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Showing drug card for Lofexidine (DB04948)

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Version 2.5
Creation Date 2007-10-21 22:23:16
Update Date 2009-06-23 18:08:08
Primary Accession Number DB04948
Secondary Accession Number Not Available
Name Lofexidine
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description Lofexidine is an alpha2-adrenergic receptor agonist. It can be used as a short acting anti-hypertensive, but is mostly used to help relieve symptoms of heroin or opiate withdrawal in opiate dependency. It is approved in the United Kingdom, but is still undergoing clinical trials in the United States.
Synonyms
  1. 2-(1-(2,6-Dichlorophenoxy)ethyl)-4,5-dihydro-1H-imidazole
  2. 2-(alpha-(2,6-Dichlorophenoxy)ethyl)2-imidazoline
  3. Lofexidina [inn-spanish]
  4. Lofexidine hydrochloride
  5. Lofexidinum [inn-latin]
  6. lofexidine
Brand Names
  1. BritLofex
Brand Mixtures Not Available
Chemical IUPAC Name 2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
Chemical Formula C11H12Cl2N2O
Chemical Structure Structure
CAS Registry Number 31036-80-3
InChI Identifier InChI=1/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15)/f/h14H
InChI Key KSMAGQUYOIHWFS-YHMJCDSICQ
KEGG Drug Not Available
KEGG Compound Not Available
PubChem Compound 30668 Link Image
PubChem Substance 14774610 Link Image
ChEBI ID Not Available
PharmGKB ID Not Available
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available
RxList Link Not Available
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Lofexidine Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Not Available
Average Molecular Weight 259.1320
Monoisotopic Molecular Weight 258.0327
State Solid
Melting Point 127 oC
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility 1.47e-01 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity Not Available Source: PhysProp
Predicted LogP 3.31 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -3.25 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 C[C@H](OC1=C(Cl)C=CC=C1Cl)C1=NCCN1
Canonical SMILES CC(OC1=C(Cl)C=CC=C1Cl)C1=NCCN1
Drug Category
  • Adrenergic alpha-Agonists
  • Antihypertensive Agents
  • Narcotic Antagonists
ATC Codes Not Available
AHFS Codes Not Available
Indication Investigated for use/treatment in addictions and substance abuse.
Pharmacology Lofexidine is an orally active imidazoline adrenergic alpha-2-receptor agonist; and is believed to have a high affinity for 2A receptor subtypes resulting in less anti-hypertensive activity than clonidine, a non-selective alpha-2-receptor agonist. Hypotension may occur in susceptible subjects, accompanied by a decrease in heart rate. Abrupt discontinuation of lofexidine has been, in some cases, associated with a transient increase in blood pressure to higher than pre-treatment levels.
Mechanism of Action Lofexidine is an alpha2-adrenergic receptor agonist.
Absorption Lofexidine is extensively absorbed and achieves peak plasma concentration at 3 hours after administration of a single dose. Bioavailability is over 90% following oral administration.
Toxicity Lofexidine was tolerated at high dosage in singe dose toxicity studies in animals, the LD50 being >77 mg/kg. With repeat dosing in mice, rats and dogs symptoms related to the pharmacology of the drug (ataxia, sedation, tremor, unkempt appearance and exhaustion) appeared. Overdosage may cause hypotension, bradycardia and sedation.
Protein Binding 80–90%
Biotransformation Lofexidine undergoes extensive metabolism in the liver and excretion is mainly by the kidney.
Half Life 11 hours
Dosage Forms
Form Route
Tablet, film coated Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Walsh SL, Strain EC, Bigelow GE: Evaluation of the effects of lofexidine and clonidine on naloxone-precipitated withdrawal in opioid-dependent humans. Addiction. 2003 Apr;98(4):427-39. [PubMed Link Image]
  2. Manufacturer Website Link Image
  3. Wikipedia Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. Alpha-2A adrenergic receptor
  2. Alpha-2C adrenergic receptor
  3. Alpha-2B 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. Strang J, Bearn J, Gossop M: Lofexidine for opiate detoxification: review of recent randomised and open controlled trials. Am J Addict. 1999 Fall;8(4):337-48. [PubMed Link Image]
  2. Jin Y, Verstappen A, Elko E, Cammarata P, Yorio T: Effects of lofexidine, an alpha 2-adrenoreceptor agonist, on ocular blood flow and ion transport of rabbit iris-ciliary body. J Ocul Pharmacol. 1992 Spring;8(1):23-33. [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. Strang J, Bearn J, Gossop M: Lofexidine for opiate detoxification: review of recent randomised and open controlled trials. Am J Addict. 1999 Fall;8(4):337-48. [PubMed Link Image]
  2. Jin Y, Verstappen A, Elko E, Cammarata P, Yorio T: Effects of lofexidine, an alpha 2-adrenoreceptor agonist, on ocular blood flow and ion transport of rabbit iris-ciliary body. J Ocul Pharmacol. 1992 Spring;8(1):23-33. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 629
Target 3 Name Alpha-2B adrenergic receptor
Target 3 Synonyms
  1. Alpha-2 adrenergic receptor subtype C2
  2. Alpha-2B adrenoceptor
  3. Alpha-2B adrenoreceptor
Target 3 Gene Name ADRA2B
Target 3 Protein Sequence >Alpha-2B adrenergic receptor 
MDHQDPYSVQATAAIAAAITFLILFTIFGNALVILAVLTSRSLRAPQNLFLVSLAAADIL
VATLIIPFSLANELLGYWYFRRTWCEVYLALDVLFCTSSIVHLCAISLDRYWAVSRALEY
NSKRTPRRIKCIILTVWLIAAVISLPPLIYKGDQGPQPRGRPQCKLNQEAWYILASSIGS
FFAPCLIMILVYLRIYLIAKRSNRRGPRAKGGPGQGESKQPRPDHGGALASAKLPALASV
ASAREVNGHSKSTGEKEEGETPEDTGTRALPPSWAALPNSGQGQKEGVCGASPEDEAEEE
EEEEEEEEECEPQAVPVSPASACSPPLQQPQGSRVLATLRGQVLLGRGVGAIGGQWWRRR
AQLTREKRFTFVLAVVIGVFVLCWFPFFFSYSLGAICPKHCKVPHGLFQFFFWIGYCNSS
LNPVIYTIFNQDFRRAFRRILCRPWTQTAW
Target 3 Number of Residues 457
Target 3 Molecular Weight 49954
Target 3 Theoretical pI 8.52
Target 3 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 3 General Function Involved in alpha2-adrenergic receptor activity
Target 3 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 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 13-38
  • 50-75
  • 86-108
  • 131-153
  • 170-193
  • 373-396
  • 406-429
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 178198 Link Image
Target 3 UniProtKB/Swiss-Prot ID P18089 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name ADA2B_HUMAN Link Image
Target 3 PDB ID 1HOF Link Image
Target 3 PDB File Show
Target 3 3D Structure
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 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 3 GenBank Gene ID
Target 3 GeneCard ID ADRA2B Link Image
Target 3 GenAtlas ID ADRA2B Link Image
Target 3 HGNC ID HGNC:282 Link Image
Target 3 Chromosome Location 2
Target 3 Locus 2p13-q13
Target 3 SNPs SNPJam Report Link Image
Target 3 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 3 Drug References
  1. Strang J, Bearn J, Gossop M: Lofexidine for opiate detoxification: review of recent randomised and open controlled trials. Am J Addict. 1999 Fall;8(4):337-48. [PubMed Link Image]
  2. Jin Y, Verstappen A, Elko E, Cammarata P, Yorio T: Effects of lofexidine, an alpha 2-adrenoreceptor agonist, on ocular blood flow and ion transport of rabbit iris-ciliary body. J Ocul Pharmacol. 1992 Spring;8(1):23-33. [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.