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α1A-adrenoceptor

Family: Adrenoceptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Allosteric Regulators
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 466 8p21-p11.2 ADRA1A adrenoceptor alpha 1A
Mouse 7 466 14 D1 Adra1a adrenergic receptor, alpha 1a
Rat 7 466 15p12 Adra1a adrenoceptor alpha 1A
Previous and Unofficial Names
adrenergic receptor
α1a
α1c
ADRA1C
ADRA1L1
adrenergic, alpha-1A-, receptor
adrenergic receptor, alpha 1a
adrenergic alpha 1c receptor
adrenergic receptor alpha 1c
adrenergic receptor alpha 1c subtype
adrenergic receptor, alpha 1c
alpha 1A-adrenoceptor
alpha 1A-adrenoreceptor
alpha 1C-adrenergic receptor
alpha-1A adrenergic receptor
alpha-1A adrenoceptor
alpha-1A adrenoreceptor
alpha-1C adrenergic receptor
Database Links
ChEMBL Target 125 (Hs), 12271 (Mm), 12514 (Rn)
DrugBank Target 556 (Hs)
Ensembl ENSG00000120907 (Hs), ENSMUSG00000045875 (Mm), ENSRNOG00000009522 (Rn)
Entrez Gene 148 (Hs), 11549 (Mm), 29412 (Rn)
GeneCards ADRA1A (Hs)
GenitoUrinary Development Molecular Anatomy Project Adra1a (Mm)
HomoloGene 68078 (Hs)
Human Protein Reference Database 00081 (Hs)
InterPro P35348 (Hs), P97718 (Mm), P43140 (Rn)
KEGG Gene hsa:148 (Hs), mmu:11549 (Mm), rno:29412 (Rn)
OMIM 104221 (Hs)
PharmGKB Gene PA34 (Hs)
PhosphoSitePlus P35348 (Hs), P97718 (Mm), P43140 (Rn)
Protein Ontology (PRO) PRO:000001183 (Hs)
RefSeq Nucleotide NM_000680 (Hs), NM_013461 (Mm), NM_017191 (Rn)
RefSeq Protein NP_000671 (Hs), NP_038489 (Mm), NP_058887 (Rn)
TreeFam ENSG00000120907 (Hs), ENSMUSG00000045875 (Mm), ENSRNOG00000009522 (Rn)
UniGene Hs. 52931 (Hs)
UniProt P35348 (Hs), P97718 (Mm), P43140 (Rn)
Wikipedia α1A-adrenoceptor
Adrenoceptors
Search for 3D structures on the PDB
Search by keyword: Adrenoceptors α1A-adrenoceptor Search by accession number: P43140, P35348, P97718
Natural/Endogenous Ligand(s)
(-)-adrenaline
(-)-noradrenaline
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]HEAT Hs Full agonist 10.0 pKd 24
oxymetazoline Hs Full agonist 8.0 – 8.2 pKi 18,24,27
dabuzalgron Hs Agonist 7.4 pKi 1
(-)-adrenaline Hs Full agonist 6.3 pKi 24
NS-49 Hs Partial agonist 6.2 pKi 18
(-)-noradrenaline Hs Full agonist 5.8 – 6.0 pKi 24,27
phenylephrine Hs Full agonist 5.2 – 5.4 pKi 27
methoxamine Hs Full agonist 5.0 – 5.2 pKi 24,27
(+)-adrenaline Hs Full agonist 5.0 pKi 24
A61603 Hs Full agonist 7.8 – 8.4 pIC50 6,12
Agonist Comments
The first α1A-adrenoceptor to be cloned was the bovine homolog. No species significant differences in pharmacology have been identified.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]BE-2254 Hs Antagonist 9.9 pKd 16,23
silodosin Hs Antagonist 10.4 pKi 24
tamsulosin Hs Antagonist 10.0 – 10.7 pKi 3-4,6,24,31
WB 4101 Rn Antagonist 10.2 pKi 29
NAN 190 Hs Antagonist 10.1 pKi 32
WB 4101 Hs Antagonist 9.7 – 9.8 pKi 3-4,6,24
Rec 15/2739 Hs Antagonist 9.6 pKi 6
RS-100329 Hs Antagonist 9.6 pKi 31
(+)-niguldipine Hs Antagonist 9.1 – 10.0 pKi 6,24
prazosin Rn Inverse agonist 9.5 pKi 29
prazosin Hs Inverse agonist 9.0 – 9.9 pKi 3-4,6,24,31
(+)-niguldipine Rn Antagonist 9.3 pKi 29
RS-17053 Hs Antagonist 9.2 – 9.3 pKi 3-4,6
SNAP5089 Hs Antagonist 8.8 – 9.4 pKi 9,14,30
5-methylurapidil Hs Antagonist 8.9 – 9.2 pKi 3,6,22,24,32
5-methylurapidil Rn Antagonist 9.0 pKi 29
Ro-70-0004 Hs Antagonist 8.9 pKi 31
A-119637 Hs Antagonist 8.6 pKi 2
A-119637 Rn Antagonist 8.6 pKi 2
phentolamine Hs Antagonist 8.6 pKi 24
roxindole Hs Antagonist 8.6 pKi 17
A-123189 Rn Antagonist 8.5 pKi 2
terguride Hs Antagonist 8.5 pKi 17
A-123189 Hs Antagonist 8.4 pKi 2
indoramin Hs Antagonist 8.4 pKi 4,6
risperidone Hs Antagonist 8.4 pKi 32
ritanserin Hs Antagonist 8.4 pKi 32
lisuride Hs Antagonist 8.3 pKi 17
spiperone Hs Antagonist 8.3 pKi 32
ketanserin Hs Antagonist 8.2 pKi 32
clozapine Hs Antagonist 8.1 pKi 32
phentolamine Rn Antagonist 8.1 pKi 29
(+)-cyclazosin Hs Antagonist 7.9 pKi 7
mianserin Hs Antagonist 7.6 pKi 32
cyproheptadine Hs Antagonist 7.4 pKi 32
spiroxatrine Hs Antagonist 7.3 pKi 32
BMY-7378 Rn Antagonist 7.0 pKi 2
BMY-7378 Hs Antagonist 6.9 – 7.0 pKi 2,32
cabergoline Hs Antagonist 6.5 pKi 17
piribedil Hs Antagonist 6.1 pKi 17
View species-specific antagonist tables
Antagonist Comments
Compounds such as prazosin and RS-17053 show unexpectedly low potency in certain isolated tissue assays (e.g. canine prostate) [9]. This was postulated to result from a novel α1- adrenoceptor subtype (α1L). It is now thought that this may result from differences in α1A-adrenoceptor characteristics dependent on tissue or assay environment [6].
Compounds designated as "partial inverse agonists" [16] are listed as neutral antagonists
Allosteric Regulator Comments
While no allosteric regulation of the α1A-adrenoceptor has been proven, possible allosteric enhancement has been shown with high concentrations of benzodiazepines. Amiloride analogs will increase the dissociation rate of prazosin from the α1A- adrenoceptor [8]

Explore drug-target interactions for this set of compounds using iPHACE

Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Calcium channel
Other - See Comments
Comments:  The α1A-adrenoceptor is coupled to calcium release and inositol phosphate production more efficiently than the other subtypes.
References:  8,16
Secondary Transduction Mechanisms
Transducer Effector/Response
Phospholipase D stimulation
Other - See Comments
Comments:  α1-adrenoceptors (all subtypes) can also activate protein Kinase C, mitogen activated protein kinases.
References:  8,16
Tissue Distribution
In the human brain, the highest levels of α1A message are found in olfactory system, hypothalamic nuclei and in regions of the brainstem and spinal cord related to motor function.
Species:  Human
Technique:  in situ hybridisation.
References:  5
High expression levels of α1A-adrenoceptor mRNA are found in the heart, liver, cerebelum and cerebral cortex
Species:  Human
Technique:  RNase Protection
References:  20
The α1A-adrenoceptor is the predominant subtype in human prostate and urethra.
Species:  Human
Technique:  Immunohistochemistry.
References:  28
Expression Datasets

Click here to show/hide data

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
Isolated longitudinal strip of Vas Deferens.
Species:  Rat
Tissue:  Vas deferens
Response measured:  Contraction
References:  19
Isolated strips of prostate tissue containing both glandular and smooth muscle elements.
Species:  Human
Tissue:  Prostrate
Response measured:  Contraction
References:  6
Physiological Functions
Contraction of stromal and capsular smooth muscle to control urethral resistance.
Species:  Human
Tissue:  Prostate.
References:  10
Contraction of urethral smooth muscle.
Species:  Human
Tissue:  Urethra.
References:  26
Stimulation of myocyte hypertrophy.
Species:  Rat
Tissue:  Myocardium.
References:  13
Activation of sarcolemmal Na+-H+ exchanger.
Species:  Rat
Tissue:  Ventricular Myocytes.
References:  25
Contraction of skeletal muscle resistance arteries.
Species:  Human
Tissue:  Vasculature.
References:  11
Physiological Consequences of Altering Gene Expression
Cardiac specific overexpression of α1A-adrenoceptors enhanced cardiac contractility.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  15
Hypotension and a decreased pressor response to phenylephrine were observed in α1A- knockout mice.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  21
Phenotypes, Alleles and Disease Models Mouse data from MGI

Click here to show/hide data

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
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 
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 
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 
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 
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 
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 Adra1atm1Pcs/Adra1atm1Pcs
involves: 129X1/SvJ * FVB/N		 MGI:104773  MP:0003929 decreased heart rate variability PMID: 12093905 
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 
Adra1atm1Pcs Adra1atm1Pcs/Adra1atm1Pcs
involves: 129X1/SvJ * FVB/N		 MGI:104773  MP:0003026 decreased vasoconstriction PMID: 12093905 
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 
Adra1atm1Pcs Adra1atm1Pcs/Adra1atm1Pcs
involves: 129X1/SvJ * FVB/N		 MGI:104773  MP:0001596 hypotension PMID: 12093905 
Adra1a+|Adra1atm1Pcs Adra1atm1Pcs/Adra1a+
involves: 129X1/SvJ * FVB/N		 MGI:104773  MP:0001596 hypotension PMID: 12093905 
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 
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 
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 
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 

REFERENCES

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To cite this database page, please use the following:

Richard A. Bond, David B. Bylund, Douglas C. Eikenburg, J. Paul Hieble, Rebecca Hills, Kenneth P. Minneman, Sergio Parra.
Adrenoceptors: α1A-adrenoceptor. Last modified on 19/02/2013. Accessed on 21/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=22.


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