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{{Short description|Protein-coding gene in the species Homo sapiens}}
{{PBB|geneid=148}}
{{cs1 config|name-list-style=vanc}}
⚫
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=10.1159/000052227}}</ref> is an [[alpha-1 adrenergic receptor]], and also denotes the human [[gene]] encoding it.<ref name="entrez" />
{{Infobox_gene}}
⚫
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 |pages=2–6 |year=1998 |issue=Suppl 2 |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.


==Receptor==
==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]].
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==
==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.<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>
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}}</ref>


==Ligands==
==Ligands==


===Agonists===
===Agonists===
* 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 |author=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>
* 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 }}</ref>
* further partial agonistic imidazole compounds<ref name="pmid19394220">{{cite journal |author=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 |author=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>
* 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 }}</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 }}</ref>
* A-61603<ref name="pmid7616455">{{cite journal | author = 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>
* 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 }}</ref>
* [[Metaraminol]]


===Antagonists===
===Antagonists===
* [[Tamsulosin]]: for treatment of [[benign prostatic hyperplasia]]
* [[Tamsulosin]]: for treatment of [[benign prostatic hyperplasia]]
* [[Silodosin]]: for treatment of [[benign prostatic hyperplasia]]
* [[Silodosin]]: for treatment of [[benign prostatic hyperplasia]]
* [[Doxazosin]]: for treatment of [[benign prostatic hyperplasia]] and/or [[Hypertension]]
* [[Risperidone]]: used to treat [[schizophrenia]] and [[bipolar disorder]]
* [[WB-4101]]
* [[Ziprasidone]]
*[[Nicergoline]]
* Most [[Tricyclic antidepressant|tricyclic antidepressants]]

== Role in neural circuits ==
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==
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==External links==
==External links==
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2175 | title = &alpha;<sub>1A</sub>-adrenoceptor | accessdate = | author = | authorlink = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2175 | title = α<sub>1A</sub>-adrenoceptor | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | access-date = 2008-11-25 | archive-date = 2020-11-22 | archive-url = https://web.archive.org/web/20201122072016/https://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2175 | url-status = dead }}
* {{UCSC gene info|ADRA1A}}


==Further reading==
==Further reading==
{{refbegin | 2}}
{{refbegin | 2}}
*{{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=10.1002/(SICI)1098-1128(199711)17:6<523::AID-MED2>3.0.CO;2-3 }}
*{{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 |s2cid=71177193 |doi-access=free }}
*{{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=10.1093/hmg/1.5.349-a }}
*{{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=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=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 |doi=10.1016/S0021-9258(19)39055-6 |pmid= 1970822 |display-authors=etal|doi-access=free }}
*{{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=10.1016/0014-5793(95)00330-C }}
*{{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 |s2cid=21462256 |display-authors=etal|doi-access=free }}
*{{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= 10.1016/0922-4106(94)90064-7}}
*{{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=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=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 |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=10.1006/bbrc.1994.1845 }}
*{{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=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=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 |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=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=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= | pmc=1908895 }}
*{{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=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= | pmc=1909672 }}
*{{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=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=10.1016/S0014-5793(98)00024-6 }}
*{{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 |s2cid=46173714 |display-authors=etal|doi-access=free }}
*{{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=10.1016/S0014-2999(99)00154-5 }}
*{{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=Cogé F, Guenin SP, Renouard-Try A, ''et al.'' |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 }}
*{{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=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=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|doi-access=free }}
*{{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=10.1074/jbc.275.7.4803 }}
*{{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|doi-access=free }}
*{{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=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=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 | 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|doi-access=free }}
*{{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 }}
*{{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|doi-access=free }}
{{refend}}
{{refend}}


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[[Category:Adrenergic receptors]]
[[Category:Adrenergic receptors]]

{{transmembranereceptor-stub}}

Latest revision as of 10:20, 23 June 2024

ADRA1A
Identifiers
AliasesADRA1A, ADRA1C, ADRA1L1, ALPHA1AAR, adrenoceptor alpha 1A
External IDsOMIM: 104221; MGI: 104773; HomoloGene: 68078; GeneCards: ADRA1A; OMA:ADRA1A - orthologs
Orthologs
SpeciesHumanMouse
Entrez

148

11549

Ensembl

ENSG00000120907

ENSMUSG00000045875

UniProt

P35348

P97718

RefSeq (mRNA)

NM_001271759
NM_001271760
NM_001271761
NM_013461

RefSeq (protein)

NP_001258688
NP_001258689
NP_001258690
NP_038489

Location (UCSC)Chr 8: 26.75 – 26.87 MbChr 14: 66.87 – 67.01 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic receptor,[5] is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.[6] 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

[edit]

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

[edit]

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.[6]

Ligands

[edit]

Agonists

[edit]
  • 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[7]
  • further partial agonistic imidazole compounds[8][9]
  • A-61603[10]
  • Metaraminol

Antagonists

[edit]

Role in neural circuits

[edit]

α1A-adrenergic receptor subtypes increase inhibition at dendrodendritic synapses, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors.[11]

See also

[edit]

References

[edit]
  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000120907 – Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000045875 – Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ 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.
  6. ^ a b "Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor".
  7. ^ 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.
  8. ^ 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.
  9. ^ 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.
  10. ^ 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.
  11. ^ 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.
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Further reading

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