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Alpha-2A adrenergic receptor
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<h2 id="receptor">Receptor</h2> <p>α2-adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating <a href="/facts/Neurotransmitter/LlpYFSU3">neurotransmitter</a> release from <a href="/facts/Sympathetic_nerves/hs8psNRd">sympathetic nerves</a> and from adrenergic neurons in the <a href="/facts/Central_nervous_system/k8I6To97">central nervous system</a>. Studies in mice revealed that both the α2A and α2C subtypes were required for normal <a href="/facts/Presynaptic/vdMRJCUn">presynaptic</a> control of transmitter release from sympathetic nerves in the <a href="/facts/Heart/fF4KSGdk">heart</a> and from central noradrenergic neurons; the α2A subtype inhibited transmitter release at high stimulation frequencies, whereas the α2C subtype modulated neurotransmission at lower levels of nerve activity.<a class="footnote-ref" id="fnref:2" href="#fn:2"><sup>2</sup></a> </p> <h2 id="gene">Gene</h2> <p>This gene encodes α2A subtype and it contains no <a href="/facts/Introns/LS6YdBEK">introns</a> in either its <a href="/facts/Coding_sequence/eSR9aIKr">coding</a> or <a href="/facts/Untranslated_sequence/aXqyV5so">untranslated sequences</a>.<a class="footnote-ref" id="fnref:3" href="#fn:3"><sup>3</sup></a> </p> <h2 id="ligands">Ligands</h2> <h3>Agonists</h3> <ul><li><a href="/facts/4-NEMD/wSt8fgfA">4-NEMD</a></li> <li><a href="/facts/Brimonidine/oYXMh7SE">Brimonidine</a></li> <li><a href="/facts/Clonidine/xPebaeST">Clonidine</a></li> <li><a href="/facts/Detomidine/IlUbucLs">Detomidine</a></li> <li><a href="/facts/Dexmedetomidine/PfMrGLg6">Dexmedetomidine</a></li> <li><a href="/facts/Guanfacine/kXNP14wn">Guanfacine</a></li> <li><a href="/facts/Lofexidine/xnheAUfm">Lofexidine</a></li> <li><a href="/facts/Myrcene/Y2tR3rlN">Myrcene</a></li> <li><a href="/facts/Medetomidine/ckuE7jNg">Medetomidine</a></li> <li><a href="/facts/PS75/SHgW7rW7">PS75</a><a class="footnote-ref" id="fnref:4" href="#fn:4"><sup>4</sup></a></li> <li><a href="/facts/Tizanidine/2ny5FuRt">Tizanidine</a></li> <li><a href="/facts/Xylazine/3fkrmSN6">Xylazine</a></li></ul> <h3>Antagonists</h3> <ul><li><a href="/facts/Atipamezole/HBaJIG51">Atipamezole</a></li> <li><a href="/facts/Idazoxan/KfJywqDw">Idazoxan</a></li> <li><a href="/facts/1-PP/ESeRVRIB">1-PP</a> (active metabolite of <a href="/facts/Buspirone/IeoGp3eD">buspirone</a> and <a href="/facts/Gepirone/90mSpkwt">gepirone</a>)</li> <li><a href="/facts/Asenapine/QqBmPoyK">Asenapine</a></li> <li><a href="/facts/BRL-44408/J05I28x5">BRL-44408</a></li> <li><a href="/facts/Clozapine/N0Lqztg1">Clozapine</a></li> <li><a href="/facts/Lurasidone/DddawwKj">Lurasidone</a></li> <li><a href="/facts/Mianserin/pV7Q1lnL">Mianserin</a></li> <li><a href="/facts/Mirtazapine/VyxPQttv">Mirtazapine</a></li> <li><a href="/facts/Paliperidone/LkFLSe4v">Paliperidone</a></li> <li><a href="/facts/Risperidone/xpFEYzoF">Risperidone</a></li> <li><a href="/facts/Yohimbine/5HcoTsKu">Yohimbine</a></li></ul> <h2 id="see-also">See also</h2> <ul><li><a href="/facts/Adrenergic_receptor/uoAeJbcN">Adrenergic receptor</a></li></ul> <h2 id="further-reading">Further reading</h2> <ul><li>Perälä M, Hirvonen H, Kalimo H, Ala-Uotila S, Regan JW, Akerman KE, et al. (November 1992). "Differential expression of two alpha 2-adrenergic receptor subtype mRNAs in human tissues". <i>Brain Research. Molecular Brain Research</i>. 16 (1–2): 57–63. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1016%2F0169-328X%2892%2990193-F">10.1016/0169-328X(92)90193-F</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/1334200">1334200</a>.</li> <li>Surprenant A, Horstman DA, Akbarali H, Limbird LE (August 1992). "A point mutation of the alpha 2-adrenoceptor that blocks coupling to potassium but not calcium currents". <i>Science</i>. 257 (5072): 977–980. <a href="/facts/Bibcode_(identifier)/9HtdQSGB">Bibcode</a>:<a href="https://ui.adsabs.harvard.edu/abs/1992Sci...257..977S">1992Sci...257..977S</a>. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1126%2Fscience.1354394">10.1126/science.1354394</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/1354394">1354394</a>.</li> <li>Handy DE, Gavras H (November 1992). <a href="https://doi.org/10.1016%2FS0021-9258%2818%2935938-6">"Promoter region of the human alpha 2A adrenergic receptor gene"</a>. <i>The Journal of Biological Chemistry</i>. 267 (33): 24017–24022. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1016%2FS0021-9258%2818%2935938-6">10.1016/S0021-9258(18)35938-6</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/1385431">1385431</a>.</li> <li>Suryanarayana S, Daunt DA, Von Zastrow M, Kobilka BK (August 1991). <a href="https://doi.org/10.1016%2FS0021-9258%2818%2998642-4">"A point mutation in the seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists"</a>. <i>The Journal of Biological Chemistry</i>. 266 (23): 15488–15492. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1016%2FS0021-9258%2818%2998642-4">10.1016/S0021-9258(18)98642-4</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/1678390">1678390</a>.</li> <li>Wang CD, Buck MA, Fraser CM (August 1991). "Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists". <i>Molecular Pharmacology</i>. 40 (2): 168–179. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/1678850">1678850</a>.</li> <li>Chhajlani V, Rangel N, Uhlén S, Wikberg JE (March 1991). <a href="https://doi.org/10.1016%2F0014-5793%2891%2980301-I">"Identification of an additional gene belonging to the alpha 2 adrenergic receptor family in the human genome by PCR"</a>. <i>FEBS Letters</i>. 280 (2): 241–244. <a href="/facts/Bibcode_(identifier)/9HtdQSGB">Bibcode</a>:<a href="https://ui.adsabs.harvard.edu/abs/1991FEBSL.280..241C">1991FEBSL.280..241C</a>. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1016%2F0014-5793%2891%2980301-I">10.1016/0014-5793(91)80301-I</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/1849485">1849485</a>. <a href="/facts/S2CID_(identifier)/ldJsHa2Y">S2CID</a> <a href="https://api.semanticscholar.org/CorpusID:26642747">26642747</a>.</li> <li>Guyer CA, Horstman DA, Wilson AL, Clark JD, Cragoe EJ, Limbird LE (October 1990). <a href="https://doi.org/10.1016%2FS0021-9258%2817%2944904-0">"Cloning, sequencing, and expression of the gene encoding the porcine alpha 2-adrenergic receptor. Allosteric modulation by Na+, H+, and amiloride analogs"</a>. <i>The Journal of Biological Chemistry</i>. 265 (28): 17307–17317. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1016%2FS0021-9258%2817%2944904-0">10.1016/S0021-9258(17)44904-0</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/2170371">2170371</a>.</li> <li>Fraser CM, Arakawa S, McCombie WR, Venter JC (July 1989). <a href="https://doi.org/10.1016%2FS0021-9258%2818%2980130-2">"Cloning, sequence analysis, and permanent expression of a human alpha 2-adrenergic receptor in Chinese hamster ovary cells. Evidence for independent pathways of receptor coupling to adenylate cyclase attenuation and activation"</a>. <i>The Journal of Biological Chemistry</i>. 264 (20): 11754–11761. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1016%2FS0021-9258%2818%2980130-2">10.1016/S0021-9258(18)80130-2</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/2568356">2568356</a>.</li> <li>Kobilka BK, Matsui H, Kobilka TS, Yang-Feng TL, Francke U, Caron MG, et al. (October 1987). "Cloning, sequencing, and expression of the gene coding for the human platelet alpha 2-adrenergic receptor". <i>Science</i>. 238 (4827): 650–656. <a href="/facts/Bibcode_(identifier)/9HtdQSGB">Bibcode</a>:<a href="https://ui.adsabs.harvard.edu/abs/1987Sci...238..650K">1987Sci...238..650K</a>. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1126%2Fscience.2823383">10.1126/science.2823383</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/2823383">2823383</a>.</li> <li>Lynch CJ, Steer ML (April 1981). <a href="https://doi.org/10.1016%2FS0021-9258%2819%2969606-7">"Evidence for high and low affinity alpha 2-receptors. Comparison of [3H]norepinephrine and [3H]phentolamine binding to human platelet membranes"</a>. <i>The Journal of Biological Chemistry</i>. 256 (7): 3298–3303. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1016%2FS0021-9258%2819%2969606-7">10.1016/S0021-9258(19)69606-7</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/6259160">6259160</a>.</li> <li>Eason MG, Moreira SP, Liggett SB (March 1995). <a href="https://doi.org/10.1074%2Fjbc.270.9.4681">"Four consecutive serines in the third intracellular loop are the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor"</a>. <i>The Journal of Biological Chemistry</i>. 270 (9): 4681–4688. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1074%2Fjbc.270.9.4681">10.1074/jbc.270.9.4681</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/7876239">7876239</a>.</li> <li>Grassie MA, Milligan G (March 1995). <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1136549">"Analysis of the relative interactions between the alpha 2C10 adrenoceptor and the guanine-nucleotide-binding proteins G(o)1 alpha and Gi 2 alpha following co-expression of these polypeptides in rat 1 fibroblasts"</a>. <i>The Biochemical Journal</i>. 306 ( Pt 2) (Pt 2): 525–530. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1042%2Fbj3060525">10.1042/bj3060525</a>. <a href="/facts/PMC_(identifier)/dX1zMt71">PMC</a> <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1136549">1136549</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/7887906">7887906</a>.</li> <li>Shilo L, Sakaue M, Thomas JM, Philip M, Hoffman BB (January 1994). "Enhanced transcription of the human alpha 2A-adrenergic receptor gene by cAMP: evidence for multiple cAMP responsive sequences in the promoter region of this gene". <i>Cellular Signalling</i>. 6 (1): 73–82. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1016%2F0898-6568%2894%2990062-0">10.1016/0898-6568(94)90062-0</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/8011430">8011430</a>.</li> <li>Valet P, Senard JM, Devedjian JC, Planat V, Salomon R, Voisin T, et al. (May 1993). <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC288203">"Characterization and distribution of alpha 2-adrenergic receptors in the human intestinal mucosa"</a>. <i>The Journal of Clinical Investigation</i>. 91 (5): 2049–2057. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1172%2FJCI116427">10.1172/JCI116427</a>. <a href="/facts/PMC_(identifier)/dX1zMt71">PMC</a> <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC288203">288203</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/8098045">8098045</a>.</li> <li>Alblas J, van Corven EJ, Hordijk PL, Milligan G, Moolenaar WH (October 1993). <a href="https://doi.org/10.1016%2FS0021-9258%2818%2941514-1">"Gi-mediated activation of the p21ras-mitogen-activated protein kinase pathway by alpha 2-adrenergic receptors expressed in fibroblasts"</a>. <i>The Journal of Biological Chemistry</i>. 268 (30): 22235–22238. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1016%2FS0021-9258%2818%2941514-1">10.1016/S0021-9258(18)41514-1</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/8226727">8226727</a>.</li> <li>Klein U, Ramirez MT, Kobilka BK, von Zastrow M (August 1997). <a href="https://doi.org/10.1074%2Fjbc.272.31.19099">"A novel interaction between adrenergic receptors and the alpha-subunit of eukaryotic initiation factor 2B"</a>. <i>The Journal of Biological Chemistry</i>. 272 (31): 19099–19102. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1074%2Fjbc.272.31.19099">10.1074/jbc.272.31.19099</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/9235896">9235896</a>.</li> <li>Bétuing S, Daviaud D, Pagès C, Bonnard E, Valet P, Lafontan M, et al. (June 1998). <a href="https://doi.org/10.1074%2Fjbc.273.25.15804">"Gbeta gamma-independent coupling of alpha2-adrenergic receptor to p21(rhoA) in preadipocytes"</a>. <i>The Journal of Biological Chemistry</i>. 273 (25): 15804–15810. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1074%2Fjbc.273.25.15804">10.1074/jbc.273.25.15804</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/9624180">9624180</a>.</li> <li>Prezeau L, Richman JG, Edwards SW, Limbird LE (May 1999). <a href="https://doi.org/10.1074%2Fjbc.274.19.13462">"The zeta isoform of 14-3-3 proteins interacts with the third intracellular loop of different alpha2-adrenergic receptor subtypes"</a>. <i>The Journal of Biological Chemistry</i>. 274 (19): 13462–13469. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1074%2Fjbc.274.19.13462">10.1074/jbc.274.19.13462</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/10224112">10224112</a>.</li> <li>Hein L, Altman JD, Kobilka BK (November 1999). "Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission". <i>Nature</i>. 402 (6758): 181–184. <a href="/facts/Bibcode_(identifier)/9HtdQSGB">Bibcode</a>:<a href="https://ui.adsabs.harvard.edu/abs/1999Natur.402..181H">1999Natur.402..181H</a>. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1038%2F46040">10.1038/46040</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/10647009">10647009</a>. <a href="/facts/S2CID_(identifier)/ldJsHa2Y">S2CID</a> <a href="https://api.semanticscholar.org/CorpusID:205047992">205047992</a>.</li> <li>Schaak S, Cussac D, Cayla C, Devedjian JC, Guyot R, Paris H, et al. (August 2000). <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1728001">"Alpha(2) adrenoceptors regulate proliferation of human intestinal epithelial cells"</a>. <i>Gut</i>. 47 (2): 242–250. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1136%2Fgut.47.2.242">10.1136/gut.47.2.242</a>. <a href="/facts/PMC_(identifier)/dX1zMt71">PMC</a> <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1728001">1728001</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/10896916">10896916</a>.</li></ul> <h2 id="external-links">External links</h2> <ul><li><a href="https://web.archive.org/web/20150402142451/http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2181">"α2A-adrenoceptor"</a>. <i>IUPHAR Database of Receptors and Ion Channels</i>. International Union of Basic and Clinical Pharmacology. Archived from <a href="http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2181">the original</a> on 2015-04-02. Retrieved 2008-11-25.</li> <li>Human <a href="https://genome.ucsc.edu/cgi-bin/hgTracks?db=hg38&singleSearch=knownCanonical&position=ADRA2A"><i>ADRA2A</i></a> genome location and <a href="https://genome.ucsc.edu/cgi-bin/hgGene?db=hg38&hgg_type=knownGene&hgg_gene=ADRA2A"><i>ADRA2A</i></a> gene details page in the <a href="/facts/UCSC_Genome_Browser/kwumPyLb">UCSC Genome Browser</a>.</li> <li>Human <a href="https://genome.ucsc.edu/cgi-bin/hgTracks?db=hg38&singleSearch=knownCanonical&position=ZNF32"><i>ZNF32</i></a> genome location and <a href="https://genome.ucsc.edu/cgi-bin/hgGene?db=hg38&hgg_type=knownGene&hgg_gene=ZNF32"><i>ZNF32</i></a> gene details page in the <a href="/facts/UCSC_Genome_Browser/kwumPyLb">UCSC Genome Browser</a>.</li></ul> <h2 id="references">References</h2> <ol> <li id="fn:1"><p>"Entrez Gene: ADRA2A adrenergic, alpha-2A-, receptor". <a href="https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=150" target="_blank">https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=150</a> <a href="#fnref:1" class="footnote-back-ref">↩</a></p></li> <li id="fn:2"><p>Hein L, Altman JD, Kobilka BK (November 1999). "Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission". Nature. 402 (6758): 181–184. Bibcode:1999Natur.402..181H. doi:10.1038/46040. PMID 10647009. S2CID 205047992. <a href="/wiki/Bibcode_(identifier)" target="_blank">/wiki/Bibcode_(identifier)</a> <a href="#fnref:2" class="footnote-back-ref">↩</a></p></li> <li id="fn:3"><p>"Entrez Gene: ADRA2A adrenergic, alpha-2A-, receptor". <a href="https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=150" target="_blank">https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=150</a> <a href="#fnref:3" class="footnote-back-ref">↩</a></p></li> <li id="fn:4"><p>Fink EA, Xu J, Hübner H, Braz JM, Seemann P, Avet C, et al. (September 2022). "Structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor". Science. 377 (6614): eabn7065. doi:10.1126/science.abn7065. PMC 10360211. PMID 36173843. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10360211" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10360211</a> <a href="#fnref:4" class="footnote-back-ref">↩</a></p></li> </ol>