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α2C-adrenoceptor

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Target not currently curated in GtoImmuPdb

Target id: 27

Nomenclature: α2C-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 7 462 4p16.3 ADRA2C adrenoceptor alpha 2C 34
Mouse 7 458 5 18.09 cM Adra2c adrenergic receptor, alpha 2c 23
Rat 7 458 14q21 Adra2c adrenoceptor alpha 2C 12
Previous and Unofficial Names Click here for help
α2-C4 | ADRA2L2 | ADRA2RL2 | Adrenergic alpha2C- receptor class I | alpha-2 adrenergic receptor subtype C4 | alpha-2C adrenergic receptor | alpha-2C adrenoreceptor | Adra-2c | adrenergic receptor
Database Links Click here for help
Specialist databases
GPCRdb ada2c_human (Hs), ada2c_mouse (Mm), ada2c_rat (Rn)
Other databases
Alphafold P18825 (Hs), Q01337 (Mm), P22086 (Rn)
ChEMBL Target CHEMBL1916 (Hs), CHEMBL4826 (Mm), CHEMBL314 (Rn)
DrugBank Target P18825 (Hs), P18825 (Hs), P18825 (Hs)
Ensembl Gene ENSG00000184160 (Hs), ENSMUSG00000045318 (Mm), ENSRNOG00000009299 (Rn)
Entrez Gene 152 (Hs), 11553 (Mm), 24175 (Rn)
Human Protein Atlas ENSG00000184160 (Hs)
KEGG Gene hsa:152 (Hs), mmu:11553 (Mm), rno:24175 (Rn)
OMIM 104250 (Hs)
Pharos P18825 (Hs)
RefSeq Nucleotide NM_000683 (Hs), NM_007418 (Mm), NM_138506 (Rn)
RefSeq Protein NP_000674 (Hs), NP_031444 (Mm), NP_612515 (Rn)
UniProtKB P18825 (Hs), Q01337 (Mm), P22086 (Rn)
Wikipedia ADRA2C (Hs)
Natural/Endogenous Ligands Click here for help
(-)-adrenaline
(-)-noradrenaline
Comments: Adrenaline exhibits greater relative potency than noradrenaline

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
dexmedetomidine 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 Full agonist 7.0 – 9.3 pKi 18,28,30,33
⤷ pKi 7.0 – 9.3 [18,28,30,33]
apraclonidine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Agonist 7.5 pKi 27,33
⤷ pKi 7.5 (Ki 3x10-8 M) [27,33]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 7.2 pKi 26
⤷ pKi 7.2 [26]
lofexidine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist 7.2 pKi 7
⤷ pKi 7.2 (Ki 6.92x10-8 M) [7]
Description: Calculated from [3H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human α2C-AR.
clonidine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 6.0 – 7.8 pKi 18,28,30
⤷ pKi 6.0 – 7.8 [18,28,30]
oxymetazoline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 6.7 pKi 18,21,33,36
⤷ pKi 6.7 [18,21,33,36]
brimonidine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Partial agonist 5.7 – 7.6 pKi 18,25,28,30,33
⤷ pKi 5.7 – 7.6 [18,25,28,30,33]
(-)-noradrenaline Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 5.7 – 6.8 pKi 18,21,30,33
⤷ pKi 5.7 – 6.8 [18,21,30,33]
(±)-adrenaline Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.8 – 6.2 pKi 18
⤷ pKi 5.8 – 6.2 [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 5.8 pKi 18,33
⤷ pKi 5.8 [18,33]
guanfacine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 5.4 – 6.2 pKi 18
⤷ pKi 5.4 – 6.2 [18]
xylazine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 4.8 – 5.9 pKi 18
⤷ pKi 4.8 – 5.9 [18]
guanabenz Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Agonist 6.0 pIC50 1,33
⤷ pIC50 6.0 (IC50 1.106x10-6 M) [1,33]
moxonidine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist - - 33
⤷ [33]
Agonist Comments
[125I]p-iodoclonidine binds to the human α2C receptor with a Kd of 1.3 nM [31].
Apraclonidine is an approved drug agonist of α2-adrenoceptors [27].
As an endogenous ligand, (-)-noradrenaline has intrinsic activity across the adrenoceptor family, but we've only tagged α2B and α2C subtypes as primary drug target as the drug has highest affinity at these isoforms.
Guanabenz order of affinity is α2A-AR>α2B-AR>α2C-AR [1].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
JP1302 Small molecule or natural product Hs Antagonist 6.9 – 7.8 pKB 32,35
⤷ pKB 6.9 – 7.8 [32,35]
[3H]MK-912 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 10.1 pKd 36
⤷ pKd 10.1 (Kd 8.6x10-11 M) [36]
[3H]rauwolscine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.9 pKd 3,5
⤷ pKd 9.9 [3,5]
[3H]RX821002 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 8.2 – 9.2 pKd 5-6
⤷ pKd 8.2 – 9.2 [5-6]
MK-912 Small molecule or natural product Hs Antagonist 9.8 – 10.0 pKi 32
⤷ pKi 9.8 – 10.0 [32]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 9.3 – 9.9 pKi 25-26,32
⤷ pKi 9.3 – 9.9 [25-26,32]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 9.1 pKi 26
⤷ pKi 9.1 [26]
rauwolscine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.1 pKi 36
⤷ pKi 9.1 [36]
yohimbine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.5 – 9.5 pKi 3,6,32,36
⤷ pKi 8.5 – 9.5 [3,6,32,36]
spiroxatrine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.7 – 9.0 pKi 32,36
⤷ pKi 8.7 – 9.0 [32,36]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 26
⤷ pKi 8.8 [26]
WB 4101 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 9.4 pKi 3,6,32,36
⤷ pKi 8.2 – 9.4 [3,6,32,36]
atipamezole Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 32
⤷ pKi 8.5 [32]
RX821002 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.1 – 8.7 pKi 32,35-36
⤷ pKi 8.1 – 8.7 [32,35-36]
lurasidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.0 pKi 17
⤷ pKi 8.0 (Ki 1.08x10-8 M) [17]
EGIS-11150 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.9 pKi 13
⤷ pKi 7.9 (Ki 1.3x10-8 M) [13]
phentolamine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.6 – 7.9 pKi 3,6
⤷ pKi 7.6 – 7.9 [3,6]
all-trans-4-oxo-retinoic acid Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.7 pKi 11
⤷ pKi 7.7 (Ki 1.8x10-8 M) [11]
mirtazapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.7 pKi 11
⤷ pKi 7.7 (Ki 1.8x10-8 M) [11]
Description: Inhibition of [3H]rauwolscine binding.
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.7 pKi 26
⤷ pKi 7.7 [26]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.6 pKi 26
⤷ pKi 7.6 [26]
ARC-239 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 – 8.4 pKi 3,6,36
⤷ pKi 6.7 – 8.4 [3,6,36]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.4 pKi 26
⤷ pKi 7.4 [26]
prazosin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.7 – 8.0 pKi 3,6,36
⤷ pKi 6.7 – 8.0 [3,6,36]
piribedil Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.2 pKi 26
⤷ pKi 7.2 [26]
idazoxan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.2 pKi 32
⤷ pKi 7.2 [32]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.9 – 7.4 pKi 3,6
⤷ pKi 6.9 – 7.4 [3,6]
BRL 44408 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 36
⤷ pKi 6.8 [36]
tolazoline Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 5.4 pKi 18
⤷ pKi 5.4 (Ki 3.715x10-6 M) [18]
Description: Inhibition of agonist-stimulated [35S]GTPγS binding
mirtazapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.7 pIC50 20
⤷ pIC50 6.7 (IC50 1.995x10-7 M) [20]
Antagonist Comments
Mirtazapine is an antagonist of α2-adrenoceptors and serotonin 5-HT2a and 5-HT2c receptors.
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
Potassium channel
Calcium channel
References:  4,22
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family Adenylyl cyclase stimulation
Comments:  The physiological significance of this mechanism is unknown.
References:  9
Tissue Distribution Click here for help
Brain = kidney > aorta = lung = skeletal muscle = heart = spleen.
Absent in the liver.
Species:  Human
Technique:  RNAse protection of mRNA.
References:  10,29
Brain >> kidney.
Absent in spleen, aorta, heart, liver, lung, skeletal muscle.
Species:  Human
Technique:  RNAse protection of mRNA.
References:  2,15
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
Measurment of adenylate cyclase activity. This assay is done intact cell preparations (either native or transfected) using the [3H]adenine prelabeling technique to measure cAMP accumulation.
Species:  Human
Tissue: 
Response measured:  Inhibition of cAMP accumulation.
References:  4
Isometric contraction is measured with rings of human saphenous veins (3–5 mm) attached to myograph transducers under 1 g tension in organ bath at 37 °C.
Species:  Human
Tissue:  Saphenous vein.
Response measured:  Contraction.
References:  8,14
Physiological Functions Click here for help
Presynaptic inhibition of noradrenaline release.
Species:  Mouse
Tissue:  Heart; central noradrenergic neurons.
References:  16,19
Physiological Consequences of Altering Gene Expression Click here for help
α2C-adrenoceptor knock-out mice show no change in cardiovascular and sedative effects with a non-selective adrenoceptor agonist.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  19
The development of α2B and α2C knock-out mice has shown that these two subtypes are not involved in the central hypotensive response to α2 agonists.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  24
α2C knockout mice exhibit disruption of presynaptic inhibition of noradrenaline release at low stimulation frequencies.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  16
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
Adra2atm1Bkk|Adra2btm1Gsb|Adra2ctm1Gsb Adra2atm1Bkk/Adra2atm1Bkk,Adra2btm1Gsb/Adra2btm1Gsb,Adra2ctm1Gsb/Adra2ctm1Gsb
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * DBA/2J		 MGI:87934  MGI:87935  MGI:87936  MP:0001712 abnormal placenta development PMID: 12068299 
Adra2ctm1Gsb Adra2ctm1Gsb/Adra2ctm1Gsb
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * DBA/2J		 MGI:87936  MP:0008428 abnormal spatial working memory PMID: 10051760  11642653 
Adra2atm1Bkk|Adra2ctm1Gsb Adra2atm1Bkk/Adra2atm1Bkk,Adra2ctm1Gsb/Adra2ctm1Gsb
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * DBA/2J		 MGI:87934  MGI:87936  MP:0005447 abnormal synaptic norepinephrine release PMID: 10647009 
Adra2atm1Bkk|Adra2btm1Gsb|Adra2ctm1Gsb Adra2atm1Bkk/Adra2atm1Bkk,Adra2btm1Gsb/Adra2btm1Gsb,Adra2ctm1Gsb/Adra2ctm1Gsb
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * DBA/2J		 MGI:87934  MGI:87935  MGI:87936  MP:0001718 abnormal yolk sac morphology PMID: 12068299 
Adra2ctm1Gsb Adra2ctm1Gsb/Adra2ctm1Gsb
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * DBA/2J		 MGI:87936  MP:0002573 behavioral despair PMID: 10523817 
Adra2atm1Bkk|Adra2ctm1Gsb Adra2atm1Bkk/Adra2atm1Bkk,Adra2ctm1Gsb/Adra2ctm1Gsb
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * DBA/2J		 MGI:87934  MGI:87936  MP:0001625 cardiac hypertrophy PMID: 10647009 
Adra2atm1Bkk|Adra2btm1Gsb|Adra2ctm1Gsb Adra2atm1Bkk/Adra2atm1Bkk,Adra2btm1Gsb/Adra2btm1Gsb,Adra2ctm1Gsb/Adra2ctm1Gsb
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * DBA/2J		 MGI:87934  MGI:87935  MGI:87936  MP:0005333 decreased heart rate PMID: 12068299 
Adra2atm1Bkk|Adra2btm1Gsb|Adra2ctm1Gsb Adra2atm1Bkk/Adra2atm1Bkk,Adra2btm1Gsb/Adra2btm1Gsb,Adra2ctm1Gsb/Adra2ctm1Gsb
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * DBA/2J		 MGI:87934  MGI:87935  MGI:87936  MP:0006207 embryonic lethality during organogenesis PMID: 12068299 
Adra2ctm1Gsb Adra2ctm1Gsb/Adra2ctm1Gsb
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * DBA/2J		 MGI:87936  MP:0001488 increased startle reflex PMID: 9526020 

References

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1. Auerbach SS, DrugMatrix® and ToxFX® Coordinator National Toxicology Program. National Toxicology Program: Dept of Health and Human Services. Accessed on 02/05/2014. Modified on 02/05/2014. DrugMatrix, https://ntp.niehs.nih.gov/drugmatrix/index.html

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17. Ishibashi T, Horisawa T, Tokuda K, Ishiyama T, Ogasa M, Tagashira R, Matsumoto K, Nishikawa H, Ueda Y, Toma S et al.. (2010) Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther, 334 (1): 171-81. [PMID:20404009]

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21. Kurko D, Kapui Z, Nagy J, Lendvai B, Kolok S. (2014) Analysis of functional selectivity through G protein-dependent and -independent signaling pathways at the adrenergic α(2C) receptor. Brain Res Bull, 107: 89-101. [PMID:25080296]

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24. Link RE, Desai K, Hein L, Stevens ME, Chruscinski A, Bernstein D, Barsh GS, Kobilka BK. (1996) Cardiovascular regulation in mice lacking alpha2-adrenergic receptor subtypes b and c. Science, 273 (5276): 803-5. [PMID:8670422]

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26. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A. (2002) Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther, 303 (2): 791-804. [PMID:12388666]

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30. Pihlavisto M, Sjöholm B, Scheinin M, Wurster S. (1998) Modulation of agonist binding to recombinant human alpha2-adrenoceptors by sodium ions. Biochim Biophys Acta, 1448 (1): 135-46. [PMID:9824686]

31. Piletz JE, Zhu H, Chikkala DN. (1996) Comparison of ligand binding affinities at human I1-imidazoline binding sites and the high affinity state of alpha-2 adrenoceptor subtypes. J Pharmacol Exp Ther, 279 (2): 694-702. [PMID:8930173]

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