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Showing drug card for Guanethidine (DB01170)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:06:43
Primary Accession Number DB01170
Secondary Accession Number
  • APRD01007
Name Guanethidine
Drug Type
  • Approved
  • Small Molecule
Description An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. [PubChem]
Synonyms
  1. Guanethidine Monosulfate
  2. Guanethidine Sulphae
Brand Names
  1. Abapresin
  2. Apo-Guanethidine
  3. Eutensol
  4. Ismelin
  5. Oktadin
Brand Mixtures Not Available
Chemical IUPAC Name 2-[2-(azocan-1-yl)ethyl]guanidine
Chemical Formula C10H22N4
Chemical Structure Structure
CAS Registry Number 645-43-2
InChI Identifier InChI=1/C10H22N4/c11-10(12)13-6-9-14-7-4-2-1-3-5-8-14/h1-9H2,(H4,11,12,13)/f/h11-12H2
InChI Key ACGDKVXYNVEAGU-LLDOCCBOCW
KEGG Drug D02237 Link Image
KEGG Compound Not Available
PubChem Compound 3518 Link Image
PubChem Substance 7854193 Link Image
ChEBI ID Not Available
PharmGKB ID PA449824 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available
RxList Link http://www.rxlist.com/cgi/generic3/guanethidine.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Guanethidine Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 198.3085
Monoisotopic Molecular Weight 198.1844
State Solid
Melting Point 250 oC (sulfate salt)
Experimental Water Solubility Very soluble Source: PhysProp
Predicted Water Solubility 2.25e+00 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 0.8 Source: PhysProp
Predicted LogP 0.89 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -1.95 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES N\C(N)=N/CCN1CCCCCCC1
Canonical SMILES NC(N)=NCCN1CCCCCCC1
Drug Category
  • Adrenergic Agents
  • Antihypertensive Agents
  • Sympatholytics
ATC Codes
AHFS Codes
  • 24:08.32
Indication For the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension.
Pharmacology High blood pressure can cause the heart and arteries to not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled. Guanethidine works by decreasing the heart rate and relaxing the blood vessels so that blood can flow more easily through the body, thereby reducing these risks. It is a postganglionic sympathetic nerve terminal blocker that prevents the release of norepinephrine from nerve terminals.
Mechanism of Action Guanethidine acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine, rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. In contrast to ganglionic blocking agents, Guanethidine suppresses equally the responses mediated by alpha-and beta-adrenergic receptors but does not produce parasympathetic blockade. Since sympathetic blockade results in modest decreases in peripheral resistance and cardiac output, Guanethidine lowers blood pressure in the supine position. It further reduces blood pressure by decreasing the degree of vasoconstriction that normally results from reflex sympathetic nervous activity upon assumption of the upright posture, thus reducing venous return and cardiac output more.
Absorption 3-30% of oral dose (poor and highly variable)
Toxicity Side effects include drowsiness, dizziness, tiredness or confusion. LD50=1000 mg/kg (mouse, oral)
Protein Binding Not Available
Biotransformation Guanethidine is converted by the liver to three metabolites, which are excreted in the urine. The metabolites are pharmacologically less active than the parent compound.
Half Life 1.5 days
Dosage Forms
Form Route
Tablet Oral
Patient Information Not Available
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Acetophenazine The agent decreases the effect of guanethidine
Amitriptyline The tricyclic decreases the effect of guanethidine
Amoxapine The tricyclic decreases the effect of guanethidine
Amphetamine The agent decreases the effect of guanethidine
Benzphetamine The agent decreases the effect of guanethidine
Chlorpromazine The agent decreases the effect of guanethidine
Chlorprothixene The agent decreases the effect of guanethidine
Clomipramine The tricyclic decreases the effect of guanethidine
Desipramine The tricyclic decreases the effect of guanethidine
Dexfenfluramine The agent decreases the effect of guanethidine
Dextroamphetamine The agent decreases the effect of guanethidine
Diethylpropion The agent decreases the effect of guanethidine
Dobutamine The agent decreases the effect of guanethidine
Dopamine The agent decreases the effect of guanethidine
Doxepin The tricyclic decreases the effect of guanethidine
Ephedra The agent decreases the effect of guanethidine
Ephedrine The agent decreases the effect of guanethidine
Epinephrine The agent decreases the effect of guanethidine
Ethopropazine The agent decreases the effect of guanethidine
Fenfluramine The agent decreases the effect of guanethidine
Fluphenazine The agent decreases the effect of guanethidine
Haloperidol The agent decreases the effect of guanethidine
Imipramine The tricyclic decreases the effect of guanethidine
Isocarboxazid The agent decreases the effect of guanethidine
Mazindol The agent decreases the effect of guanethidine
Mesoridazine The agent decreases the effect of guanethidine
Metaraminol The agent decreases the effect of guanethidine
Methamphetamine The agent decreases the effect of guanethidine
Methdilazine The agent decreases the effect of guanethidine
Methotrimeprazine The agent decreases the effect of guanethidine
Methoxamine The agent decreases the effect of guanethidine
Methylphenidate The agent decreases the effect of guanethidine
Norepinephrine The agent decreases the effect of guanethidine
Nortriptyline The tricyclic decreases the effect of guanethidine
Pargyline The agent decreases the effect of guanethidine
Perphenazine The agent decreases the effect of guanethidine
Phendimetrazine The agent decreases the effect of guanethidine
Phenelzine The agent decreases the effect of guanethidine
Phenmetrazine The agent decreases the effect of guanethidine
Phentermine The agent decreases the effect of guanethidine
Phenylephrine The agent decreases the effect of guanethidine
Phenylpropanolamine The agent decreases the effect of guanethidine
Prochlorperazine The agent decreases the effect of guanethidine
Promazine The agent decreases the effect of guanethidine
Promethazine The agent decreases the effect of guanethidine
Propericiazine The agent decreases the effect of guanethidine
Propiomazine The agent decreases the effect of guanethidine
Protriptyline The tricyclic decreases the effect of guanethidine
Pseudoephedrine The agent decreases the effect of guanethidine
Thiethylperazine The agent decreases the effect of guanethidine
Thioridazine The agent decreases the effect of guanethidine
Thiothixene The agent decreases the effect of guanethidine
Tranylcypromine The agent decreases the effect of guanethidine
Trifluoperazine The agent decreases the effect of guanethidine
Triflupromazine The agent decreases the effect of guanethidine
Trimeprazine The agent decreases the effect of guanethidine
Trimipramine The tricyclic decreases the effect of guanethidine
Food Interactions
  • Take without regard to meals.
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
  3. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. Alpha-2A adrenergic receptor
  2. Alpha-2C adrenergic receptor
  3. Sodium-dependent noradrenaline transporter
  4. Alpha-1A adrenergic receptor
  5. Alpha-2B adrenergic receptor
  6. Alpha-1B adrenergic receptor
  7. Alpha-1D adrenergic receptor
Drug Target 1 [top]
Target 1 ID 318
Target 1 Name Alpha-2A adrenergic receptor
Target 1 Synonyms
  1. Alpha-2 adrenergic receptor subtype C10
  2. Alpha-2A adrenoceptor
  3. Alpha-2A adrenoreceptor
  4. Alpha-2AAR
Target 1 Gene Name ADRA2A
Target 1 Protein Sequence >Alpha-2A adrenergic receptor 
MGSLQPDAGNASWNGTEAPGGGARATPYSLQVTLTLVCLAGLLMLLTVFGNVLVIIAVFT
SRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKAWCEIYLALDVLFCTSS
IVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIITVWVISAVISFPPLISIEKKGGGGG
PQPAEPRCEINDQKWYVISSCIGSFFAPCLIMILVYVRIYQIAKRRTRVPPSRRGPDAVA
APPGGTERRPNGLGPERSAGPGGAEAEPLPTQLNGAPGEPAPAGPRDTDALDLEESSSSD
HAERPPGPRRPERGPRGKGKARASQVKPGDSLPRRGPGATGIGTPAAGPGEERVGAAKAS
RWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLTAVGCSVPRTLFKFFFWFGYCNSS
LNPVIYTIFNHDFRRAFKKILCRGDRKRIV
Target 1 Number of Residues 457
Target 1 Molecular Weight 48957
Target 1 Theoretical pI 10.20
Target 1 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha2-adrenergic receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in alpha2-adrenergic receptor activity
Target 1 Specific 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
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 34-59
  • 71-96
  • 107-129
  • 150-173
  • 193-217
  • 375-399
  • 407-430
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 178196 Link Image
Target 1 UniProtKB/Swiss-Prot ID P08913 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name ADA2A_HUMAN Link Image
Target 1 PDB ID 1HOF Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1353 bp 
ATGGGCTCCCTGCAGCCGGACGCGGGCAACGCGAGCTGGAACGGGACCGAGGCGCCGGGG
GGCGGCGCCCGGGCCACCCCTTACTCCCTGCAGGTGACGCTGACGCTGGTGTGCCTGGCC
GGCCTGCTCATGCTGCTCACCGTGTTCGGCAACGTGCTCGTCATCATCGCCGTGTTCACG
AGCCGCGCGCTCAAGGCGCCCCAAAACCTCTTCCTGGTGTCTCTGGCCTCGGCCGACATC
CTGGTGGCCACGCTCGTCATCCCTTTCTCGCTGGCCAACGAGGTCATGGGCTACTGGTAC
TTCGGCAAGGCTTGGTGCGAGATCTACCTGGCGCTCGACGTGCTCTTCTGCACGTCGTCC
ATCGTGCACCTGTGCGCCATCAGCCTGGACCGCTACTGGTCCATCACACAGGCCATCGAG
TACAACCTGAAGCGCACGCCGCGCCGCATCAAGGCCATCATCATCACCGTGTGGGTCATC
TCGGCCGTCATCTCCTTCCCGCCGCTCATCTCCATCGAGAAGAAGGGCGGCGGCGGCGGC
CCGCAGCCGGCCGAGCCGCGCTGCGAGATCAACGACCAGAAGTGGTACGTCATCTCGTCG
TGCATCGGCTCCTTCTTCGCTCCCTGCCTCATCATGATCCTGGTCTACGTGCGCATCTAC
CAGATCGCCAAGCGTCGCACCCGCGTGCCACCCAGCCGCCGGGGTCCGGACGCCGTCGCC
GCGCCGCCGGGGGGCACCGAGCGCAGGCCCAACGGTCTGGGCCCCGAGCGCAGCGCGGGC
CCGGGGGGCGCAGAGGCCGAACCGCTGCCCACCCAGCTCAACGGCGCCCCTGGCGAGCCC
GCGCCGGCCGGGCCGCGCGACACCGACGCGCTGGACCTGGAGGAGAGCTCGTCTTCCGAC
CACGCCGAGCGGCCTCCAGGGCCCCGCAGACCCGAGCGCGGTCCCCGGGGCAAAGGCAAG
GCCCGAGCGAGCCAGGTGAAGCCGGGCGACAGCCTGCGCGGCGCGGGCCGGGGGCGACGG
GGATCGGGACGCCGGCTGCAGGGCCGGGGGAGGAGCGCGTCGGGGCTGCCAAGGCGTCGC
GCTGGCGCGGGCGGGCAGAACCGCGAGAAGCGCTTCACGTTCGTGCTGGCCGTGGTCATC
GGAGTGTTCGTGGTGTGCTGGTTCCCCTTCTTCTTCACCTACACGCTCACGGCCGTCGGG
TGCTCCGTGCCACGCACGCTCTTCAAATTCTTCTTCTGGTTCGGCTACTGCAACAGCTCG
TTGAACCCGGTCATCTACACCATCTTCAACCACGATTTCCGCCGCGCCTTCAAGAAGATC
CTCTGTCGGGGGGACAGGAAGCGGATCGTGTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID ADRA2A Link Image
Target 1 GenAtlas ID ADRA2A Link Image
Target 1 HGNC ID HGNC:281 Link Image
Target 1 Chromosome Location 10
Target 1 Locus 10q24-q26
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. 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. [PubMed Link Image]
  2. 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. [PubMed Link Image]
  3. 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. [PubMed Link Image]
  4. 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. [PubMed Link Image]
  5. 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. [PubMed Link Image]
  6. 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. [PubMed Link Image]
  7. 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. [PubMed Link Image]
Target 1 Drug References
  1. Blandizzi C, Fornai M, Colucci R, Baschiera F, Barbara G, De Giorgio R, De Ponti F, Breschi MC, Del Tacca M: Altered prejunctional modulation of intestinal cholinergic and noradrenergic pathways by alpha2-adrenoceptors in the presence of experimental colitis. Br J Pharmacol. 2003 May;139(2):309-20. [PubMed Link Image]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  3. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 378
Target 2 Name Alpha-2C adrenergic receptor
Target 2 Synonyms
  1. Alpha-2 adrenergic receptor subtype C4
  2. Alpha-2C adrenoceptor
  3. Alpha-2C adrenoreceptor
Target 2 Gene Name ADRA2C
Target 2 Protein Sequence >Alpha-2C adrenergic receptor 
MASPALAAALAVAAAAGPNASGAGERGSGGVANASGASWGPPRGQYSAGAVAGLAAVVGF
LIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFG
QVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISA
VISFPPLVSLYRQPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLR
TRTLSEKRAPVGPDGASPTTENGLGAAAGAGENGHCAPPPADVEPDESSAAAERRRRRGA
LRRGGRRRAGAEGGAGGADGQGAGPGAAESGALTASRSPGPGGRLSRASSRSVEFFLSRR
RRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQVPGPLFK
FFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ
Target 2 Number of Residues 469
Target 2 Molecular Weight 49523
Target 2 Theoretical pI 10.69
Target 2 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha2-adrenergic receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in alpha2-adrenergic receptor activity
Target 2 Specific Function Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 52-76
  • 89-114
  • 125-147
  • 169-191
  • 208-231
  • 380-407
  • 421-441
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 178194 Link Image
Target 2 UniProtKB/Swiss-Prot ID P18825 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name ADA2C_HUMAN Link Image
Target 2 PDB ID 1HOF Link Image
Target 2 PDB File Show
Target 2 3D Structure
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >1386 bp 
ATGGCGTCCCCGGCGCTGGCGGCGGCGCTGGCGGTGGCGGCAGCGGCGGGCCCCAATGCG
AGCGGCGCGGGCGAGAGGGGCAGCGGCGGGGTTGCCAATGCCTCGGGGGCTTCCTGGGGG
CCGCCGCGCGGCCAGTACTCGGCGGGCGCGGTGGCAGGGCTGGCTGCCGTGGTGGGCTTC
CTCATCGTCTTCACCGTGGTGGGCAACGTGCTGGTGGTGATCGCCGTGCTGACCAGCCGG
GCGCTGCGCGCGCCACAGAACCTCTTCCTGGTGTCGCTGGCCTCGGCCGACATCCTGGTG
GCCACGCTGGTCATGCCCTTCTCGTTGGCCAACGAGCTCATGGCCTACTGGTACTTCGGG
CAGGTGTGGTGCGGCGTGTACCTGGCGCTCGATGTGCTGTTTTGCACCTCGTCGATCGTG
CATCTGTGTGCCATCAGCCTGGACCGCTACTGGTCGGTGACGCAGGCCGTCGAGTACAAC
CTGAAGCGCACACCACGCCGCGTCAAGGCCACCATCGTCGCCGTGTGGCTCATCTCGGCC
GTCATCTCCTTCCCGCCGCTGGTCTCGCTCTACCGCCAGCCCGACGGCGCCGCCTACCCG
CAGTGCGGCCTCAACGACGAGACCTGGTACATCCTGTCCTCCTGCATCGGCTCCTTCTTC
GCGCCCTGCCTCATCATGGGCCTGGTCTACGCGCGCATCTACCGAGTGGCCAAGCGTCGC
ACGCGCACGCTCAGCGAGAAGCGCGCCCCCGTGGGCCCCGACGGTGCGTCCCCGACTACC
GAAAACGGGCTGGGCGCGGCGGCAGGCGAGGCGAGAACGGGCACTGCGCGCCCCCGCCCG
CCGACGTGGAGCCGGACGAGAGCAGCGCAGCGGCCGAGAGGCGGCGCGCCGGGGCCGTTG
CGGCGGGGCGGGCGGCGGCGAGCGGGCGCGGAGGGGGGCGCGGGCGGTGCGGACGGGCAG
GGGGCGGGGCCGGGGGCGGCTCAGTCGGGGGCGCTGACCGCCTCCAGGTCCCCGGGGCCC
GGTGGCCGCCTCTCGCGCGCCAGCTCGCGCTCCGTCGAGTTCTTCCTGTCGCGCCGGCGC
CGGGCGCGCAGCAGCGTGTGCCGCCGCAAGGTGGCCCAGGCGCGCGAGAAGCGCTTCACC
TTTGTGCTGGCTGTGGTCATGGGCGTGTTCGTGCTCTGCTGGTTCCCCTTCTTCTTCATC
TACAGCCTGTACGGCATCTGCCGCGAGGCCTGCCAGGTGCCCGGCCCGCTCTTCAAGTTC
TTCTTCTGGATCGGCTACTGCAACAGCTCGCTCAACCCGGTCATCTACACGGTCTTCAAC
CAGGATTTCCGGCCATCCTTCAAGCACATCCTCTTCCGACGGAGGAGAAGGGGCTTCAGG
CAGTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID ADRA2C Link Image
Target 2 GenAtlas ID ADRA2C Link Image
Target 2 HGNC ID HGNC:283 Link Image
Target 2 Chromosome Location 4
Target 2 Locus 4p16
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Small KM, Forbes SL, Rahman FF, Bridges KM, Liggett SB: A four amino acid deletion polymorphism in the third intracellular loop of the human alpha 2C-adrenergic receptor confers impaired coupling to multiple effectors. J Biol Chem. 2000 Jul 28;275(30):23059-64. [PubMed Link Image]
  2. 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. [PubMed Link Image]
  3. Regan JW, Kobilka TS, Yang-Feng TL, Caron MG, Lefkowitz RJ, Kobilka BK: Cloning and expression of a human kidney cDNA for an alpha 2-adrenergic receptor subtype. Proc Natl Acad Sci U S A. 1988 Sep;85(17):6301-5. [PubMed Link Image]
  4. Schaak S, Devedjian JC, Cayla C, Sender Y, Paris H: Molecular cloning, sequencing and functional study of the promoter region of the human alpha2C4-adrenergic receptor gene. Biochem J. 1997 Dec 1;328 ( Pt 2):431-8. [PubMed Link Image]
Target 2 Drug References
  1. Honda M, Suzuki M, Nakayama K, Ishikawa T: Role of alpha2C-adrenoceptors in the reduction of skin blood flow induced by local cooling in mice. Br J Pharmacol. 2007 Sep;152(1):91-100. Epub 2007 Jul 9. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 540
Target 3 Name Sodium-dependent noradrenaline transporter
Target 3 Synonyms
  1. NET
  2. Norepinephrine transporter
Target 3 Gene Name SLC6A2
Target 3 Protein Sequence >Sodium-dependent noradrenaline transporter 
MLLARMNPQVQPENNGADTGPEQPLRARKTAELLVVKERNGVQCLLAPRDGDAQPRETWG
KKIDFLLSVVGFAVDLANVWRFPYLCYKNGGGAFLIPYTLFLIIAGMPLFYMELALGQYN
REGAATVWKICPFFKGVGYAVILIALYVGFYYNVIIAWSLYYLFSSFTLNLPWTDCGHTW
NSPNCTDPKLLNGSVLGNHTKYSKYKFTPAAEFYERGVLHLHESSGIHDIGLPQWQLLLC
LMVVVIVLYFSLWKGVKTSGKVVWITATLPYFVLFVLLVHGVTLPGASNGINAYLHIDFY
RLKEATVWIDAATQIFFSLGAGFGVLIAFASYNKFDNNCYRDALLTSSINCITSFVSGFA
IFSILGYMAHEHKVNIEDVATEGAGLVFILYPEAISTLSGSTFWAVVFFVMLLALGLDSS
MGGMEAVITGLADDFQVLKRHRKLFTFGVTFSTFLLALFCITKGGIYVLTLLDTFAAGTS
ILFAVLMEAIGVSWFYGVDRFSNDIQQMMGFRPGLYWRLCWKFVSPAFLLFVVVVSIINF
KPLTYDDYIFPPWANWVGWGIALSSMVLVPIYVIYKFLSTQGSLWERLAYGITPENEHHL
VAQRDIRQFQLQHWLAI
Target 3 Number of Residues 627
Target 3 Molecular Weight 69333
Target 3 Theoretical pI 7.53
Target 3 GO Classification
Function
transporter activity
neurotransmitter transporter activity
neurotransmitter:sodium symporter activity
Process
physiological process
cellular physiological process
transport
neurotransmitter transport
Component
cell
membrane
intrinsic to membrane
integral to membrane
integral to plasma membrane
Target 3 General Function Involved in neurotransmitter:sodium symporter activity
Target 3 Specific Function Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 65-85
  • 93-112
  • 136-156
  • 235-253
  • 262-279
  • 315-332
  • 344-365
  • 398-417
  • 444-462
  • 478-498
  • 519-538
  • 557-575
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 189258 Link Image
Target 3 UniProtKB/Swiss-Prot ID P23975 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name SC6A2_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >1854 bp 
ATGCTTCTGGCGCGGATGAACCCGCAGGTGCAGCCCGAGAACAACGGGGCGGACACGGGT
CCAGAGCAGCCCCTTCGGGCGCGCAAAACTGCGGAGCTGCTGGTGGTGAAGGAGCGCAAC
GGCGTCCAGTGCCTGCTGGCGCCCCGCGACGGCGACGCGCAGCCCCGGGAGACCTGGGGC
AAGAAGATCGACTTCCTGCTGTCCGTAGTCGGCTTCGCAGTGGACCTGGCCAACGTGTGG
CGCTTCCCCTACCTCTGCTACAAGAACGGCGGCGGTGCCTTCTTGATCCCGTACACACTG
TTCCTTATCATCGCGGGGATGCCCCTGTTCTACATGGAGCTGGCTCTGGGACAGTACAAC
CGGGAGGGGGCTGCCACCGTTTGGAAAATCTGCCCATTCTTCAAAGGCGTTGGCTATGCT
GTCATCCTGATCGCCCTGTACGTTGGCTTCTACTACAACGTCATCATCGCCTGGTCACTC
TACTACCTCTTCTCCTCCTTCACCCTCAACCTGCCCTGGACCGACTGTGGCCACACCTGG
AACAGCCCCAACTGTACCGACCCCAAGCTCCTCAATGGCTCCGTGCTTGGCAACCACACC
AAGTACTCCAAGTACAAGTTCACGCCGGCAGCCGAGTTTTATGAGCGTGGTGTCCTGCAC
CTTCACGAGAGCAGCGGGATTCATGACATCGGCCTGCCCCAGTGGCAGCTCTTGCTCTGT
CTGATGGTCGTCGTCATCGTCTTGTATTTTAGCCTCTGGAAAGGGGTGAAGACATCAGGA
AAGGTGGTGTGGATCACAGCCACGCTGCCTTACTTCGTGCTGTTCGTGCTCCTGGTCCAT
GGCGTCACGCTGCCCGGAGCCTCCAATGGCATCAATGCCTACCTGCACATCGACTTCTAC
CGCTTGAAAGAGGCCACGGTATGGATTGATGCCGCAACTCAGATATTTTTTTCCTTGGGG
GCTGGATTTGGAGTATTGATTGCATTTGCCAGTTACAACAAATTTGACAACAACTGTTAC
AGGGATGCCCTGCTGACCAGCAGCATCAACTGTATCACCAGCTTCGTCTCTGGGTTCGCC
ATCTTCTCCATCCTTGGTTACATGGCCCATGAACACAAGGTCAACATTGAGGATGTGGCC
ACAGAAGGAGCTGGCCTAGTGTTCATCCTGTATCCAGAGGCCATTTCTACCCTGTCTGGA
TCTACATTCTGGGCTGTTGTGTTTTTCGTCATGCTCCTGGCGCTGGGCCTTGACAGCTCA
ATGGGAGGCATGGAGGCTGTCATCACGGGCCTGGCAGATGACTTCCAGGTCCTGAAGCGA
CACCGGAAACTCTTCACATTTGGCGTCACCTTCAGCACTTTCCTTCTCGCCCTGTTCTGC
ATAACCAAGGGTGGAATTTACGTCTTGACCCTCCTGGACACCTTTGCTGCGGGCACCTCC
ATCCTTTTTGCTGTCCTCATGGAAGCCATCGGAGTTTCCTGGTTTTATGGAGTGGACAGG
TTCAGCAACGACATCCAGCAGATGATGGGGTTCAGGCCGGGTCTATACTGGAGACTGTGC
TGGAAGTTCGTCAGTCCTGCCTTCCTCCTGTTCGTGGTTGTGGTCAGCATCATCAACTTC
AAGCCACTCACCTACGACGACTACATCTTCCCGCCCTGGGCCAACTGGGTGGGGTGGGGC
ATCGCCCTGTCCTCCATGGTCCTGGTGCCCATCTACGTCATCTATAAGTTCCTCAGCACG
CAGGGCTCTCTTTGGGAGAGACTGGCCTATGGCATCACGCCAGAGAACGAGCACCACCTG
GTGGCTCAGAGGGACATCAGACAGTTCCAGTTGCAACACTGGCTGGCCATCTGA
Target 3 GenBank Gene ID
Target 3 GeneCard ID SLC6A2 Link Image
Target 3 GenAtlas ID SLC6A2 Link Image
Target 3 HGNC ID HGNC:11048 Link Image
Target 3 Chromosome Location 16
Target 3 Locus 16q12.2
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Shannon JR, Flattem NL, Jordan J, Jacob G, Black BK, Biaggioni I, Blakely RD, Robertson D: Orthostatic intolerance and tachycardia associated with norepinephrine-transporter deficiency. N Engl J Med. 2000 Feb 24;342(8):541-9. [PubMed Link Image]
  2. Torres GE, Yao WD, Mohn AR, Quan H, Kim KM, Levey AI, Staudinger J, Caron MG: Functional interaction between monoamine plasma membrane transporters and the synaptic PDZ domain-containing protein PICK1. Neuron. 2001 Apr;30(1):121-34. [PubMed Link Image]
  3. Pacholczyk T, Blakely RD, Amara SG: Expression cloning of a cocaine- and antidepressant-sensitive human noradrenaline transporter. Nature. 1991 Mar 28;350(6316):350-4. [PubMed Link Image]
  4. Porzgen P, Bonisch H, Bruss M: Molecular cloning and organization of the coding region of the human norepinephrine transporter gene. Biochem Biophys Res Commun. 1995 Oct 24;215(3):1145-50. [PubMed Link Image]
Target 3 Drug References
  1. Joyce PI, Atcheson R, Marcus RJ, Heffernan AM, Rowbotham DJ, Lambert DG: Interaction of local anaesthetic agents with the endogenous norepinephrine transporter in SH-SY5Y human neuroblastoma cells. Neurosci Lett. 2001 Jun 15;305(3):161-4. [PubMed Link Image]
  2. Yi E, Love JA: Alpha-adrenergic modulation of synaptic transmission in rabbit pancreatic ganglia. Auton Neurosci. 2005 Oct 30;122(1-2):45-57. Epub 2005 Aug 25. [PubMed Link Image]
Drug Target 4 [top]
Target 4 ID 556
Target 4 Name Alpha-1A adrenergic receptor
Target 4 Synonyms
  1. Alpha 1A- adrenoreceptor
  2. Alpha 1A-adrenoceptor
  3. Alpha adrenergic receptor 1c
  4. Alpha-1C adrenergic receptor
Target 4 Gene Name ADRA1A
Target 4 Protein Sequence >Alpha-1A adrenergic receptor 
MVFLSGNASDSSNCTQPPAPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSV
THYYIVNLAVADLLLTSTVLPFSAIFEVLGYWAFGRVFCNIWAAVDVLCCTASIMGLCII
SIDRYIGVSYPLRYPTIVTQRRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINE
EPGYVLFSALGSFYLPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKN
APAGGSGMASAKTKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPD
FKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLCRKQSSKHALGYTL
HPPSQAVEGQHKDMVRIPVGSRETFYRISKTDGVCEWKFFSSMPRGSARITVSKDQSSCT
TARVRSKSFLQVCCCVGPSTPSLDKNHQVPTIKVHTISLSENGEEV
Target 4 Number of Residues 473
Target 4 Molecular Weight 51487
Target 4 Theoretical pI 9.23
Target 4 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 4 General Function Involved in alpha1-adrenergic receptor activity
Target 4 Specific Function This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 28-51
  • 65-88
  • 100-122
  • 144-167
  • 182-205
  • 274-297
  • 306-329
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 433201 Link Image
Target 4 UniProtKB/Swiss-Prot ID P35348 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name ADA1A_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 4 Gene Sequence >1401 bp 
ATGGTGTTTCTCTCGGGAAATGCTTCCGACAGCTCCAACTGCACCCAACCGCCGGCACCG
GTGAACATTTCCAAGGCCATTCTGCTCGGGGTGATCTTGGGGGGCCTCATTCTTTTCGGG
GTGCTGGGTAACATCCTAGTGATCCTCTCCGTAGCCTGTCACCGACACCTGCACTCAGTC
ACGCACTACTACATCGTCAACCTGGCGGTGGCCGACCTCCTGCTCACCTCCACGGTGCTG
CCCTTCTCCGCCATCTTCGAGGTCCTAGGCTACTGGGCCTTCGGCAGGGTCTTCTGCAAC
ATCTGGGCGGCAGTGGATGTGCTGTGCTGCACCGCGTCCATCATGGGCCTCTGCATCATC
TCCATCGACCGCTACATCGGCGTGAGCTACCCGCTGCGCTACCCAACCATCGTCACCCAG
AGGAGGGGTCTCATGGCTCTGCTCTGCGTCTGGGCACTCTCCCTGGTCATATCCATTGGA
CCCCTGTTCGGCTGGAGGCAGCCGGCCCCCGAGGACGAGACCATCTGCCAGATCAACGAG
GAGCCGGGCTACGTGCTCTTCTCAGCGCTGGGCTCCTTCTACCTGCCTCTGGCCATCATC
CTGGTCATGTACTGCCGCGTCTACGTGGTGGCCAAGAGGGAGAGCCGGGGCCTCAAGTCT
GGCCTCAAGACCGACAAGTCGGACTCGGAGCAAGTGACGCTCCGCATCCATCGGAAAAAC
GCCCCGGCAGGAGGCAGCGGGATGGCCAGCGCCAAGACCAAGACGCACTTCTCAGTGAGG
CTCCTCAAGTTCTCCCGGGAGAAGAAAGCGGCCAAAACGCTGGGCATCGTGGTCGGCTGC
TTCGTCCTCTGCTGGCTGCCTTTTTTCTTAGTCATGCCCATTGGGTCTTTCTTCCCTGAT
TTCAAGCCCTCTGAAACAGTTTTTAAAATAGTATTTTGGCTCGGATATCTAAACAGCTGC
ATCAACCCCATCATATACCCATGCTCCAGCCAAGAGTTCAAAAAGGCCTTTCAGAATGTC
TTGAGAATCCAGTGTCTCCGCAGAAAGCAGTCTTCCAAACATGCCCTGGGCTACACCCTG
CACCCGCCCAGCCAGGCCGTGGAAGGGCAACACAAGGACATGGTGCGCATCCCCGTGGGA
TCAAGAGAGACCTTCTACAGGATCTCCAAGACGGATGGCGTTTGTGAATGGAAATTTTTC
TCTTCCATGCCCCGTGGATCTGCCAGGATTACAGTGTCCAAAGACCAATCCTCCTGTACC
ACAGCCCGGGTGAGAAGTAAAAGCTTTTTGGAGGTCTGCTGCTGTGTAGGGCCCTCAACC
CCCAGCCTTGACAAGAACCATCAAGTTCCAACCATTAAGGTCCACACCATCTCCCTCAGT
GAGAACGGGGAGGAAGTCTAG
Target 4 GenBank Gene ID
Target 4 GeneCard ID ADRA1A Link Image
Target 4 GenAtlas ID ADRA1A Link Image
Target 4 HGNC ID HGNC:277 Link Image
Target 4 Chromosome Location 8
Target 4 Locus 8p21-p11.2
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Hirasawa A, Shibata K, Horie K, Takei Y, Obika K, Tanaka T, Muramoto N, Takagaki K, Yano J, Tsujimoto G: Cloning, functional expression and tissue distribution of human alpha 1c-adrenoceptor splice variants. FEBS Lett. 1995 Apr 24;363(3):256-60. [PubMed Link Image]
  2. Schwinn DA, Johnston GI, Page SO, Mosley MJ, Wilson KH, Worman NP, Campbell S, Fidock MD, Furness LM, Parry-Smith DJ, et al.: Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. J Pharmacol Exp Ther. 1995 Jan;272(1):134-42. [PubMed Link Image]
  3. Weinberg DH, Trivedi P, Tan CP, Mitra S, Perkins-Barrow A, Borkowski D, Strader CD, Bayne M: Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c. Biochem Biophys Res Commun. 1994 Jun 30;201(3):1296-304. [PubMed Link Image]
  4. Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA, et al.: The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol. 1994 Apr;45(4):703-8. [PubMed Link Image]
  5. Hirasawa A, Horie K, Tanaka T, Takagaki K, Murai M, Yano J, Tsujimoto G: Cloning, functional expression and tissue distribution of human cDNA for the alpha 1C-adrenergic receptor. Biochem Biophys Res Commun. 1993 Sep 15;195(2):902-9. [PubMed Link Image]
  6. Tseng-Crank J, Kost T, Goetz A, Hazum S, Roberson KM, Haizlip J, Godinot N, Robertson CN, Saussy D: The alpha 1C-adrenoceptor in human prostate: cloning, functional expression, and localization to specific prostatic cell types. Br J Pharmacol. 1995 Aug;115(8):1475-85. [PubMed Link Image]
  7. Chang DJ, Chang TK, Yamanishi SS, Salazar FH, Kosaka AH, Khare R, Bhakta S, Jasper JR, Shieh IS, Lesnick JD, Ford AP, Daniels DV, Eglen RM, Clarke DE, Bach C, Chan HW: Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms. FEBS Lett. 1998 Jan 30;422(2):279-83. [PubMed Link Image]
Target 4 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 5 [top]
Target 5 ID 629
Target 5 Name Alpha-2B adrenergic receptor
Target 5 Synonyms
  1. Alpha-2 adrenergic receptor subtype C2
  2. Alpha-2B adrenoceptor
  3. Alpha-2B adrenoreceptor
Target 5 Gene Name ADRA2B
Target 5 Protein Sequence >Alpha-2B adrenergic receptor 
MDHQDPYSVQATAAIAAAITFLILFTIFGNALVILAVLTSRSLRAPQNLFLVSLAAADIL
VATLIIPFSLANELLGYWYFRRTWCEVYLALDVLFCTSSIVHLCAISLDRYWAVSRALEY
NSKRTPRRIKCIILTVWLIAAVISLPPLIYKGDQGPQPRGRPQCKLNQEAWYILASSIGS
FFAPCLIMILVYLRIYLIAKRSNRRGPRAKGGPGQGESKQPRPDHGGALASAKLPALASV
ASAREVNGHSKSTGEKEEGETPEDTGTRALPPSWAALPNSGQGQKEGVCGASPEDEAEEE
EEEEEEEEECEPQAVPVSPASACSPPLQQPQGSRVLATLRGQVLLGRGVGAIGGQWWRRR
AQLTREKRFTFVLAVVIGVFVLCWFPFFFSYSLGAICPKHCKVPHGLFQFFFWIGYCNSS
LNPVIYTIFNQDFRRAFRRILCRPWTQTAW
Target 5 Number of Residues 457
Target 5 Molecular Weight 49954
Target 5 Theoretical pI 8.52
Target 5 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha2-adrenergic receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 5 General Function Involved in alpha2-adrenergic receptor activity
Target 5 Specific 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 clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • 13-38
  • 50-75
  • 86-108
  • 131-153
  • 170-193
  • 373-396
  • 406-429
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 178198 Link Image
Target 5 UniProtKB/Swiss-Prot ID P18089 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name ADA2B_HUMAN Link Image
Target 5 PDB ID 1HOF Link Image
Target 5 PDB File Show
Target 5 3D Structure
Target 5 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 5 Gene Sequence >1353 bp 
ATGGACCACCAGGACCCCTACTCCGTGCAGGCCACAGCGGCCATAGCGGCGGCCATCACC
TTCCTCATTCTCTTTACCATCTTCGGCAACGCTCTGGTCATCCTGGCTGTGTTGACCAGC
CGCTCGCTGCGCGCCCCTCAGAACCTGTTCCTGGTGTCGCTGGCCGCCGCCGACATCCTG
GTGGCCACGCTCATCATCCCTTTCTCGCTGGCCAACGAGCTGCTGGGCTACTGGTACTTC
CGGCGCACGTGGTGCGAGGTGTACCTGGCGCTCGACGTGCTCTTCTGCACCTCGTCCATC
GTGCACCTGTGCGCCATCAGCCTGGACCGCTACTGGGCCGTGAGCCGCGCGCTGGAGTAC
AACTCCAAGCGCACCCCGCGCCGCATCAAGTGCATCATCCTCACTGTGTGGCTCATCGCC
GCCGTCATCTCGCTGCCGCCCCTCATCTACAAGGGCGACCAGGGCCCCCAGCCGCGCGGG
CGCCCCCAGTGCAAGCTCAACCAGGAGGCCTGGTACATCCTGGCCTCCAGCATCGGATCT
TTCTTTGCTCCTTGCCTCATCATGATCCTTGTCTACCTGCGCATCTACCTGATCGCCAAA
CGCAGCAACCGCAGAGGTCCCAGGGCCAAGGGGGGGCCTGGGCAGGGTGAGTCCAAGCAG
CCCCGACCCGACCATGGTGGGGCTTTGGCCTCAGCCAAACTGCCAGCCCTGGCCTCTGTG
GCTTCTGCCAGAGAGGTCAACGGACACTCGAAGTCCACTGGGGAGAAGGAGGAGGGGGAG
ACCCCTGAAGATACTGGGACCCGGGCCTTGCCACCCAGTTGGGCTGCCCTTCCCAACTCA
GGCCAGGGCCAGAAGGAGGGTGTTTGTGGGGCATCTCCAGAGGATGAAGCTGAAGAGGAG
GAAGAGGAGGAGGAGGAGGAGGAAGAGTGTGAACCCCAGGCAGTGCCAGTGTCTCCGGCC
TCAGCTTGCAGCCCCCCGCTGCAGCAGCCACAGGGCTCCCGGGTGCTGGCCACCCTACGT
GGCCAGGTGCTCCTGGGCAGGGGCGTGGGTGCTATAGGTGGGCAGTGGTGGCGTCGAAGG
GCGCACGTGACCCGGGAGAAGCGCTTCACCTTCGTGCTGGCTGTGGTCATTGGCGTTTTT
GTGCTCTGCTGGTTCCCCTTCTTCTTCAGCTACAGCCTGGGCGCCATCTGCCCGAAGCAC
TGCAAGGTGCCCCATGGCCTCTTCCAGTTCTTCTTCTGGATCGGCTACTGCAACAGCTCA
CTGAACCCTGTTATCTACACCATCTTCAACCAGGACTTCCGCCGTGCCTTCCGGAGGATC
CTGTGCCGCCCGTGGACCCAGACGGCCTGGTGA
Target 5 GenBank Gene ID
Target 5 GeneCard ID ADRA2B Link Image
Target 5 GenAtlas ID ADRA2B Link Image
Target 5 HGNC ID HGNC:282 Link Image
Target 5 Chromosome Location 2
Target 5 Locus 2p13-q13
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Lomasney JW, Lorenz W, Allen LF, King K, Regan JW, Yang-Feng TL, Caron MG, Lefkowitz RJ: Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor subtype, the gene for which is located on chromosome 2. Proc Natl Acad Sci U S A. 1990 Jul;87(13):5094-8. [PubMed Link Image]
  2. Weinshank RL, Zgombick JM, Macchi M, Adham N, Lichtblau H, Branchek TA, Hartig PR: Cloning, expression, and pharmacological characterization of a human alpha 2B-adrenergic receptor. Mol Pharmacol. 1990 Nov;38(5):681-8. [PubMed Link Image]
  3. Chang AC, Ho TF, Chang NC: In vitro amplification by polymerase chain reaction of a partial gene encoding the third subtype of alpha-2 adrenergic receptor in humans. Biochem Biophys Res Commun. 1990 Oct 30;172(2):817-23. [PubMed Link Image]
Target 5 Drug References
  1. Fuder H, Selbach M: Characterization of sensory neurotransmission and its inhibition via alpha 2B-adrenoceptors and via non-alpha 2-receptors in rabbit iris. Naunyn Schmiedebergs Arch Pharmacol. 1993 Apr;347(4):394-401. [PubMed Link Image]
Drug Target 6 [top]
Target 6 ID 632
Target 6 Name Alpha-1B adrenergic receptor
Target 6 Synonyms
  1. Alpha 1B- adrenoreceptor
  2. Alpha 1B-adrenoceptor
Target 6 Gene Name ADRA1B
Target 6 Protein Sequence >Alpha-1B adrenergic receptor 
MNPDLDTGHNTSAPAHWGELKNANFTGPNQTSSNSTLPQLDITRAISVGLVLGAFILFAI
VGNILVILSVACNRHLRTPTNYFIVNLAMADLLLSFTVLPFSAALEVLGYWVLGRIFCDI
WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP
LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG
VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV
GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFV
RILGCQCRGRGRRRRRRRRRLGGCAYTYRPWTRGGSLERSQSRKDSLDDSGSCLSGSQRT
LPSASPSPGYLGRGAPPPVELCAFPEWKAPGALLSLPAPEPPGRRGRHDSGPLFTFKLLT
EPESPGTDGGASNGGCEAAADVANGQPGFKSNMPLAPGQF
Target 6 Number of Residues 528
Target 6 Molecular Weight 56837
Target 6 Theoretical pI 9.79
Target 6 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 6 General Function Involved in alpha1-adrenergic receptor activity
Target 6 Specific Function This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Pfam Domain Function
Target 6 Signals
  • None
Target 6 Transmembrane Regions
  • 46-70
  • 84-105
  • 116-141
  • 162-182
  • 202-224
  • 296-319
  • 327-340
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein Not Available
Target 6 UniProtKB/Swiss-Prot ID P35368 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name ADA1B_HUMAN Link Image
Target 6 PDB ID Not Available
Target 6 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 6 Gene Sequence Not Available
Target 6 GenBank Gene ID
Target 6 GeneCard ID ADRA1B Link Image
Target 6 GenAtlas ID ADRA1B Link Image
Target 6 HGNC ID HGNC:278 Link Image
Target 6 Chromosome Location 5
Target 6 Locus 5q23-q32
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Ramarao CS, Denker JM, Perez DM, Gaivin RJ, Riek RP, Graham RM: Genomic organization and expression of the human alpha 1B-adrenergic receptor. J Biol Chem. 1992 Oct 25;267(30):21936-45. [PubMed Link Image]
  2. Schwinn DA, Johnston GI, Page SO, Mosley MJ, Wilson KH, Worman NP, Campbell S, Fidock MD, Furness LM, Parry-Smith DJ, et al.: Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. J Pharmacol Exp Ther. 1995 Jan;272(1):134-42. [PubMed Link Image]
  3. Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA, et al.: The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol. 1994 Apr;45(4):703-8. [PubMed Link Image]
Target 6 Drug References
  1. Peng T, Jiang X, Wang Y, Hand A, Gillies C, Cone RE, O'Rourke J: Sympathectomy decreases and adrenergic stimulation increases the release of tissue plasminogen activator (t-PA) from blood vessels: functional evidence for a neurologic regulation of plasmin production within vessel walls and other tissue matrices. J Neurosci Res. 1999 Sep 1;57(5):680-92. [PubMed Link Image]
  2. Soydan G, Tekes E, Tuncer M: Investigation of serotonin receptors in the isolated penile bulb of rats. Int J Impot Res. 2006 Nov-Dec;18(6):510-6. Epub 2006 Mar 9. [PubMed Link Image]
  3. Pool JL: Combination antihypertensive therapy with terazosin and other antihypertensive agents: results of clinical trials. Am Heart J. 1991 Sep;122(3 Pt 2):926-31. [PubMed Link Image]
  4. Cruise JL, Knechtle SJ, Bollinger RR, Kuhn C, Michalopoulos G: Alpha 1-adrenergic effects and liver regeneration. Hepatology. 1987 Nov-Dec;7(6):1189-94. [PubMed Link Image]
  5. Fazan Junior R, Castania JA, Ballejo G, Salgado MC, Salgado HC: Influence of sympathetic blockade on the acute hypertensive response to aortic constriction. Am J Physiol. 1997 Dec;273(6 Pt 2):H2648-51. [PubMed Link Image]
Drug Target 7 [top]
Target 7 ID 789
Target 7 Name Alpha-1D adrenergic receptor
Target 7 Synonyms
  1. Alpha 1D- adrenoreceptor
  2. Alpha 1D-adrenoceptor
  3. Alpha adrenergic receptor 1a
  4. Alpha-1A adrenergic receptor
Target 7 Gene Name ADRA1D
Target 7 Protein Sequence >Alpha-1D adrenergic receptor 
MTFRDLLSVSFEGPRPDSSAGGSSAGGGGGSAGGAAPSEGPAVGGVPGGAGGGGGVVGAG
SGEDNRSSAGEPGSAGAGGDVNGTAAVGGLVVSAQGVGVGVFLAAFILMAVAGNLLVILS
VACNRHLQTVTNYFIVNLAVADLLLSATVLPFSATMEVLGFWAFGRAFCDVWAAVDVLCC
TASILSLCTISVDRYVGVRHSLKYPAIMTERKAAAILALLWVVALVVSVGPLLGWKEPVP
PDERFCGITEEAGYAVFSSVCSFYLPMAVIVVMYCRVYVVARSTTRSLEAGVKRERGKAS
EVVLRIHCRGAATGADGAHGMRSAKGHTFRSSLSVRLLKFSREKKAAKTLAIVVGVFVLC
WFPFFFVLPLGSLFPQLKPSEGVFKVIFWLGYFNSCVNPLIYPCSSREFKRAFLRLLRCQ
CRRRRRRRPLWRVYGHHWRASTSGLRQDCAPSSGDAPPGAPLALTALPDPDPEPPGTPEM
QAPVASRRKPPSAFREWRLLGPFRRPTTQLRAKVSSLSHKIRAGGAQRAEAACAQRSEVE
AVSLGVPHEVAEGATCQAYELADYSNLRETDI
Target 7 Number of Residues 581
Target 7 Molecular Weight 60463
Target 7 Theoretical pI 9.44
Target 7 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 7 General Function Carbohydrate transport and metabolism
Target 7 Specific Function This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium
Target 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Pfam Domain Function
Target 7 Signals
  • None
Target 7 Transmembrane Regions
  • 96-121
  • 134-159
  • 170-192
  • 214-238
  • 252-275
  • 349-373
  • 381-405
Target 7 Essentiality Non-Essential
Target 7 GenBank ID Protein 177807 Link Image
Target 7 UniProtKB/Swiss-Prot ID P25100 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name ADA1D_HUMAN Link Image
Target 7 PDB ID Not Available
Target 7 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 7 Gene Sequence >1719 bp 
ATGACTTTCCGCGATCTCCTGAGCGTCAGTTTCGAGGGACCCCGCCCGGACAGCAGCGCA
GGGGGCTCCAGCGCGGGCGGCGGCGGGGGCAGCGCGGGCGGCGCGGCCCCCTCGGAGGGC
CCGGCGGTGGGCGGCGTGCCGGGGGGCGCGGGCGGCGGCGGCGGCGTGGTGGGCGCAGGC
AGCGGCGAGGACAACCGGAGCTCCGCGGGGGAGCCGGGGAGCGCGGGCGCGGGCGGCGAC
GTGAATGGCACGGCGGCCGTCGGGGGACTGGTGGTGAGCGCGCAGGGCGTGGGCGTGGGC
GTCTTCCTGGCAGCCTTCATCCTTATGGCCGTGGCAGGTAACCTGCTTGTCATCCTCTCA
GTGGCCTGCAACCGCCACCTGCAGACCGTCACCAACTATTTCATCGTGAACCTGGCCGTG
GCCGACCTGCTGCTGAGCGCCACCGTACTGCCCTTCTCGGCCACCATGGAGGTTCTGGGC
TTCTGGGCCTTTGGCCGCGCCTTCTGCGACGTATGGGCCGCCGTGGACGTGCTGTGCTGC
ACGGCCTCCATCCTCAGCCTCTGCACCATCTCCGTGGACCGGTACGTGGGCGTGCGCCAC
TCACTCAAGTACCCAGCCATCATGACCGAGCGCAAGGCGGCCGCCATCCTGGCCCTGCTC
TGGGTCGTAGCCCTGGTGGTGTCCGTAGGGCCCCTGCTGGGCTGGAAGGAGCCCGTGCCC
CCTGACGAGCGCTTCTGCGGTATCACCGAGGAGGCGGGCTACGCTGTCTTCTCCTCCGTG
TGCTCCTTCTACCTGCCCATGGCGGTCATCGTGGTCATGTACTGCCGCGTGTACGTGGTC
GCGCGCAGCACCACGCGCAGCCTCGAGGCAGGCGTCAAGCGCGAGCGAGGCAAGGCCTCC
GAGGTGGTGCTGCGCATCCACTGTCGCGGCGCGGCCACGGGCGCCGACGGGGCGCACGGC
ATGCGCAGCGCCAAGGGCCACACCTTCCGCAGCTCGCTCTCCGTGCGCCTGCTCAAGTTC
TCCCGTGAGAAGAAAGCGGCCAAGACTCTGGCCATCGTCGTGGGTGTCTTCGTGCTCTGC
TGGTTCCCTTTCTTCTTTGTCCTGCCGCTCGGCTCCTTGTTCCCGCAGCTGAAGCCATCG
GAGGGCGTCTTCAAGGTCATCTTCTGGCTCGGCTACTTCAACAGCTGCGTGAACCCGCTC
ATCTACCCCTGTTCCAGCCGCGAGTTCAAGCGCGCCTTCCTCCGTCTCCTGCGCTGCCAG
TGCCGTCGTCGCCGGCGCCGCCGCCCTCTCTGGCGTGTCTACGGCCACCACTGGCGGGCC
TCCACCAGCGGCCTGCGCCAGGACTGCGCCCCGAGTTCGGGCGACGCGCCCCCCGGAGCG
CCGCTGGCCCTCACCGCGCTCCCCGACCCCGACCCCGAACCCCCAGGCACGCCCGAGATG
CAGGCTCCGGTCGCCAGCCGTCGAAAGCCACCCAGCGCCTTCCGCGAGTGGAGGCTGCTG
GGGCCGTTCCGGAGACCCACGACCCAGCTGCGCGCCAAAGTCTCCAGCCTGTCGCACAAG
ATCCGCGCCGGGGGCGCGCAGCGCGCAGAGGCAGCGTGCGCCCAGCGCTCAGAGGTGGAG
GCTGTGTCCCTAGGCGTCCCACACGAGGTGGCCGAGGGCGCCACCTGCCAGGCCTACGAA
TTGGCCGACTACAGCAACCTACGGGAGACCGATATTTAA
Target 7 GenBank Gene ID
Target 7 GeneCard ID ADRA1D Link Image
Target 7 GenAtlas ID ADRA1D Link Image
Target 7 HGNC ID HGNC:280 Link Image
Target 7 Chromosome Location 20
Target 7 Locus 20p13
Target 7 SNPs SNPJam Report Link Image
Target 7 General References
  1. Deloukas P, Matthews LH, Ashurst J, Burton J, Gilbert JG, Jones M, Stavrides G, Almeida JP, Babbage AK, Bagguley CL, Bailey J, Barlow KF, Bates KN, Beard LM, Beare DM, Beasley OP, Bird CP, Blakey SE, Bridgeman AM, Brown AJ, Buck D, Burrill W, Butler AP, Carder C, Carter NP, Chapman JC, Clamp M, Clark G, Clark LN, Clark SY, Clee CM, Clegg S, Cobley VE, Collier RE, Connor R, Corby NR, Coulson A, Coville GJ, Deadman R, Dhami P, Dunn M, Ellington AG, Frankland JA, Fraser A, French L, Garner P, Grafham DV, Griffiths C, Griffiths MN, Gwilliam R, Hall RE, Hammond S, Harley JL, Heath PD, Ho S, Holden JL, Howden PJ, Huckle E, Hunt AR, Hunt SE, Jekosch K, Johnson CM, Johnson D, Kay MP, Kimberley AM, King A, Knights A, Laird GK, Lawlor S, Lehvaslaiho MH, Leversha M, Lloyd C, Lloyd DM, Lovell JD, Marsh VL, Martin SL, McConnachie LJ, McLay K, McMurray AA, Milne S, Mistry D, Moore MJ, Mullikin JC, Nickerson T, Oliver K, Parker A, Patel R, Pearce TA, Peck AI, Phillimore BJ, Prathalingam SR, Plumb RW, Ramsay H, Rice CM, Ross MT, Scott CE, Sehra HK, Shownkeen R, Sims S, Skuce CD, Smith ML, Soderlund C, Steward CA, Sulston JE, Swann M, Sycamore N, Taylor R, Tee L, Thomas DW, Thorpe A, Tracey A, Tromans AC, Vaudin M, Wall M, Wallis JM, Whitehead SL, Whittaker P, Willey DL, Williams L, Williams SA, Wilming L, Wray PW, Hubbard T, Durbin RM, Bentley DR, Beck S, Rogers J: The DNA sequence and comparative analysis of human chromosome 20. Nature. 2001 Dec 20-27;414(6866):865-71. [PubMed Link Image]
  2. Bruno JF, Whittaker J, Song JF, Berelowitz M: Molecular cloning and sequencing of a cDNA encoding a human alpha 1A adrenergic receptor. Biochem Biophys Res Commun. 1991 Sep 30;179(3):1485-90. [PubMed Link Image]
  3. Esbenshade TA, Hirasawa A, Tsujimoto G, Tanaka T, Yano J, Minneman KP, Murphy TJ: Cloning of the human alpha 1d-adrenergic receptor and inducible expression of three human subtypes in SK-N-MC cells. Mol Pharmacol. 1995 May;47(5):977-85. [PubMed Link Image]
  4. Schwinn DA, Johnston GI, Page SO, Mosley MJ, Wilson KH, Worman NP, Campbell S, Fidock MD, Furness LM, Parry-Smith DJ, et al.: Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. J Pharmacol Exp Ther. 1995 Jan;272(1):134-42. [PubMed Link Image]
  5. Weinberg DH, Trivedi P, Tan CP, Mitra S, Perkins-Barrow A, Borkowski D, Strader CD, Bayne M: Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c. Biochem Biophys Res Commun. 1994 Jun 30;201(3):1296-304. [PubMed Link Image]
  6. Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA, et al.: The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol. 1994 Apr;45(4):703-8. [PubMed Link Image]
Target 7 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.