Alpha-1A adrenergic receptor: Difference between revisions

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{{Infobox_gene}}
{{PBB_Controls
The '''alpha-1A adrenergic receptor''' (α<sub>1A</sub> adrenoreceptor), also known as '''ADRA1A''', formerly known also as the  '''alpha-1C adrenergic receptor''',<ref>{{cite journal |author =Langer SZ |title=Nomenclature and state of the art on alpha1-adrenoceptors |journal=Eur. Urol. |volume=33 Suppl 2 |issue= |pages=2–6 |year=1998 |pmid=9556189 |doi=10.1159/000052227}}</ref> is an [[alpha-1 adrenergic receptor]], and also denotes the human [[gene]] encoding it.<ref name="entrez" /> There is no longer a subtype α<sub>1C</sub> receptor. At one time, there was a subtype known as α<sub>1C</sub>, but it was found to be identical to the previously discovered α<sub>1A</sub> receptor subtype. To avoid confusion, the naming convention was continued with the letter D.
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<!-- The GNF_Protein_box is automatically maintained by Protein Box Bot.  See Template:PBB_Controls to Stop updates. -->
==Receptor==
{{GNF_Protein_box
There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins.  Different subtypes show different patterns of activation.  The majority of alpha-1 receptors are directed toward the function of epinephrine, a hormone that has to do with the [[fight-or-flight response]].
| image =
 
| image_source =
==Gene==
| PDB =  
This gene encodes the alpha-1A-adrenergic receptor. Alternative splicing of this gene generates four transcript variants, which encode four different isoforms with distinct C-termini but having similar ligand binding properties.<ref name="entrez">{{cite web | title = Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=148| accessdate = }}</ref>
| Name = Adrenergic, alpha-1A-, receptor
| HGNCid = 277
| Symbol = ADRA1A
| AltSymbols =; ADRA1C; ADRA1L1; ALPHA1AAR
| OMIM = 104221
| ECnumber = 
| Homologene = 68078
| MGIid = 104773
| GeneAtlas_image1 = PBB_GE_ADRA1A_211492_s_at_tn.png
  | GeneAtlas_image2 = PBB_GE_ADRA1A_211490_at_tn.png
  | GeneAtlas_image3 = PBB_GE_ADRA1A_211491_at_tn.png
| Function = {{GNF_GO|id=GO:0001584 |text = rhodopsin-like receptor activity}} {{GNF_GO|id=GO:0004872 |text = receptor activity}} {{GNF_GO|id=GO:0004935 |text = adrenoceptor activity}} {{GNF_GO|id=GO:0004937 |text = alpha1-adrenergic receptor activity}}
| Component = {{GNF_GO|id=GO:0005887 |text = integral to plasma membrane}} {{GNF_GO|id=GO:0016020 |text = membrane}}
| Process = {{GNF_GO|id=GO:0006915 |text = apoptosis}} {{GNF_GO|id=GO:0006939 |text = smooth muscle contraction}} {{GNF_GO|id=GO:0007165 |text = signal transduction}} {{GNF_GO|id=GO:0007186 |text = G-protein coupled receptor protein signaling pathway}} {{GNF_GO|id=GO:0007243 |text = protein kinase cascade}} {{GNF_GO|id=GO:0007267 |text = cell-cell signaling}} {{GNF_GO|id=GO:0008285 |text = negative regulation of cell proliferation}}
| Orthologs = {{GNF_Ortholog_box
    | Hs_EntrezGene = 148
    | Hs_Ensembl = ENSG00000120907
    | Hs_RefseqProtein = NP_000671
    | Hs_RefseqmRNA = NM_000680
    | Hs_GenLoc_db = 
    | Hs_GenLoc_chr = 8
    | Hs_GenLoc_start = 26661584
    | Hs_GenLoc_end = 26778839
    | Hs_Uniprot = P35348
    | Mm_EntrezGene = 11549
    | Mm_Ensembl = ENSMUSG00000045875
    | Mm_RefseqmRNA = NM_013461
    | Mm_RefseqProtein = NP_038489
    | Mm_GenLoc_db = 
    | Mm_GenLoc_chr = 14
    | Mm_GenLoc_start = 65589368
    | Mm_GenLoc_end = 65687439
    | Mm_Uniprot = Q8BUE5
  }}
}}
The '''alpha-1A adrenergic receptor''' (α<sub>1A</sub> adrenoreceptor), also known as '''ADRA1A''', formerly known as the  '''alpha-1C adrenergic receptor'''<ref>{{cite journal |author=Langer SZ |title=Nomenclature and state of the art on alpha1-adrenoceptors |journal=Eur. Urol. |volume=33 Suppl 2 |issue= |pages=2–6 |year=1998 |pmid=9556189 |doi=}}</ref>, is an [[alpha-1 adrenergic receptor]], and also denotes the human [[gene]] encoding it.<ref name="entrez" />


<!-- The PBB_Summary template is not automatically maintained by Protein Box Bot.  See Template:PBB_Controls to continue updates. -->
==Ligands==
{{PBB_Summary
| section_title =  
| summary_text =  


==Receptor==
===Agonists===
There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation.  
* 6-(5-fluoro-2-pyrimidin-5-yl-phenyl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole: EC<sub>50</sub> = 1nM, E<sub>max</sub> = 65%; good selectivity over α1B, α1D and α2A subtypes<ref name="pmid19414260">{{cite journal |vauthors =Roberts LR, Fish PV, Ian Storer R, Whitlock GA |title=6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha(1A) adrenoceptor partial agonists |journal=Bioorg. Med. Chem. Lett. |volume= 19|issue= 11|pages= 3113–7|date=April 2009 |pmid=19414260 |doi=10.1016/j.bmcl.2009.03.166 |url=}}</ref>
* further partial agonistic imidazole compounds<ref name="pmid19394220">{{cite journal |vauthors =Whitlock GA, Brennan PE, Roberts LR, Stobie A |title=Potent and selective alpha(1A) adrenoceptor partial agonists-Novel imidazole frameworks |journal=Bioorg. Med. Chem. Lett. |volume= 19|issue= 11|pages= 3118–21|date=April 2009 |pmid=19394220 |doi=10.1016/j.bmcl.2009.03.162 |url=}}</ref><ref name="pmid18980842">{{cite journal |vauthors =Roberts LR, Bryans J, Conlon K, McMurray G, Stobie A, Whitlock GA |title=Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists |journal=Bioorg. Med. Chem. Lett. |volume=18 |issue=24 |pages=6437–40 |date=December 2008 |pmid=18980842 |doi=10.1016/j.bmcl.2008.10.066 |url=}}</ref>
* A-61603<ref name="pmid7616455">{{cite journal | vauthors = Knepper SM, Buckner SA, Brune ME, DeBernardis JF, Meyer MD, Hancock AA | title = A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype | journal = J. Pharmacol. Exp. Ther. | volume = 274 | issue = 1 | pages = 97–103 | year = 1995 | pmid = 7616455 | doi =  }}</ref>


==Gene==
===Antagonists===
This gene encodes the alpha-1A-adrenergic receptor. Alternative splicing of this gene generates four transcript variants, which encode four different isoforms with distinct C-termini but having similar ligand binding properties.<ref name="entrez">{{cite web | title = Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=148| accessdate = }}</ref>
* [[Tamsulosin]]: for treatment of [[benign prostatic hyperplasia]]
}}
* [[Silodosin]]: for treatment of [[benign prostatic hyperplasia]]
* [[Risperidone]]
* [[WB-4101]]
* [[Ziprasidone]]


==Antagonists==
== Role in neural circuits ==
[[Alpha-blockers]] specific for 1A include [[tamsulosin]] (in [[benign prostatic hyperplasia]].
α1A-adrenergic receptor subtypes increase inhibition at dendrodendritic synapses, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors.<ref name="pmid23266935">{{cite journal | vauthors = Zimnik NC, Treadway T, Smith RS, Araneda RC | title = α(1A)-Adrenergic regulation of inhibition in the olfactory bulb | journal = J. Physiol. | volume = 591 | issue = Pt 7 | pages = 1631–43 | year = 2013 | pmid = 23266935 | pmc = 3624843 | doi = 10.1113/jphysiol.2012.248591 }}</ref>


==See also==
==See also==
Line 69: Line 29:


==References==
==References==
{{reflist|2}}
{{reflist}}
 
==External links==
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2175 | title = &alpha;<sub>1A</sub>-adrenoceptor  | accessdate = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}
* {{UCSC gene info|ADRA1A}}


==Further reading==
==Further reading==
{{refbegin | 2}}
{{refbegin | 2}}
{{PBB_Further_reading
*{{cite journal  | vauthors=Mátyus P, Horváth K |title=Alpha-adrenergic approach in the medical management of benign prostatic hyperplasia |journal=Med Res Rev |volume=17 |issue= 6 |pages= 523–35 |year= 1998 |pmid= 9359081 |doi=10.1002/(SICI)1098-1128(199711)17:6<523::AID-MED2>3.0.CO;2-3  }}
| citations =
*{{cite journal | vauthors=Hoehe MR, Berrettini WH, Schwinn DA, Hsieh WT |title=A two-allele PstI RFLP for the alpha-1C adrenergic receptor gene (ADRA1C) |journal=Hum. Mol. Genet. |volume=1 |issue= 5 |pages= 349 |year= 1993 |pmid= 1363873 |doi=10.1093/hmg/1.5.349-a  }}
*{{cite journal  | author=Mátyus P, Horváth K |title=Alpha-adrenergic approach in the medical management of benign prostatic hyperplasia. |journal=Med Res Rev |volume=17 |issue= 6 |pages= 523-35 |year= 1998 |pmid= 9359081 |doi=  }}
*{{cite journal  | vauthors=Schwinn DA, Lomasney JW, Lorenz W |title=Molecular cloning and expression of the cDNA for a novel alpha 1-adrenergic receptor subtype |journal=J. Biol. Chem. |volume=265 |issue= 14 |pages= 8183–9 |year= 1990 |pmid= 1970822 |doi=  |display-authors=etal}}
*{{cite journal  | author=Hoehe MR, Berrettini WH, Schwinn DA, Hsieh WT |title=A two-allele PstI RFLP for the alpha-1C adrenergic receptor gene (ADRA1C). |journal=Hum. Mol. Genet. |volume=1 |issue= 5 |pages= 349 |year= 1993 |pmid= 1363873 |doi= }}
*{{cite journal  | vauthors=Hirasawa A, Shibata K, Horie K |title=Cloning, functional expression and tissue distribution of human alpha 1c-adrenoceptor splice variants |journal=FEBS Lett. |volume=363 |issue= 3 |pages= 256–60 |year= 1995 |pmid= 7737411 |doi=10.1016/0014-5793(95)00330-C  |display-authors=etal}}
*{{cite journal  | author=Schwinn DA, Lomasney JW, Lorenz W, ''et al.'' |title=Molecular cloning and expression of the cDNA for a novel alpha 1-adrenergic receptor subtype. |journal=J. Biol. Chem. |volume=265 |issue= 14 |pages= 8183-9 |year= 1990 |pmid= 1970822 |doi=  }}
*{{cite journal  | vauthors=Diehl NL, Shreeve SM |title=Identification of the alpha 1c-adrenoceptor in rabbit arteries and the human saphenous vein using the polymerase chain reaction |journal=Eur. J. Pharmacol. |volume=268 |issue= 3 |pages= 393–8 |year= 1995 |pmid= 7805763 |doi=  10.1016/0922-4106(94)90064-7}}
*{{cite journal  | author=Hirasawa A, Shibata K, Horie K, ''et al.'' |title=Cloning, functional expression and tissue distribution of human alpha 1c-adrenoceptor splice variants. |journal=FEBS Lett. |volume=363 |issue= 3 |pages= 256-60 |year= 1995 |pmid= 7737411 |doi= }}
*{{cite journal  | vauthors=Schwinn DA, Johnston GI, Page SO |title=Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues |journal=J. Pharmacol. Exp. Ther. |volume=272 |issue= 1 |pages= 134–42 |year= 1995 |pmid= 7815325 |doi=  |display-authors=etal}}
*{{cite journal  | author=Diehl NL, Shreeve SM |title=Identification of the alpha 1c-adrenoceptor in rabbit arteries and the human saphenous vein using the polymerase chain reaction. |journal=Eur. J. Pharmacol. |volume=268 |issue= 3 |pages= 393-8 |year= 1995 |pmid= 7805763 |doi=  }}
*{{cite journal  | vauthors=Weinberg DH, Trivedi P, Tan CP |title=Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c |journal=Biochem. Biophys. Res. Commun. |volume=201 |issue= 3 |pages= 1296–304 |year= 1994 |pmid= 8024574 |doi=10.1006/bbrc.1994.1845 |display-authors=etal}}
*{{cite journal  | author=Schwinn DA, Johnston GI, Page SO, ''et al.'' |title=Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. |journal=J. Pharmacol. Exp. Ther. |volume=272 |issue= 1 |pages= 134-42 |year= 1995 |pmid= 7815325 |doi=  }}
*{{cite journal  | vauthors=Forray C, Bard JA, Wetzel JM |title=The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype |journal=Mol. Pharmacol. |volume=45 |issue= 4 |pages= 703–8 |year= 1994 |pmid= 8183249 |doi=  |display-authors=etal}}
*{{cite journal  | author=Weinberg DH, Trivedi P, Tan CP, ''et al.'' |title=Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c. |journal=Biochem. Biophys. Res. Commun. |volume=201 |issue= 3 |pages= 1296-304 |year= 1994 |pmid= 8024574 |doi=  }}
*{{cite journal  | vauthors=Hirasawa A, Horie K, Tanaka T |title=Cloning, functional expression and tissue distribution of human cDNA for the alpha 1C-adrenergic receptor |journal=Biochem. Biophys. Res. Commun. |volume=195 |issue= 2 |pages= 902–9 |year= 1993 |pmid= 8396931 |doi= 10.1006/bbrc.1993.2130 |display-authors=etal}}
*{{cite journal  | author=Forray C, Bard JA, Wetzel JM, ''et al.'' |title=The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. |journal=Mol. Pharmacol. |volume=45 |issue= 4 |pages= 703-8 |year= 1994 |pmid= 8183249 |doi=  }}
*{{cite journal  | vauthors=Tseng-Crank J, Kost T, Goetz A |title=The alpha 1C-adrenoceptor in human prostate: cloning, functional expression, and localization to specific prostatic cell types |journal=Br. J. Pharmacol. |volume=115 |issue= 8 |pages= 1475–85 |year= 1996 |pmid= 8564208 |doi=  10.1111/j.1476-5381.1995.tb16640.x| pmc=1908895  |display-authors=etal}}
*{{cite journal  | author=Hirasawa A, Horie K, Tanaka T, ''et al.'' |title=Cloning, functional expression and tissue distribution of human cDNA for the alpha 1C-adrenergic receptor. |journal=Biochem. Biophys. Res. Commun. |volume=195 |issue= 2 |pages= 902-9 |year= 1993 |pmid= 8396931 |doi= 10.1006/bbrc.1993.2130 }}
*{{cite journal  | vauthors=Shibata K, Hirasawa A, Moriyama N |title=Alpha 1a-adrenoceptor polymorphism: pharmacological characterization and association with benign prostatic hypertrophy |journal=Br. J. Pharmacol. |volume=118 |issue= 6 |pages= 1403–8 |year= 1997 |pmid= 8832064 |doi=  10.1111/j.1476-5381.1996.tb15552.x| pmc=1909672  |display-authors=etal}}
*{{cite journal  | author=Tseng-Crank J, Kost T, Goetz A, ''et al.'' |title=The alpha 1C-adrenoceptor in human prostate: cloning, functional expression, and localization to specific prostatic cell types. |journal=Br. J. Pharmacol. |volume=115 |issue= 8 |pages= 1475-85 |year= 1996 |pmid= 8564208 |doi=  }}
*{{cite journal  | vauthors=Chang DJ, Chang TK, Yamanishi SS |title=Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms |journal=FEBS Lett. |volume=422 |issue= 2 |pages= 279–83 |year= 1998 |pmid= 9490024 |doi=10.1016/S0014-5793(98)00024-6  |display-authors=etal}}
*{{cite journal  | author=Shibata K, Hirasawa A, Moriyama N, ''et al.'' |title=Alpha 1a-adrenoceptor polymorphism: pharmacological characterization and association with benign prostatic hypertrophy. |journal=Br. J. Pharmacol. |volume=118 |issue= 6 |pages= 1403-8 |year= 1997 |pmid= 8832064 |doi=  }}
*{{cite journal  | vauthors=Daniels DV, Gever JR, Jasper JR |title=Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies |journal=Eur. J. Pharmacol. |volume=370 |issue= 3 |pages= 337–43 |year= 1999 |pmid= 10334511 |doi=10.1016/S0014-2999(99)00154-5 |display-authors=etal}}
*{{cite journal  | author=Chang DJ, Chang TK, Yamanishi SS, ''et al.'' |title=Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms. |journal=FEBS Lett. |volume=422 |issue= 2 |pages= 279-83 |year= 1998 |pmid= 9490024 |doi= }}
*{{cite journal  | vauthors=Cogé F, Guenin SP, Renouard-Try A |title=Truncated isoforms inhibit 3Hprazosin binding and cellular trafficking of native human alpha1A-adrenoceptors |journal=Biochem. J. |volume=343 Pt 1 |issue=  Pt 1|pages= 231–9 |year= 1999 |pmid= 10493934 |doi=10.1042/0264-6021:3430231  | pmc=1220546 |display-authors=etal}}
*{{cite journal  | author=Daniels DV, Gever JR, Jasper JR, ''et al.'' |title=Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies. |journal=Eur. J. Pharmacol. |volume=370 |issue= 3 |pages= 337-43 |year= 1999 |pmid= 10334511 |doi=  }}
*{{cite journal  | vauthors=Rudner XL, Berkowitz DE, Booth JV |title=Subtype specific regulation of human vascular alpha(1)-adrenergic receptors by vessel bed and age |journal=Circulation |volume=100 |issue= 23 |pages= 2336–43 |year= 1999 |pmid= 10587338 |doi=  10.1161/01.cir.100.23.2336|display-authors=etal}}
*{{cite journal  | author=Cogé F, Guenin SP, Renouard-Try A, ''et al.'' |title=Truncated isoforms inhibit [3H]prazosin binding and cellular trafficking of native human alpha1A-adrenoceptors. |journal=Biochem. J. |volume=343 Pt 1 |issue=  |pages= 231-9 |year= 1999 |pmid= 10493934 |doi=  }}
*{{cite journal  | vauthors=Ballou LM, Cross ME, Huang S |title=Differential regulation of the phosphatidylinositol 3-kinase/Akt and p70 S6 kinase pathways by the alpha(1A)-adrenergic receptor in rat-1 fibroblasts |journal=J. Biol. Chem. |volume=275 |issue= 7 |pages= 4803–9 |year= 2000 |pmid= 10671514 |doi=10.1074/jbc.275.7.4803  |display-authors=etal}}
*{{cite journal  | author=Rudner XL, Berkowitz DE, Booth JV, ''et al.'' |title=Subtype specific regulation of human vascular alpha(1)-adrenergic receptors by vessel bed and age. |journal=Circulation |volume=100 |issue= 23 |pages= 2336-43 |year= 1999 |pmid= 10587338 |doi=  }}
*{{cite journal  | vauthors=Keffel S, Alexandrov A, Goepel M, Michel MC |title=alpha(1)-adrenoceptor subtypes differentially couple to growth promotion and inhibition in Chinese hamster ovary cells |journal=Biochem. Biophys. Res. Commun. |volume=272 |issue= 3 |pages= 906–11 |year= 2000 |pmid= 10860850 |doi= 10.1006/bbrc.2000.2850 }}
*{{cite journal  | author=Ballou LM, Cross ME, Huang S, ''et al.'' |title=Differential regulation of the phosphatidylinositol 3-kinase/Akt and p70 S6 kinase pathways by the alpha(1A)-adrenergic receptor in rat-1 fibroblasts. |journal=J. Biol. Chem. |volume=275 |issue= 7 |pages= 4803-9 |year= 2000 |pmid= 10671514 |doi= }}
*{{cite journal  | vauthors=Richman JG, Brady AE, Wang Q |title=Agonist-regulated Interaction between alpha2-adrenergic receptors and spinophilin |journal=J. Biol. Chem. |volume=276 |issue= 18 |pages= 15003–8 |year= 2001 |pmid= 11154706 |doi= 10.1074/jbc.M011679200 |display-authors=etal}}
*{{cite journal  | author=Keffel S, Alexandrov A, Goepel M, Michel MC |title=alpha(1)-adrenoceptor subtypes differentially couple to growth promotion and inhibition in Chinese hamster ovary cells. |journal=Biochem. Biophys. Res. Commun. |volume=272 |issue= 3 |pages= 906-11 |year= 2000 |pmid= 10860850 |doi= 10.1006/bbrc.2000.2850 }}
*{{cite journal  | vauthors=Shibata K, Katsuma S, Koshimizu T |title=alpha 1-Adrenergic receptor subtypes differentially control the cell cycle of transfected CHO cells through a cAMP-dependent mechanism involving p27Kip1 |journal=J. Biol. Chem. |volume=278 |issue= 1 |pages= 672–8 |year= 2003 |pmid= 12409310 |doi= 10.1074/jbc.M201375200 |display-authors=etal}}
*{{cite journal  | author=Richman JG, Brady AE, Wang Q, ''et al.'' |title=Agonist-regulated Interaction between alpha2-adrenergic receptors and spinophilin. |journal=J. Biol. Chem. |volume=276 |issue= 18 |pages= 15003-8 |year= 2001 |pmid= 11154706 |doi= 10.1074/jbc.M011679200 }}
*{{cite journal  | author=Shibata K, Katsuma S, Koshimizu T, ''et al.'' |title=alpha 1-Adrenergic receptor subtypes differentially control the cell cycle of transfected CHO cells through a cAMP-dependent mechanism involving p27Kip1. |journal=J. Biol. Chem. |volume=278 |issue= 1 |pages= 672-8 |year= 2003 |pmid= 12409310 |doi= 10.1074/jbc.M201375200 }}
}}
{{refend}}
{{refend}}


{{membrane-protein-stub}}
{{G protein-coupled receptors}}
{{G protein-coupled receptors}}
[[Category:Adrenergic receptors‎]]
 
[[Category:G protein coupled receptors]]
[[Category:Adrenergic receptors]]

Latest revision as of 20:27, 29 August 2017

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Identifiers
Aliases
External IDsGeneCards: [1]
Orthologs
SpeciesHumanMouse
Entrez

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Ensembl

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UniProt

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RefSeq (mRNA)

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RefSeq (protein)

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Location (UCSC)n/an/a
PubMed searchn/an/a
Wikidata
View/Edit Human

The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic receptor,[1] is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.[2] There is no longer a subtype α1C receptor. At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. To avoid confusion, the naming convention was continued with the letter D.

Receptor

There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins. Different subtypes show different patterns of activation. The majority of alpha-1 receptors are directed toward the function of epinephrine, a hormone that has to do with the fight-or-flight response.

Gene

This gene encodes the alpha-1A-adrenergic receptor. Alternative splicing of this gene generates four transcript variants, which encode four different isoforms with distinct C-termini but having similar ligand binding properties.[2]

Ligands

Agonists

  • 6-(5-fluoro-2-pyrimidin-5-yl-phenyl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole: EC50 = 1nM, Emax = 65%; good selectivity over α1B, α1D and α2A subtypes[3]
  • further partial agonistic imidazole compounds[4][5]
  • A-61603[6]

Antagonists

Role in neural circuits

α1A-adrenergic receptor subtypes increase inhibition at dendrodendritic synapses, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors.[7]

See also

References

  1. ↑ Langer SZ (1998). "Nomenclature and state of the art on alpha1-adrenoceptors". Eur. Urol. 33 Suppl 2: 2–6. doi:10.1159/000052227. PMID 9556189.
  2. ↑ 2.0 2.1 "Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor".
  3. ↑ Roberts LR, Fish PV, Ian Storer R, Whitlock GA (April 2009). "6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha(1A) adrenoceptor partial agonists". Bioorg. Med. Chem. Lett. 19 (11): 3113–7. doi:10.1016/j.bmcl.2009.03.166. PMID 19414260.
  4. ↑ Whitlock GA, Brennan PE, Roberts LR, Stobie A (April 2009). "Potent and selective alpha(1A) adrenoceptor partial agonists-Novel imidazole frameworks". Bioorg. Med. Chem. Lett. 19 (11): 3118–21. doi:10.1016/j.bmcl.2009.03.162. PMID 19394220.
  5. ↑ Roberts LR, Bryans J, Conlon K, McMurray G, Stobie A, Whitlock GA (December 2008). "Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists". Bioorg. Med. Chem. Lett. 18 (24): 6437–40. doi:10.1016/j.bmcl.2008.10.066. PMID 18980842.
  6. ↑ Knepper SM, Buckner SA, Brune ME, DeBernardis JF, Meyer MD, Hancock AA (1995). "A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype". J. Pharmacol. Exp. Ther. 274 (1): 97–103. PMID 7616455.
  7. ↑ Zimnik NC, Treadway T, Smith RS, Araneda RC (2013). "α(1A)-Adrenergic regulation of inhibition in the olfactory bulb". J. Physiol. 591 (Pt 7): 1631–43. doi:10.1113/jphysiol.2012.248591. PMC 3624843. PMID 23266935.

External links

Further reading

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