Alpha-1A adrenergic 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.

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.{{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}}

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

• Tamsulosin: 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 antidepressants

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

• Adrenergic receptor

{{reflist}}

• {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2175 | title = α_1A-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}}

{{refbegin | 2}}

• {{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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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}}

{{G protein-coupled receptors}}

Category:Adrenergic receptors