001147 small testis PMID: 17951539 

References

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