Alpha-2A adrenergic receptor
Details
- Name
- Alpha-2A adrenergic receptor
- Synonyms
- ADRA2R
- ADRAR
- Alpha-2 adrenergic receptor subtype C10
- Alpha-2A adrenoceptor
- Alpha-2A adrenoreceptor
- Alpha-2AAR
- Gene Name
- ADRA2A
- UniProtKB Entry
- P08913Swiss-Prot
- Organism
- Humans
- NCBI Taxonomy ID
- 9606
- Amino acid sequence
>lcl|BSEQ0055723|Alpha-2A adrenergic receptor MFRQEQPLAEGSFAPMGSLQPDAGNASWNGTEAPGGGARATPYSLQVTLTLVCLAGLLML LTVFGNVLVIIAVFTSRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKAW CEIYLALDVLFCTSSIVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIITVWVISAVIS FPPLISIEKKGGGGGPQPAEPRCEINDQKWYVISSCIGSFFAPCLIMILVYVRIYQIAKR RTRVPPSRRGPDAVAAPPGGTERRPNGLGPERSAGPGGAEAEPLPTQLNGAPGEPAPAGP RDTDALDLEESSSSDHAERPPGPRRPERGPRGKGKARASQVKPGDSLPRRGPGATGIGTP AAGPGEERVGAAKASRWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLTAVGCSVPR TLFKFFFWFGYCNSSLNPVIYTIFNHDFRRAFKKILCRGDRKRIV
- Number of residues
- 465
- Molecular Weight
- 50646.17
- Theoretical pI
- 10.2
- GO Classification
- Processesadenylate cyclase-activating adrenergic receptor signaling pathway / adenylate cyclase-activating G protein-coupled receptor signaling pathway / adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway / adrenergic receptor signaling pathway / G protein-coupled receptor signaling pathway / positive regulation of cell population proliferation / positive regulation of epidermal growth factor receptor signaling pathway / positive regulation of MAPK cascade / presynaptic modulation of chemical synaptic transmission / receptor transactivation / vasodilationComponentsaxon terminus / dopaminergic synapse / GABA-ergic synapse / glutamatergic synapse / neuronal cell body / postsynaptic density membrane / presynaptic active zone membrane
- General Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol
- Specific Function
- Alpha-1b adrenergic receptor binding
- Pfam Domain Function
- 7tm_1 (PF00001)
- Signal Regions
- Not Available
- Transmembrane Regions
- 49-74 86-111 122-144 167-187 210-232 390-410 425-444
- Cellular Location
- Cell membrane
- Gene sequence
>lcl|BSEQ0021256|Alpha-2A adrenergic receptor (ADRA2A) ATGTTCCGCCAGGAGCAGCCGTTGGCCGAGGGCAGCTTTGCGCCCATGGGCTCCCTGCAG CCGGACGCGGGCAACGCGAGCTGGAACGGGACCGAGGCGCCGGGGGGCGGCGCCCGGGCC ACCCCTTACTCCCTGCAGGTGACGCTGACGCTGGTGTGCCTGGCCGGCCTGCTCATGCTG CTCACCGTGTTCGGCAACGTGCTCGTCATCATCGCCGTGTTCACGAGCCGCGCGCTCAAG GCGCCCCAAAACCTCTTCCTGGTGTCTCTGGCCTCGGCCGACATCCTGGTGGCCACGCTC GTCATCCCTTTCTCGCTGGCCAACGAGGTCATGGGCTACTGGTACTTCGGCAAGGCTTGG TGCGAGATCTACCTGGCGCTCGACGTGCTCTTCTGCACGTCGTCCATCGTGCACCTGTGC GCCATCAGCCTGGACCGCTACTGGTCCATCACACAGGCCATCGAGTACAACCTGAAGCGC ACGCCGCGCCGCATCAAGGCCATCATCATCACCGTGTGGGTCATCTCGGCCGTCATCTCC TTCCCGCCGCTCATCTCCATCGAGAAGAAGGGCGGCGGCGGCGGCCCGCAGCCGGCCGAG CCGCGCTGCGAGATCAACGACCAGAAGTGGTACGTCATCTCGTCGTGCATCGGCTCCTTC TTCGCTCCCTGCCTCATCATGATCCTGGTCTACGTGCGCATCTACCAGATCGCCAAGCGT CGCACCCGCGTGCCACCCAGCCGCCGGGGTCCGGACGCCGTCGCCGCGCCGCCGGGGGGC ACCGAGCGCAGGCCCAACGGTCTGGGCCCCGAGCGCAGCGCGGGCCCGGGGGGCGCAGAG GCCGAACCGCTGCCCACCCAGCTCAACGGCGCCCCTGGCGAGCCCGCGCCGGCCGGGCCG CGCGACACCGACGCGCTGGACCTGGAGGAGAGCTCGTCTTCCGACCACGCCGAGCGGCCT CCAGGGCCCCGCAGACCCGAGCGCGGTCCCCGGGGCAAAGGCAAGGCCCGAGCGAGCCAG GTGAAGCCGGGCGACAGCCTGCCGCGGCGCGGGCCGGGGGCGACGGGGATCGGGACGCCG GCTGCAGGGCCGGGGGAGGAGCGCGTCGGGGCTGCCAAGGCGTCGCGCTGGCGCGGGCGG CAGAACCGCGAGAAGCGCTTCACGTTCGTGCTGGCCGTGGTCATCGGAGTGTTCGTGGTG TGCTGGTTCCCCTTCTTCTTCACCTACACGCTCACGGCCGTCGGGTGCTCCGTGCCACGC ACGCTCTTCAAATTCTTCTTCTGGTTCGGCTACTGCAACAGCTCGTTGAACCCGGTCATC TACACCATCTTCAACCACGATTTCCGCCGCGCCTTCAAGAAGATCCTCTGTCGGGGGGAC AGGAAGCGGATCGTGTGA
- Chromosome Location
- 10
- Locus
- 10q25.2
- External Identifiers
Resource Link UniProtKB ID P08913 UniProtKB Entry Name ADA2A_HUMAN GenBank Protein ID 178196 GenBank Gene ID M23533 GeneCard ID ADRA2A GenAtlas ID ADRA2A HGNC ID HGNC:281 PDB ID(s) 1HLL, 1HO9, 1HOD, 1HOF, 6K42, 6KUX, 6KUY, 7EJ0, 7EJ8, 7EJA, 7EJK, 7W6P, 7W7E KEGG ID hsa:150 IUPHAR/Guide To Pharmacology ID 25 NCBI Gene ID 150 - General References
- Kobilka BK, Matsui H, Kobilka TS, Yang-Feng TL, Francke U, Caron MG, Lefkowitz RJ, Regan JW: Cloning, sequencing, and expression of the gene coding for the human platelet alpha 2-adrenergic receptor. Science. 1987 Oct 30;238(4827):650-6. [Article]
- Fraser CM, Arakawa S, McCombie WR, Venter JC: 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. J Biol Chem. 1989 Jul 15;264(20):11754-61. [Article]
- Guyer CA, Horstman DA, Wilson AL, Clark JD, Cragoe EJ Jr, Limbird LE: Cloning, sequencing, and expression of the gene encoding the porcine alpha 2-adrenergic receptor. Allosteric modulation by Na+, H+, and amiloride analogs. J Biol Chem. 1990 Oct 5;265(28):17307-17. [Article]
- Small KM, Forbes SL, Brown KM, Liggett SB: An asn to lys polymorphism in the third intracellular loop of the human alpha 2A-adrenergic receptor imparts enhanced agonist-promoted Gi coupling. J Biol Chem. 2000 Dec 8;275(49):38518-23. [Article]
- Small KM, Brown KM, Seman CA, Theiss CT, Liggett SB: Complex haplotypes derived from noncoding polymorphisms of the intronless alpha2A-adrenergic gene diversify receptor expression. Proc Natl Acad Sci U S A. 2006 Apr 4;103(14):5472-7. Epub 2006 Mar 27. [Article]
- Deloukas P, Earthrowl ME, Grafham DV, Rubenfield M, French L, Steward CA, Sims SK, Jones MC, Searle S, Scott C, Howe K, Hunt SE, Andrews TD, Gilbert JG, Swarbreck D, Ashurst JL, Taylor A, Battles J, Bird CP, Ainscough R, Almeida JP, Ashwell RI, Ambrose KD, Babbage AK, Bagguley CL, Bailey J, Banerjee R, Bates K, Beasley H, Bray-Allen S, Brown AJ, Brown JY, Burford DC, Burrill W, Burton J, Cahill P, Camire D, Carter NP, Chapman JC, Clark SY, Clarke G, Clee CM, Clegg S, Corby N, Coulson A, Dhami P, Dutta I, Dunn M, Faulkner L, Frankish A, Frankland JA, Garner P, Garnett J, Gribble S, Griffiths C, Grocock R, Gustafson E, Hammond S, Harley JL, Hart E, Heath PD, Ho TP, Hopkins B, Horne J, Howden PJ, Huckle E, Hynds C, Johnson C, Johnson D, Kana A, Kay M, Kimberley AM, Kershaw JK, Kokkinaki M, Laird GK, Lawlor S, Lee HM, Leongamornlert DA, Laird G, Lloyd C, Lloyd DM, Loveland J, Lovell J, McLaren S, McLay KE, McMurray A, Mashreghi-Mohammadi M, Matthews L, Milne S, Nickerson T, Nguyen M, Overton-Larty E, Palmer SA, Pearce AV, Peck AI, Pelan S, Phillimore B, Porter K, Rice CM, Rogosin A, Ross MT, Sarafidou T, Sehra HK, Shownkeen R, Skuce CD, Smith M, Standring L, Sycamore N, Tester J, Thorpe A, Torcasso W, Tracey A, Tromans A, Tsolas J, Wall M, Walsh J, Wang H, Weinstock K, West AP, Willey DL, Whitehead SL, Wilming L, Wray PW, Young L, Chen Y, Lovering RC, Moschonas NK, Siebert R, Fechtel K, Bentley D, Durbin R, Hubbard T, Doucette-Stamm L, Beck S, Smith DR, Rogers J: The DNA sequence and comparative analysis of human chromosome 10. Nature. 2004 May 27;429(6990):375-81. [Article]
- Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [Article]
- Chhajlani V, Rangel N, Uhlen S, Wikberg JE: Identification of an additional gene belonging to the alpha 2 adrenergic receptor family in the human genome by PCR. FEBS Lett. 1991 Mar 25;280(2):241-4. [Article]
- Suryanarayana S, Daunt DA, Von Zastrow M, Kobilka BK: A point mutation in the seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists. J Biol Chem. 1991 Aug 15;266(23):15488-92. [Article]
- Wang CD, Buck MA, Fraser CM: Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists. Mol Pharmacol. 1991 Aug;40(2):168-79. [Article]
- Li C, Fan Y, Lan TH, Lambert NA, Wu G: Rab26 modulates the cell surface transport of alpha2-adrenergic receptors from the Golgi. J Biol Chem. 2012 Dec 14;287(51):42784-94. doi: 10.1074/jbc.M112.410936. Epub 2012 Oct 26. [Article]
- Chung DA, Zuiderweg ER, Fowler CB, Soyer OS, Mosberg HI, Neubig RR: NMR structure of the second intracellular loop of the alpha 2A adrenergic receptor: evidence for a novel cytoplasmic helix. Biochemistry. 2002 Mar 19;41(11):3596-604. [Article]
Associated Data
- Bio-Entities
Bio-Entity Type Alpha-2A adrenergic receptor (Humans) protein primaryAlpha-2 adrenergic receptors (Humans) protein Alpha adrenergic receptor (Humans) protein - Drug Relations
Drug Drug group Pharmacological action? Type Actions Details Dipivefrin approved yes target agonist Details Brimonidine approved yes target agonist Details Clonidine approved yes target agonist Details Guanabenz approved, investigational yes target agonist Details Dexmedetomidine approved, vet_approved yes target agonist Details Benzphetamine approved, illicit yes target agonist Details Apraclonidine approved yes target agonist Details Methyldopa approved yes target agonist Details Guanfacine approved, investigational yes target agonist Details Mirtazapine approved yes target antagonist Details Trazodone approved, investigational no target antagonist Details Fenoldopam approved unknown target antagonist Details Pseudoephedrine approved yes target agonist Details Oxymetazoline approved, investigational yes target agonistpartial agonist Details Yohimbine approved, investigational, vet_approved yes target antagonist Details Amitriptyline approved no target antagonistagonist Details 4-Methoxyamphetamine experimental, illicit yes target agonist Details Norepinephrine approved yes target agonist Details Ergotamine approved unknown target partial agonist Details Dronedarone approved yes target antagonist Details Epinastine approved, investigational unknown target unknown Details Mianserin approved, investigational unknown target antagonist Details Lofexidine approved, investigational yes target agonist Details Epicept NP-1 investigational unknown target Details Droxidopa approved, investigational yes target agonist Details Asenapine approved unknown target antagonist Details Ocaperidone investigational unknown target Details Flupirtine investigational unknown target Details Xylometazoline approved, investigational yes target agonist Details Bromocriptine approved, investigational, withdrawn unknown target agonist Details Lisuride approved, investigational unknown target other/unknown Details Cabergoline approved unknown target antagonist Details Pramipexole approved, investigational unknown target agonist Details Apomorphine approved, investigational unknown target agonist Details Paliperidone approved unknown target antagonist Details Quetiapine approved unknown target antagonist Details Ziprasidone approved unknown target antagonist Details Clozapine approved unknown target antagonist Details Aripiprazole approved, investigational no target antagonist Details Methotrimeprazine approved, investigational unknown target antagonist Details Periciazine approved, investigational yes target antagonist Details Zuclopenthixol approved, investigational unknown target antagonist Details Nefazodone approved, withdrawn unknown target antagonist Details Amoxapine approved unknown target antagonist Details Tolazoline approved, vet_approved unknown target antagonist Details Dihydroergotamine approved, investigational unknown target agonist Details Naphazoline approved, investigational yes target agonist Details Phenoxybenzamine approved yes target antagonist Details Ephedra sinica root nutraceutical yes target agonist Details Metamfetamine approved, illicit, withdrawn yes target agonist Details Epinephrine approved, vet_approved yes target agonist Details Lurasidone approved, investigational unknown target Details Loxapine approved unknown target binder Details Carvedilol approved, investigational unknown target antagonist Details Trimipramine approved unknown target antagonist Details Prazosin approved unknown target binder Details Moxonidine approved, investigational yes target agonist Details Rilmenidine approved, investigational unknown target Details Lamotrigine approved, investigational unknown target inhibitor Details Pirlindole experimental unknown target antagonist Details Pipamperone investigational unknown target antagonist Details Racepinephrine approved yes target agonist Details Pizotifen approved unknown target antagonist Details DL-Methylephedrine approved yes target agonist Details Celiprolol approved, investigational unknown target antagonist Details Aripiprazole lauroxil approved, investigational no target Details Haloperidol approved unknown target Details Iloperidone approved unknown target antagonist Details 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline experimental yes target inhibitor Details 1,2,3,4-Tetrahydro-Isoquinoline-7-Sulfonic Acid Amide experimental yes target inhibitor Details Tramazoline investigational yes target inhibitor Details Medetomidine experimental, vet_approved yes target inhibitor Details Tizanidine approved, investigational unknown target agonist Details Bethanidine approved yes target agonist Details Pergolide approved, investigational, vet_approved, withdrawn unknown target agonist Details Chlorpromazine approved, investigational, vet_approved unknown target inhibitor Details Amoxapine approved unknown target antagonist Details Nortriptyline approved unknown target antagonist Details Maprotiline approved, investigational unknown target antagonist Details Desipramine approved, investigational unknown target binder Details Cirazoline experimental yes target antagonist Details Esmirtazapine investigational unknown target antagonist Details Levonordefrin approved yes target agonist Details Tiapride investigational yes target antagonist Details Dosulepin approved yes target antagonist Details Setiptiline experimental unknown target antagonist Details Phenylpropanolamine approved, vet_approved, withdrawn unknown target Details Etoperidone withdrawn unknown target antagonist Details Lorpiprazole approved yes target antagonist Details Xylazine vet_approved yes target agonist Details Prochlorperazine approved, vet_approved no target antagonist Details Paroxetine approved, investigational unknown target binder Details Tramadol approved, investigational yes target inducer Details Escitalopram approved unknown target inhibitor Details Tetryzoline approved unknown target agonist Details Dihydroergotamine approved, investigational unknown target agonist Details Phentolamine approved unknown target antagonist Details Mephentermine approved yes target agonist Details Amphetamine approved, illicit, investigational unknown target agonist Details Moxisylyte approved, investigational yes target antagonist Details Aranidipine experimental unknown target agonist Details Indigotindisulfonic acid approved, investigational no target agonist Details Dihydroergocristine approved, experimental yes target antagonistagonist Details Ergoloid mesylate approved yes target antagonistagonist Details Dihydroergocornine approved yes target antagonistagonist Details DL-Methylephedrine approved yes target agonist Details Ropinirole approved, investigational unknown target antagonist Details Promethazine approved, investigational unknown target antagonist Details Dextroamphetamine approved, illicit unknown target inhibitorinducer Details