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Showing drug card for Methadone (DB00333)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:06:25
Primary Accession Number DB00333
Secondary Accession Number
  • APRD00485
Name Methadone
Drug Type
  • Approved
  • Small Molecule
Description A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of morphine. It also has a depressant action on the cough center and may be given to control intractable cough associated with terminal lung cancer. Methadone is also used as part of the treatment of dependence on opioid drugs, although prolonged use of methadone itself may result in dependence. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3)
Synonyms
  1. (+/-)-Methadone
  2. (+/-)-Methadone hydrochloride
  3. DL-Methadone hydrochloride
  4. Methadon
  5. Methadone HCL
  6. Methadone hydrochloride
  7. Phenadone hydrochloride
  8. dl-Methadone
Brand Names
  1. (+/-)-Tussal
  2. Adanon
  3. Adanon hydrochloride
  4. Adolan
  5. Algidon
  6. Algolysin
  7. Algovetin
  8. Althose hydrochloride
  9. Amidon
  10. Amidone
  11. Biscuits
  12. Butalgin
  13. Depridol
  14. Diaminon
  15. Diaminon hydrochloride
  16. Dollies
  17. Dolly
  18. Dolofin hydrochloride
  19. Dolohepton
  20. Dolophin
  21. Dolophin hydrochloride
  22. Dolophine
  23. Dolophine HCL
  24. Fenadon
  25. Fenadone
  26. Heptadon
  27. Heptadone
  28. Heptanon
  29. Ketalgin
  30. Ketalgin hydrochloride
  31. Mecodin
  32. Mephenon
  33. Methadone HCL Intensol
  34. Methadone M
  35. Methadose
  36. Methaquaione
  37. Miadone
  38. Moheptan
  39. Phenadone
  40. Physeptone
  41. Polamidon
  42. Polamidone
  43. Tussol
  44. Westadone
Brand Mixtures Not Available
Chemical IUPAC Name 6-dimethylamino-4,4-di(phenyl)heptan-3-one
Chemical Formula C21H27NO
Chemical Structure Structure
CAS Registry Number 76-99-3
InChI Identifier InChI=1/C21H27NO/c1-5-20(23)21(16-17(2)22(3)4,18-12-8-6-9-13-18)19-14-10-7-11-15-19/h6-15,17H,5,16H2,1-4H3
InChI Key USSIQXCVUWKGNF-UHFFFAOYAH
KEGG Drug Not Available
KEGG Compound C07163 Link Image
PubChem Compound 4095 Link Image
PubChem Substance 149416 Link Image
ChEBI ID Not Available
PharmGKB ID PA450401 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02247698 Link Image
RxList Link http://www.rxlist.com/cgi/generic/methdone.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Methadone Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 309.4452
Monoisotopic Molecular Weight 309.2093
State Solid
Melting Point 235.0 oC
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility 5.90e-03 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 3.93 [HANSCH,C ET AL. (1995)] Source: PhysProp
Predicted LogP 4.14 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -4.72 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 8.94
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 CCC(=O)C(C[C@H](C)N(C)C)(C1=CC=CC=C1)C1=CC=CC=C1
Canonical SMILES CCC(=O)C(CC(C)N(C)C)(C1=CC=CC=C1)C1=CC=CC=C1
Drug Category
  • Analgesics
  • Analgesics, Opioid
  • Antitussive Agents
  • Antitussives
  • Narcotics
  • Opiate Agonists
ATC Codes
AHFS Codes
  • 28:08.08
Indication For the treatment of dry cough, drug withdrawal syndrome, opioid type drug dependence, and pain.
Pharmacology Methadone is a synthetic opioid analgesic with multiple actions quantitatively similar to those at morphine, the most prominent of which involve the central nervous system and organs composed of smooth muscle. However, Methadone is more active and more toxic than morphine. Methadone is indicated for relief of severe pain, for detoxification treatment of narcotic addiction, and for temporary maintenance treatment of narcotic addiction. The principal actions of therapeutic value are analgesia and sedation and detoxification or temporary maintenance in narcotic addiction. The Methadone abstinence syndrome, although qualitatively similar to that of morphine, differs in that the onset is slower, the course is more prolonged, and the symptoms are less severe.
Mechanism of Action Methadone is a mu-agonist; a synthetic opioid analgesic with multiple actions qualitatively similar to those of morphine, the most prominent of which involves the central nervous system and organs composed of smooth muscle. The principal therapeutic uses for methadone are for analgesia and for detoxification or maintenance in opioid addiction. The methadone abstinence syndrome, although qualitatively similar to that of morphine, differs in that the onset is slower, the course is more prolonged, and the symptoms are less severe. Some data also indicate that methadone acts as an antagonist at the N-methyl-D-aspartate (NMDA) receptor. The contribution of NMDA receptor antagonism to methadone's efficacy is unknown. Other NMDA receptor antagonists have been shown to produce neurotoxic effects in animals.
Absorption Well absorbed following oral administration. The bioavailability of methadone ranges between 36 to 100%.
Toxicity In severe overdosage, particularly by the intravenous route, apnea, circulatory collapse, cardiac arrest, and death may occur.
Protein Binding In plasma, methadone is predominantly bound to α1-acid glycoprotein (85% to 90%).
Biotransformation Hepatic. Cytochrome P450 enzymes, primarily CYP3A4, CYP2B6, and CYP2C19 and to a lesser extent CYP2C9 and CYP2D6, are responsible for conversion of methadone to EDDP and other inactive metabolites, which are excreted mainly in the urine.
Half Life 24-36 hours
Dosage Forms
Form Route
Liquid Oral
Solution Oral
Tablet Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Amobarbital The barbiturate decreases the effect of methadone
Amprenavir The protease inhibitor decreases the effect of methadone
Aprobarbital The barbiturate decreases the effect of methadone
Butabarbital The barbiturate decreases the effect of methadone
Butalbital The barbiturate decreases the effect of methadone
Butethal The barbiturate decreases the effect of methadone
Carbamazepine Carbamazepine decreases levels of methadone
Cimetidine Cimetidine increases the effect of the narcotic
Dihydroquinidine barbiturate The barbiturate decreases the effect of methadone
Efavirenz The antiretroviral agent decreases the effect of methadone
Ethotoin The hydantoin decreases the effect of methadone
Fluvoxamine Fluvoxamine increases the effect and toxicity of methadone
Fosamprenavir The protease inhibitor decreases the effect of methadone
Fosphenytoin The hydantoin decreases the effect of methadone
Heptabarbital The barbiturate decreases the effect of methadone
Hexobarbital The barbiturate decreases the effect of methadone
Mephenytoin The hydantoin decreases the effect of methadone
Methohexital The barbiturate decreases the effect of methadone
Methylphenobarbital The barbiturate decreases the effect of methadone
Naltrexone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals
Nelfinavir Nelfinavir decreases the effect of methadone
Nevirapine The antiretroviral agent decreases the effect of methadone
Pentobarbital The barbiturate decreases the effect of methadone
Phenobarbital The barbiturate decreases the effect of methadone
Phenytoin The hydantoin decreases the effect of methadone
Primidone The barbiturate decreases the effect of methadone
Quinidine barbiturate The barbiturate decreases the effect of methadone
Rifabutin The rifamycin decreases the effect of methadone
Rifampin The rifamycin decreases the effect of methadone
Rifapentine The rifamycin decreases the effect of methadone
Ritonavir The protease inhibitor decreases the effect of methadone
Secobarbital The barbiturate decreases the effect of methadone
St. John's Wort St. John's Wort decreases levels/effect of methadone
Talbutal The barbiturate decreases the effect of methadone
Zidovudine Methadone increases the effect and toxicity of zidovudine
Food Interactions
  • Take without regard to meals. Avoid alcohol. Usually diluted in fruit juice.
Pathways Not Available
General References
  1. Joseph H, Stancliff S, Langrod J: Methadone maintenance treatment (MMT): a review of historical and clinical issues. Mt Sinai J Med. 2000 Oct-Nov;67(5-6):347-64. [PubMed Link Image]
  2. Eap CB, Buclin T, Baumann P: Interindividual variability of the clinical pharmacokinetics of methadone: implications for the treatment of opioid dependence. Clin Pharmacokinet. 2002;41(14):1153-93. [PubMed Link Image]
  3. Donny EC, Brasser SM, Bigelow GE, Stitzer ML, Walsh SL: Methadone doses of 100 mg or greater are more effective than lower doses at suppressing heroin self-administration in opioid-dependent volunteers. Addiction. 2005 Oct;100(10):1496-509. [PubMed Link Image]
  4. Connock M, Juarez-Garcia A, Jowett S, Frew E, Liu Z, Taylor RJ, Fry-Smith A, Day E, Lintzeris N, Roberts T, Burls A, Taylor RS: Methadone and buprenorphine for the management of opioid dependence: a systematic review and economic evaluation. Health Technol Assess. 2007 Mar;11(9):1-171, iii-iv. [PubMed Link Image]
  5. Kell MJ: Utilization of plasma and urine methadone concentrations to optimize treatment in maintenance clinics: I. Measurement techniques for a clinical setting. J Addict Dis. 1994;13(1):5-26. [PubMed Link Image]
  6. Drugs.com Link Image
  7. Wikipedia Link Image
  8. RxList Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 2C19 (CYP2C19)
  2. Cytochrome P450 3A4 (CYP3A4)
  3. Cytochrome P450 2B6 (CYP2B6)
Targets
  1. Neuronal acetylcholine receptor subunit alpha-10
  2. Glutamate [NMDA] receptor subunit 3A
  3. Mu-type opioid receptor
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 2C19 (CYP2C19)
Enzyme 1 Gene Name CYP2C19
Enzyme 1 SwissProt ID P33261 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P33261|CP2CJ_HUMAN Cytochrome P450 2C19 (EC 1.14.13.80) 
MDPFVVLVLCLSCLLLLSIWRQSSGRGKLPPGPTPLPVIGNILQIDIKDVSKSLTNLSKI
YGPVFTLYFGLERMVVLHGYEVVKEALIDLGEEFSGRGHFPLAERANRGFGIVFSNGKRW
KEIRRFSLMTLRNFGMGKRSIEDRVQEEARCLVEELRKTKASPCDPTFILGCAPCNVICS
IIFQKRFDYKDQQFLNLMEKLNENIRIVSTPWIQICNNFPTIIDYFPGTHNKLLKNLAFM
ESDILEKVKEHQESMDINNPRDFIDCFLIKMEKEKQNQQSEFTIENLVITAADLLGAGTE
TTSTTLRYALLLLLKHPEVTAKVQEEIERVVGRNRSPCMQDRGHMPYTDAVVHEVQRYID
LIPTSLPHAVTCDVKFRNYLIPKGTTILTSLTSVLHDNKEFPNPEMFDPRHFLDEGGNFK
KSNYFMPFSAGKRICVGEGLARMELFLFLTFILQNFNLKSLIDPKDLDTTPVVNGFASVP
PFYQLCFIPV
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 2 Gene Name CYP3A4
Enzyme 2 SwissProt ID P08684 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Phase 1 Metabolizing Enzyme 3 [top]
Enzyme 3 Name Cytochrome P450 2B6 (CYP2B6)
Enzyme 3 Gene Name CYP2B6
Enzyme 3 SwissProt ID P20813 Link Image
Enzyme 3 SNPs SNPJam Report Link Image
Enzyme 3 Protein Sequence >sp|P20813|CP2B6_HUMAN Cytochrome P450 2B6 (EC 1.14.14.1) 
MELSVLLFLALLTGLLLLLVQRHPNTHDRLPPGPRPLPLLGNLLQMDRRGLLKSFLRFRE
KYGDVFTVHLGPRPVVMLCGVEAIREALVDKAEAFSGRGKIAMVDPFFRGYGVIFANGNR
WKVLRRFSVTTMRDFGMGKRSVEERIQEEAQCLIEELRKSKGALMDPTFLFQSITANIIC
SIVFGKRFHYQDQEFLKMLNLFYQTFSLISSVFGQLFELFSGFLKYFPGAHRQVYKNLQE
INAYIGHSVEKHRETLDPSAPKDLIDTYLLHMEKEKSNAHSEFSHQNLNLNTLSLFFAGT
ETTSTTLRYGFLLMLKYPHVAERVYREIEQVIGPHRPPELHDRAKMPYTEAVIYEIQRFS
DLLPMGVPHIVTQHTSFRGYIIPKDTEVFLILSTALHDPHYFEKPDAFNPDHFLDANGAL
KKTEAFIPFSLGKRICLGEGIARAELFLFFTTILQNFSMASPVAPEDIDLTPQECGVGKI
PPTYQIRFLPR
Drug Target 1 [top]
Target 1 ID 458
Target 1 Name Neuronal acetylcholine receptor subunit alpha-10
Target 1 Synonyms
  1. NACHR alpha 10
  2. Neuronal acetylcholine receptor subunit alpha-10 precursor
  3. Nicotinic acetylcholine receptor subunit alpha 10
Target 1 Gene Name CHRNA10
Target 1 Protein Sequence >Neuronal acetylcholine receptor protein subunit alpha-10 precursor 
MGLRSHHLSLGLLLLFLLPAECLGAEGRLALKLFRDLFANYTSALRPVADTDQTLNVTLE
VTLSQIIDMDERNQVLTLYLWIRQEWTDAYLRWDPNAYGGLDAIRIPSSLVWRPDIVLYN
KADAQPPGSASTNVVLRHDGAVRWDAPAITRSSCRVDVAAFPFDAQHCGLTFGSWTHGGH
QLDVRPRGAAASLADFVENVEWRVLGMPARRRVLTYGCCSEPYPDVTFTLLLRRRAAAYV
CNLLLPCVLISLLAPLAFHLPADSGEKVSLGVTVLLALTVFQLLLAESMPPAESVPLIGK
YYMATMTMVTFSTALTILIMNLHYCGPSVRPVPAWARALLLGHLARGLCVRERGEPCGQS
RPPELSPSPQSPEGGAGPPAGPCHEPRCLCRQEALLHHVATIANTFRSHRAAQRCHEDWK
RLARVMDRFFLAIFFSMALVMSLLVLVQAL
Target 1 Number of Residues 457
Target 1 Molecular Weight 49705
Target 1 Theoretical pI 7.97
Target 1 GO Classification
Function
excitatory extracellular ligand-gated ion channel activity
nicotinic acetylcholine-activated cation-selective channel activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
neurotransmitter receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
intrinsic to membrane
integral to membrane
cell
membrane
Target 1 General Function Involved in neurotransmitter receptor activity
Target 1 Specific Function Ionotropic receptor with a probable role in the modulation of auditory stimuli. Agonist binding may induce an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. In the ear, this may lead to a reduction in basilar membrane motion, altering the activity of auditory nerve fibers and reducing the range of dynamic hearing. This may protect against acoustic trauma
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • 1-24
Target 1 Transmembrane Regions
  • 238-258
  • 268-288
  • 302-322
  • 429-449
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 12053839 Link Image
Target 1 UniProtKB/Swiss-Prot ID Q9GZZ6 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name ACH10_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein (Probable)
Target 1 Gene Sequence >1353 bp 
ATGGGGCTCCGGAGCCACCACCTCAGCCTGGGCCTTCTGCTTCTGTTTCTACTCCCTGCA
GAGTGCCTGGGAGCTGAGGGCCGGCTGGCTCTCAAGCTGTTCCGTGACCTCTTTGCCAAC
TACACAAGTGCCCTGAGACCTGTGGCAGACACAGACCAGACTCTGAATGTGACCCTGGAG
GTGACACTGTCCCAGATCATCGATATGGATGAACGGAACCAGGTGCTGACCCTGTATCTG
TGGATACGGCAGGAGTGGACAGATGCCTACCTACGATGGGACCCCAATGCCTATGGTGGC
CTGGATGCCATCCGCATCCCCAGCAGTCTTGTGTGGCGGCCAGACATCGTACTCTATAAC
AAGGCCGACGCGCAGCCTCCAGGTTCCGCCAGCACCAACGTGGTCCTGCGCCACGATGGC
GCCGTGCGCTGGGACGCGCCGGCCATCACGCGCAGCTCGTGCCGCGTGGATGTAGCAGCC
TTCCCGTTCGACGCCCAGCACTGCGGCCTGACGTTCGGCTCCTGGACTCACGGCGGGCAC
CAACTGGATGTGCGGCCGCGCGGCGCTGCAGCCAGCCTGGCGGACTTCGTGGAGAACGTG
GAGTGGCGCGTGCTGGGCATGCCGGCGCGGCGGCGCGTGCTCACCTACGGCTGCTGCTCC
GAGCCCTACCCCGACGTCACCTTCACGCTGCTGCTGCGCCGCCGCGCCGCCGCCTACGTG
TGCAACCTGCTGCTGCCCTGCGTGCTCATCTCGCTGCTTGCGCCGCTCGCCTTCCACCTG
CCTGCCGACTCAGGCGAGAAGGTGTCGCTGGGCGTCACCGTGCTGCTGGCGCTCACCGTC
TTCCAGTTGCTGCTGGCCGAGAGCATGCCACCGGCCGAGAGCGTGCCGCTCATCGGGAAG
TATTACATGGCCACTATGACCATGGTCACATTCTCAACAGCACTCACCATCCTTATCATG
AACCTGCATTACTGTGGTCCCAGTGTCCGCCCAGTGCCAGCCTGGGCTAGGGCCCTCCTG
CTGGGACACCTGGCACGGGGCCTGTGCGTGCGGGAAAGAGGGGAGCCCTGTGGGCAGTCC
AGGCCACCTGAGTTATCTCCTAGCCCCCAGTCGCCTGAAGGAGGGGCTGGCCCCCCAGCG
GGCCCTTGCCACGAGCCACGATGTCTGTGCCGCCAGGAAGCCCTACTGCACCACGTAGCC
ACCATTGCCAATACCTTCCGCAGCCACCGAGCTGCCCAGCGCTGCCATGAGGACTGGAAG
CGCCTGGCCCGTGTGATGGACCGCTTCTTCCTGGCCATCTTCTTCTCCATGGCCCTGGTC
ATGAGCCTCCTGGTGCTGGTGCAGGCCCTGTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID CHRNA10 Link Image
Target 1 GenAtlas ID CHRNA10 Link Image
Target 1 HGNC ID HGNC:13800 Link Image
Target 1 Chromosome Location 11
Target 1 Locus 11p15.5
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Lustig LR, Peng H, Hiel H, Yamamoto T, Fuchs PA: Molecular cloning and mapping of the human nicotinic acetylcholine receptor alpha10 (CHRNA10). Genomics. 2001 May 1;73(3):272-83. [PubMed Link Image]
  2. Sgard F, Charpantier E, Bertrand S, Walker N, Caput D, Graham D, Bertrand D, Besnard F: A novel human nicotinic receptor subunit, alpha10, that confers functionality to the alpha9-subunit. Mol Pharmacol. 2002 Jan;61(1):150-9. [PubMed Link Image]
Target 1 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 2 [top]
Target 2 ID 706
Target 2 Name Glutamate [NMDA] receptor subunit 3A
Target 2 Synonyms
  1. Glutamate receptor subunit 3A precursor
  2. N-methyl-D-aspartate receptor subtype NR3A
  3. NMDAR-L
Target 2 Gene Name GRIN3A
Target 2 Protein Sequence >Glutamate [NMDA] receptor subunit 3A precursor 
MRRLSLWWLLSRVCLLLPPPCALVLAGVPSSSSHPQPCQILKRIGHAVRVGAVHLQPWTT
APRAASRAPDDSRAGAQRDEPEPGTRRSPAPSPGARWLGSTLHGRGPPGSRKPGEGARAE
ALWPRDALLFAVDNLNRVEGLLPYNLSLEVVMAIEAGLGDLPLLPFSSPSSPWSSDPFSF
LQSVCHTVVVQGVSALLAFPQSQGEMMELDLVSLVLHIPVISIVRHEFPRESQNPLHLQL
SLENSLSSDADVTVSILTMNNWYNFSLLLCQEDWNITDFLLLTQNNSKFHLGSIINITAN
LPSTQDLLSFLQIQLESIKNSTPTVVMFGCDMESIRRIFEITTQFGVMPPELRWVLGDSQ
NMEELRTEGLPLGLIAHGKTTQSVFEHYVQDAMELVARAVATATMIQPELALIPSTMNCM
EVETTNLTSGQYLSRFLANTTFRGLSGSIRVKGSTIVSSENNFFIWNLQHDPMGKPMWTR
LGSWQGRKIVMDYGIWPEQAQRHKTHFQHPSKLHLRVVTLIEHPFVFTREVDDEGLCPAG
QLCLDPMTNDSSTLDSLFSSLHSSNDTVPIKFKKCCYGYCIDLLEKIAEDMNFDFDLYIV
GDGKYGAWKNGHWTGLVGDLLRGTAHMAVTSFSINTARSQVIDFTSPFFSTSLGILVRTR
DTAAPIGAFMWPLHWTMWLGIFVALHITAVFLTLYEWKSPFGLTPKGRNRSKVFSFSSAL
NICYALLFGRTVAIKPPKCWTGRFLMNLWAIFCMFCLSTYTANLAAVMVGEKIYEELSGI
HDPKLHHPSQGFRFGTVRESSAEDYVRQSFPEMHEYMRRYNVPATPDGVEYLKNNPEKLD
AFIMDKALLDYEVSIDADCKLLTVGKPFAIEGYGIGLPPNSPLTANISELISQYKSHGFM
DMLHDKWYRVVPCGKRSFAVTETLQMGIKHFSGLFVLLCIGFGLSILTTIGEHIVYRLLL
PRIKNKSKLQYWLHTSQRLHRAINTSFIEEKQQHFKTKRVEKRSNVGPRQLTVWNTSNLS
HDNRRKYIFSDEEGQNQLGIRIHQDIPLPPRRRELPALRTTNGKADSLNVSRNSVMQELS
ELEKQIQVIRQELQLAVSRKTELEEYQRTSRTCES
Target 2 Number of Residues 1133
Target 2 Molecular Weight 125597
Target 2 Theoretical pI 7.81
Target 2 GO Classification
Function
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
excitatory extracellular ligand-gated ion channel activity
glutamate-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
glutamate receptor activity
ionotropic glutamate receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
cell
membrane
Target 2 General Function Involved in ionotropic glutamate receptor activity
Target 2 Specific Function NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine. May play a role in the development of dendritic spines. May play a role in PPP2CB-NMDAR mediated signaling mechanism
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • 1-23
Target 2 Transmembrane Regions
  • 675-695
  • 749-769
  • 931-951
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 20372905 Link Image
Target 2 UniProtKB/Swiss-Prot ID Q8TCU5 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name NMD3A_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Cell membrane
  • multi-pass membrane protein. Enriched in post-synaptic plasma membrane and post-synap
Target 2 Gene Sequence >3348 bp 
ATGAGGAGACTGAGTTTGTGGTGGCTGCTGAGCAGGGTCTGTCTGCTGTTGCCGCCGCCC
TGCGCACTGGTGCTGGCCGGGGTGCCCAGCTCCTCCTCGCACCCGCAGCCCTGCCAGATC
CTCAAGCGCATCGGGCACGCGGTGAGGGTGGGCGCGGTGCACTTGCAGCCCTGGACCACC
GCCCCCCGCGCGGCCAGCCGCGCTCCGGACGACAGCCGAGCAGGAGCCCAGAGGGATGAG
CCGGAGCCAGGGACTAGGCGGTCCCCGGCGCCCTCGCCGGGCGCACGCTGGTTGGGGAGC
ACCCTGCATGGCCGGGGGCCGCCGGGCTCCCGTAAGCCCGGGGAGGGCGCCAGGGCGGAG
GCCCTGTGGCCACGGGACGCCCTCCTATTTGCCGTGGACAACCTGAACCGCGTGGAAGGG
CTGCTACCCTACAACCTGTCTTTGGAAGTAGTGATGGCCATCGAGGCAGGCCTGGGCGAT
CTGCCACTTTTGCCCTTCTCCTCCCCTAGTTCGCCATGGAGCAGTGACCCTTTCTCCTTC
CTGCAAAGTGTGTGCCATACCGTGGTGGTGCAAGGGGTGTCGGCGCTGCTCGCCTTCCCC
CAGAGCCAGGGCGAAATGATGGAGCTCGACTTGGTCAGCTTAGTCCTGCACATTCCAGTG
ATCAGCATCGTGCGCCACGAGTTTCCGCGGGAGAGTCAGAATCCCCTTCACCTACAACTG
AGTTTAGAAAATTCATTAAGTTCTGATGCTGATGTCACTGTCTCAATCCTGACCATGAAC
AACTGGTACAATTTTAGCTTGTTGCTGTGCCAGGAAGACTGGAACATCACCGACTTCCTC
CTCCTTACCCAGAATAATTCCAAGTTCCACCTTGGTTCTATCATCAACATCACCGCTAAC
CTCCCCTCCACCCAGGACCTCTTGAGCTTCCTACAGATCCAGCTTGAGAGTATTAAGAAC
AGCACACCCACAGTGGTGATGTTTGGCTGCGACATGGAAAGTATCCGGCGGATTTTCGAA
ATTACAACCCAGTTTGGGGTCATGCCCCCTGAACTTCGTTGGGTGCTGGGAGATTCCCAG
AATATGGAGGAACTGAGGACAGAGGGTCTGCCCTTAGGACTCATTGCTCATGGAAAAACA
ACACAGTCTGTCTTTGAGCACTACGTACAAGATGCTATGGAGCTGGTCGCAAGAGCTGTA
GCCACAGCCACCATGATCCAACCAGAACTTGCTCTCATTCCCAGCACGATGAACTGCATG
GAGGTGGAAACTACAAATCTCACTTCAGGACAATATTTATCAAGGTTTCTAGCCAATACC
ACTTTCAGAGGCCTCAGTGGTTCCATCAGAGTAAAAGGTTCCACCATCGTCAGCTCAGAA
AACAACTTTTTCATCTGGAATCTTCAACATGACCCCATGGGAAAGCCAATGTGGACCCGC
TTGGGCAGCTGGCAGGGGAGAAAGATTGTCATGGACTATGGAATATGGCCAGAGCAGGCC
CAGAGACACAAAACCCACTTCCAACATCCAAGTAAGCTACACTTGAGAGTGGTTACCCTG
ATTGAGCATCCTTTTGTCTTCACAAGGGAGGTAGATGATGAAGGCTTGTGCCCTGCTGGC
CAACTCTGTCTAGACCCCATGACTAATGACTCTTCCACACTGGACAGCCTTTTTAGCAGC
CTCCATAGCAGTAATGATACAGTGCCCATTAAATTCAAGAAGTGCTGCTATGGATATTGC
ATTGATCTGCTGGAAAAGATAGCAGAAGACATGAACTTTGACTTCGACCTCTATATTGTA
GGGGATGGAAAGTATGGAGCCTGGAAAAATGGGCACTGGACTGGGCTAGTGGGTGATCTC
CTGAGAGGGACTGCCCACATGGCAGTCACTTCCTTTAGCATCAATACTGCACGGAGCCAG
GTGATAGATTTCACCAGCCCTTTCTTCTCCACCAGCTTGGGCATCTTAGTGAGGACCCGA
GATACAGCAGCTCCCATTGGAGCCTTCATGTGGCCACTCCACTGGACAATGTGGCTGGGG
ATTTTTGTGGCTCTGCACATCACTGCCGTCTTCCTCACTCTGTATGAATGGAAGAGTCCA
TTTGGTTTGACTCCCAAGGGGCGAAATAGAAGTAAAGTCTTCTCCTTTTCTTCAGCCTTG
AACATCTGTTATGCCCTCTTGTTTGGCAGAACAGTGGCCATCAAACCTCCAAAATGTTGG
ACTGGAAGGTTTCTAATGAACCTTTGGGCCATTTTCTGTATGTTTTGCCTTTCCACATAC
ACGGCAAACTTGGCTGCTGTCATGGTAGGTGAGAAGATCTATGAAGAGCTTTCTGGAATA
CATGACCCCAAGTTACATCATCCTTCCCAAGGATTCCGCTTTGGAACTGTCCGAGAAAGC
AGTGCTGAAGATTATGTGAGACAAAGTTTCCCAGAGATGCATGAATATATGAGAAGGTAC
AATGTTCCAGCCACCCCTGATGGAGTGGAGTATCTGAAGAACAATCCAGAGAAACTAGAC
GCCTTCATCATGGACAAAGCCCTTCTGGATTATGAAGTGTCAATAGATGCTGACTGCAAA
CTTCTCACTGTGGGGAAGCCATTTGCCATAGAAGGATACGGCATTGGCCTCCCACCCAAC
TCTCCATTGACCGCCAACATATCCGAGCTAATCAGTCAATACAAGTCACATGGGTTTATG
GATATGCTCCATGACAAGTGGTACAGGGTGGTTCCCTGTGGCAAGAGAAGTTTTGCTGTC
ACGGAGACTTTGCAAATGGGCATCAAACACTTCTCTGGGCTCTTTGTGCTGCTGTGCATT
GGATTTGGTCTGTCCATTTTGACCACCATTGGTGAGCACATAGTATACAGGCTGCTGCTA
CCACGAATCAAAAACAAATCCAAGCTGCAATACTGGCTCCACACCAGCCAGAGATTACAC
AGAGCAATAAATACATCATTTATAGAGGAAAAGCAGCAGCATTTCAAGACCAAACGTGTG
GAAAAGAGGTCTAATGTGGGACCCCGTCAGCTTACCGTATGGAATACTTCCAATCTGAGT
CATGACAACCGACGGAAATACATCTTTAGTGATGAGGAAGGACAAAACCAGCTGGGCATC
CGGATCCACCAGGACATCCCCCTCCCTCCAAGGAGAAGAGAGCTCCCTGCCTTGCGGACC
ACCAATGGGAAAGCAGACTCCCTAAATGTATCTCGGAACTCAGTGATGCAGGAACTCTCA
GAGCTCGAGAAGCAGATTCAGGTGATCCGTCAGGAGCTGCAGCTGGCTGTGAGCAGGAAA
ACGGAGCTGGAGGAGTATCAAAGGACAAGTCGGACTTGTGAGTCCTAG
Target 2 GenBank Gene ID
Target 2 GeneCard ID GRIN3A Link Image
Target 2 GenAtlas ID GRIN3A Link Image
Target 2 HGNC ID HGNC:16767 Link Image
Target 2 Chromosome Location 9
Target 2 Locus 9q31.1
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Andersson O, Stenqvist A, Attersand A, von Euler G: Nucleotide sequence, genomic organization, and chromosomal localization of genes encoding the human NMDA receptor subunits NR3A and NR3B. Genomics. 2001 Dec;78(3):178-84. [PubMed Link Image]
  2. Nagase T, Kikuno R, Ohara O: Prediction of the coding sequences of unidentified human genes. XXII. The complete sequences of 50 new cDNA clones which code for large proteins. DNA Res. 2001 Dec 31;8(6):319-27. [PubMed Link Image]
  3. Eriksson M, Nilsson A, Froelich-Fabre S, Akesson E, Dunker J, Seiger A, Folkesson R, Benedikz E, Sundstrom E: Cloning and expression of the human N-methyl-D-aspartate receptor subunit NR3A. Neurosci Lett. 2002 Mar 22;321(3):177-81. [PubMed Link Image]
Target 2 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 3 [top]
Target 3 ID 847
Target 3 Name Mu-type opioid receptor
Target 3 Synonyms
  1. MOR-1
Target 3 Gene Name OPRM1
Target 3 Protein Sequence >Mu-type opioid receptor 
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP
PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT
STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF
RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI
FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI
YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI
EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
Target 3 Number of Residues 406
Target 3 Molecular Weight 44780
Target 3 Theoretical pI 8.29
Target 3 GO Classification
Function
peptide receptor activity, G-protein coupled
opioid receptor activity
mu-opioid receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like 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 rhodopsin-like receptor activity
Target 3 Specific Function Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for beta-endorphin
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 67-96
  • 106-123
  • 146-165
  • 196-211
  • 237-259
  • 283-305
  • 314-330
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 452073 Link Image
Target 3 UniProtKB/Swiss-Prot ID P35372 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name OPRM_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >1203 bp 
ATGGACAGCAGCGCTGCCCCCACGAACGCCAGCAATTGCACTGATGCCTTGGCGTACTCA
AGTTGCTCCCCAGCACCCAGCCCCGGTTCCTGGGTCAACTTGTCCCACTTAGATGGCAAC
CTGTCCGACCCATGCGGTCCGAACCGCACCAACCTGGGCGGGAGAGACAGCCTGTGCCCT
CCGACCGGCAGTCCCTCCATGATCACGGCCATCACGATCATGGCCCTCTACTCCATCGTG
TGCGTGGTGGGGCTCTTCGGAAACTTCCTGGTCATGTATGTGATTGTCAGATACACCAAG
ATGAAGACTGCCACCAACATCTACATTTTCAACCTTGCTCTGGCAGATGCCTTAGCCACC
AGTACCCTGCCCTTCCAGAGTGTGAATTACCTAATGGGAACATGGCCATTTGGAACCATC
CTTTGCAAGATAGTGATCTCCATAGATTACTATAACATGTTCACCAGCATATTCACCCTC
TGCACCATGAGTGTTGATCGATACATTGCAGTCTGCCACCCTGTCAAGGCCTTAGATTTC
CGTACTCCCCGAAATGCCAAAATTATCAATGTCTGCAACTGGATCCTCTCTTCAGCCATT
GGTCTTCCTGTAATGTTCATGGCTACAACAAAATACAGGCAAGGTTCCATAGATTGTACA
CTAACATTCTCTCATCCAACCTGGTACTGGGAAAACCTCGTGAAGATCTGTGTTTTCATC
TTCGCCTTCATTATGCCAGTGCTCATCATTACCGTGTGCTATGGACTGATGATCTTGCGC
CTCAAGAGTGTCCGCATGCTCTCTGGCTCCAAAGAAAAGGACAGGAATCTTCGAAGGATC
ACCAGGATGGTGCTGGTGGTGGTGGCTGTGTTCATCGTCTGCTGGACTCCCATTCACATT
TACGTCATCATTAAAGCCTTGGTTACAATCCCAGAAACTACGTTCCAGACTGTTTCTTGG
CACTTCTGCATTGCTCTAGGTTACACAAACAGCTGCCTCAACCCAGTCCTTTATGCATTT
CTGGATGAAAACTTCAAACGATGCTTCAGAGAGTTCTGTATCCCAACCTCTTCCAACATT
GAGCAACAAAACTCCACTCGAATTCGTCAGAACACTAGAGACCACCCCTCCACGGCCAAT
ACAGTGGATAGAACTAATCATCAGCTAGAAAATCTGGAAGCAGAAACTGCTCCGTTGCCC
TAA
Target 3 GenBank Gene ID
Target 3 GeneCard ID OPRM1 Link Image
Target 3 GenAtlas ID OPRM1 Link Image
Target 3 HGNC ID HGNC:8156 Link Image
Target 3 Chromosome Location 6
Target 3 Locus 6q24-q25
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Uhl GR, Sora I, Wang Z: The mu opiate receptor as a candidate gene for pain: polymorphisms, variations in expression, nociception, and opiate responses. Proc Natl Acad Sci U S A. 1999 Jul 6;96(14):7752-5. [PubMed Link Image]
  2. Chuang TK, Killam KF Jr, Chuang LF, Kung HF, Sheng WS, Chao CC, Yu L, Chuang RY: Mu opioid receptor gene expression in immune cells. Biochem Biophys Res Commun. 1995 Nov 22;216(3):922-30. [PubMed Link Image]
  3. Mestek A, Hurley JH, Bye LS, Campbell AD, Chen Y, Tian M, Liu J, Schulman H, Yu L: The human mu opioid receptor: modulation of functional desensitization by calcium/calmodulin-dependent protein kinase and protein kinase C. J Neurosci. 1995 Mar;15(3 Pt 2):2396-406. [PubMed Link Image]
  4. Wang JB, Johnson PS, Persico AM, Hawkins AL, Griffin CA, Uhl GR: Human mu opiate receptor. cDNA and genomic clones, pharmacologic characterization and chromosomal assignment. FEBS Lett. 1994 Jan 31;338(2):217-22. [PubMed Link Image]
  5. Bare LA, Mansson E, Yang D: Expression of two variants of the human mu opioid receptor mRNA in SK-N-SH cells and human brain. FEBS Lett. 1994 Nov 7;354(2):213-6. [PubMed Link Image]
  6. Bergen AW, Kokoszka J, Peterson R, Long JC, Virkkunen M, Linnoila M, Goldman D: Mu opioid receptor gene variants: lack of association with alcohol dependence. Mol Psychiatry. 1997 Oct-Nov;2(6):490-4. [PubMed Link Image]
  7. Bond C, LaForge KS, Tian M, Melia D, Zhang S, Borg L, Gong J, Schluger J, Strong JA, Leal SM, Tischfield JA, Kreek MJ, Yu L: Single-nucleotide polymorphism in the human mu opioid receptor gene alters beta-endorphin binding and activity: possible implications for opiate addiction. Proc Natl Acad Sci U S A. 1998 Aug 4;95(16):9608-13. [PubMed Link Image]
Target 3 Drug References
  1. Shi J, Hui L, Xu Y, Wang F, Huang W, Hu G: Sequence variations in the mu-opioid receptor gene (OPRM1) associated with human addiction to heroin. Hum Mutat. 2002 Apr;19(4):459-60. [PubMed Link Image]
  2. Kvam TM, Baar C, Rakvag TT, Kaasa S, Krokan HE, Skorpen F: Genetic analysis of the murine mu opioid receptor: increased complexity of Oprm gene splicing. J Mol Med. 2004 Apr;82(4):250-5. Epub 2004 Jan 9. [PubMed Link Image]
  3. 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]
  4. 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]
  5. Kakko J, von Wachenfeldt J, Svanborg KD, Lidstrom J, Barr CS, Heilig M: Mood and Neuroendocrine Response to a Chemical Stressor, Metyrapone, in Buprenorphine-Maintained Heroin Dependence. Biol Psychiatry. 2007 Sep 10;. [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.