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Showing drug card for Dextromethorphan (DB00514)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-04-16 16:47:46
Primary Accession Number DB00514
Secondary Accession Number
  • APRD00655
Name Dextromethorphan
Drug Type
  • Approved
  • Small Molecule
Description The d-isomer of the codeine analog of levorphanol. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (receptors, N-methyl-D-aspartate) and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity. [PubChem]
Synonyms
  1. D-Methorphan
  2. D-Methorphan Hydrobromide
  3. Delta-Methorphan
  4. Demorphan
  5. Demorphan Hydrobromide
  6. Demorphine
  7. Destrometerfano [Dcit]
  8. Dextromethorfan [Czech]
  9. Dextromethorphan Bromhydrate
  10. Dextromethorphan Bromide
  11. Dextrometorfano [INN-Spanish]
  12. Dextrometorphan
  13. Dextromorphan
  14. Dexyromethorphan
  15. L-Methorphan
  16. Levomethorphan
  17. Levomethorphan [Ban:Dcf:Inn]
  18. Levomethorphane [INN-French]
  19. Levomethorphanum [INN-Latin]
  20. Levometorfano [INN-Spanish]
Brand Names
  1. Antussan
  2. Balminil DM
  3. Balminil DM Children
  4. Benylin Adult Formula Cough Suppressant
  5. Benylin DM
  6. Benylin DM 12 Hour
  7. Benylin DM for Children
  8. Benylin DM for Children 12 Hour
  9. Benylin Pediatric Cough Suppressant
  10. Calmylin #1
  11. Canfodion
  12. Cosylan
  13. Cough-X
  14. Creo-Terpin
  15. Delsym
  16. Delsym Cough Formula
  17. Diabe-Tuss DM Syrup
  18. Dormetan
  19. Dormethan
  20. Hihustan M.
  21. Hold DM
  22. Koffex DM
  23. Medicon
  24. Methorate Hydrobromide
  25. Methorphan
  26. Metrorat
  27. Novahistex DM
  28. Novahistine DM
  29. Pertussin CS Children's Strength
  30. Pertussin DM Extra Strength
  31. Robitussin Maximum Strength Cough Suppressant
  32. Robitussin Pediatric
  33. Robitussin Pediatric Cough Suppressant
  34. Romilar
  35. Sucrets 4 Hour Cough Suppressant
  36. Triaminic DM Long Lasting for Children
  37. Trocal
  38. Tusilan
  39. Tussade
  40. Vicks 44 Cough Relief
Brand Mixtures
  1. Actifed Dm Syrup (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride + Triprolidine Hydrochloride)
  2. Actifed Dm Tablets (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride + Triprolidine Hydrochloride)
  3. Antitussive Decong Antihistamine Syr (Dextromethorphan Hydrobromide + Pheniramine Maleate + Phenylpropanolamine Hydrochloride + Pyrilamine Maleate)
  4. Benylin 4 Flu - Syrup (Acetaminophen + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  5. Biohisdex Dm Decongestant (Dextromethorphan Hydrobromide + Diphenylpyraline Hydrochloride + Phenylephrine Hydrochloride)
  6. Biohisdine Dm Decongestant (Dextromethorphan Hydrobromide + Diphenylpyraline Hydrochloride + Phenylephrine Hydrochloride)
  7. Bronchodex Fort-Dm Syr (Ammonium Chloride + Dextromethorphan Hydrobromide + Menthol + Pyrilamine Maleate + Sodium Citrate)
  8. Bronchodex Pediatrique (Dextromethorphan Hydrobromide + Guaifenesin + Pheniramine Maleate + Pseudoephedrine Hydrochloride)
  9. Bronchosirum Pour Enfants (Dextromethorphan Hydrobromide + Pheniramine Maleate + Phenylpropanolamine Hydrochloride + Pyrilamine Maleate)
  10. Calmylin #2 Syr (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  11. Calmylin #3 Syr (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  12. Calmylin #4 Syr (Ammonium Chloride + Dextromethorphan Hydrobromide + Diphenhydramine Hydrochloride)
  13. Calmylin Cough and Flu Liq (Acetaminophen + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  14. Calmylin Pediatric Syrup (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  15. Centracol Dm - Syr (Dextromethorphan Hydrobromide + Pheniramine Maleate + Phenylpropanolamine Hydrochloride + Pyrilamine Maleate)
  16. Centracol Pediatrique - Syr (Dextromethorphan Hydrobromide + Guaifenesin + Pheniramine Maleate + Pseudoephedrine Hydrochloride)
  17. Chemhisdex Dm Decongestant (Dextromethorphan Hydrobromide + Diphenylpyraline Hydrochloride + Phenylephrine Hydrochloride)
  18. Chemhisdine Dm Decongestant (Dextromethorphan Hydrobromide + Diphenylpyraline Hydrochloride + Phenylephrine Hydrochloride)
  19. Children's Tussin Cough Medicine Dm Antitussive Decongestant (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  20. Children's Tylenol Cold Liquid with Dm (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  21. Citron Chaud Dm Cumberland Pws (Dextromethorphan Hydrobromide + Pheniramine Maleate + Phenylephrine Hydrochloride + Vitamin C)
  22. Cold Relief Dm (Brompheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  23. Cold/Flu Relief (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  24. Contac Cough Cold and Flu Caplets (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  25. Cough Syrup Dm Decongestant (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  26. Cough Syrup Dm Decongestant Expectorant (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  27. Cough Syrup Dm Decongestant for Children (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  28. Cough Syrup Dm Expectorant (Dextromethorphan Hydrobromide + Guaifenesin)
  29. Cough Syrup Dm-D-E (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  30. Cough Syrup Dm-E (Dextromethorphan Hydrobromide + Guaifenesin)
  31. Cough Syrup Dm-Expectorant (Dextromethorphan Hydrobromide + Guaifenesin)
  32. Cough Syrup W.Guaifenesin W.Dextromethorphan (Dextromethorphan Hydrobromide + Guaifenesin)
  33. Cough and Flu Syrup (Acetaminophen + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  34. Cough, Cold & Allergy Relief (Brompheniramine Maleate + Dextromethorphan Hydrobromide + Phenylephrine Hydrochloride + Phenylpropanolamine Hydrochloride)
  35. Dayquil Liquicaps (Acetaminophen + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  36. Dayquil Liquicaps - Cap (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  37. Dayquil Medicine - Liq (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  38. Daytime Cold & Flu Liquid Capsules (Acetaminophen + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  39. Daytime Liquid - Liq (Acetaminophen + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  40. Demdec Syr (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  41. Dimetapp Children's Cough and Cold Liquid (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  42. Dimetapp Cough & Cold Liqui-Gels - Cap (Brompheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  43. Dimetapp Cough, Cold & Flu (Acetaminophen + Brompheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  44. Dimetapp Dm Elixir (Brompheniramine Maleate + Dextromethorphan Hydrobromide + Phenylephrine Hydrochloride + Phenylpropanolamine Hydrochloride)
  45. Dimetapp Dm Tab (Brompheniramine Maleate + Dextromethorphan Hydrobromide + Phenylephrine Hydrochloride + Phenylpropanolamine Hydrochloride)
  46. Dm Cough Syr (Ammonium Chloride + Dextromethorphan Hydrobromide + Diphenhydramine Hydrochloride)
  47. Dm Cough Syrup Decongestant (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  48. Dm Cough Syrup Expectorant (Dextromethorphan Hydrobromide + Guaifenesin)
  49. Dm Expectorant Cough Syrup (Dextromethorphan Hydrobromide + Guaifenesin)
  50. Dm Plus Cough Syrup (Ammonium Chloride + Dextromethorphan Hydrobromide + Diphenhydramine Hydrochloride)
  51. Dm Plus Decongestant Cough Syrup (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  52. Dm Plus Decongestant Plus Expector.Ex.St.Syr (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  53. Dm Plus Decongestant Plus Expectorant Cough Syrup (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  54. Dm Plus Expectorant Syrup (Dextromethorphan Hydrobromide + Guaifenesin)
  55. Dm Syrup (Ammonium Chloride + Dextromethorphan Hydrobromide + Diphenhydramine Hydrochloride)
  56. Dm-D-Expectorant Cough and Cold Syrup (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  57. Extra Strength Cold Medication Daytime Rlf (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  58. Extra Strength Daytime Cold Relief-Caplet (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  59. Extra Strength Nighttime Cold Relief-Caplet (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  60. Extra Strength Tylenol Cold and Flu Powder (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  61. Hot Lemon Relief Dm Adult (Dextromethorphan Hydrobromide + Pheniramine Maleate + Phenylephrine Hydrochloride)
  62. Koffex Dm + Decongestant + Expectorant (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  63. Koffex Dm + Decongestant + Expectorant Extra Strength (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  64. Koffex Dm + Decongestant Syrup (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  65. Koffex Dm + Expectorant (Dextromethorphan Hydrobromide + Guaifenesin)
  66. Koffex Dm + Expectorant Extra Strength (Dextromethorphan Hydrobromide + Guaifenesin)
  67. Koffex Dm-D-E - Liq (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  68. Metrate (Dextromethorphan Hydrobromide + Diphenylpyraline Hydrochloride + Potassium Iodide + Sodium Citrate)
  69. Neo Citran Daycaps Extra Strength - Caplet (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  70. Nighttime Cold and Flu Liquid Capsules (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
  71. Nighttime Cold and Flu Relief (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
  72. Nitetime Cold Medicine (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
  73. Novahistex Dm Expectorant with Decongestant (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  74. Novahistex Dm with Decongestant (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  75. Novahistine Dm Expectorant with Decongestant (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  76. Novahistine Dm with Decongestant - Liq (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  77. Nyquil Liquicaps (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
  78. Ornade Dm 10 Liq (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  79. Ornade Dm 15 Liq (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  80. Ornade Dm 30 Liq (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  81. Pediatric Cough Syrup (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  82. Personnelle Dm Syr (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  83. Pharmacol Dm Syr (Dextromethorphan Hydrobromide + Pheniramine Maleate + Phenylpropanolamine Hydrochloride + Pyrilamine Maleate)
  84. Pharminicol Dm Syrup (Dextromethorphan Hydrobromide + Pheniramine Maleate + Phenylpropanolamine Hydrochloride + Pyrilamine Maleate)
  85. Pharmitussin Dm (Dextromethorphan Hydrobromide + Guaifenesin)
  86. Promatussin Dm Adult Formula Syr (Dextromethorphan Hydrobromide + Promethazine Hydrochloride + Pseudoephedrine Hydrochloride)
  87. Promatussin Dm Children Formula (Dextromethorphan Hydrobromide + Promethazine Hydrochloride + Pseudoephedrine Hydrochloride)
  88. Reg.Str.Cold Medic. (Night Time Relief)Caplet (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  89. Regular Strength Cold Medication (Daytime R.) (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  90. Regular Strength Tylenol Cold Chest Congestion (Acetaminophen + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  91. Regular Strength Tylenol Cold and Flu Powder (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  92. Regular Strength Tylenol Cough Suspension (Acetaminophen + Dextromethorphan Hydrobromide)
  93. Regular Strength Tylenol Cough Suspension with Decongestant (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  94. Robitussin Honey Cough and Cold (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  95. Robitussin Honey Flu (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  96. Sudafed Cold and Cough Extra Strength Caplet (Acetaminophen + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  97. Sudafed Cold and Flu Gel Caps (Acetaminophen + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  98. Sudafed Dm (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  99. Tantacol Dm Syr (Dextromethorphan Hydrobromide + Pheniramine Maleate + Phenylpropanolamine Hydrochloride + Pyrilamine Maleate)
  100. Theraflu Flu Cold and Cough Medicine (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  101. Triaminic Dm Daytime Syr (Dextromethorphan Hydrobromide + Guaifenesin + Phenylpropanolamine Hydrochloride)
  102. Triaminic Dm Expectorant Syr (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  103. Triaminic Dm Plus Decongestant Syrup (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  104. Triaminic Dm+Decongestant Liqui-Gels Capsules (Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  105. Triaminicol Dm Syrup (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  106. Tussin Cough Medicine Dm Antitussive Expectorant Decongestant (Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
Chemical IUPAC Name Not Available
Chemical Formula C18H25NO
Chemical Structure Structure
CAS Registry Number 125-71-3
InChI Identifier InChI=1/C18H25NO/c1-19-10-9-18-8-4-3-5-15(18)17(19)11-13-6-7-14(20-2)12-16(13)18/h6-7,12,15,17H,3-5,8-11H2,1-2H3/t15-,17+,18-/m1/s1
InChI Key MKXZASYAUGDDCJ-BPQIPLTHBH
KEGG Drug D03742 Link Image
KEGG Compound C06947 Link Image
PubChem Compound 5360696 Link Image
PubChem Substance 173392 Link Image
ChEBI ID 4470 Link Image
PharmGKB ID PA449273 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 00816000 Link Image
RxList Link Not Available
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Dextromethorphan Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 271.3972
Monoisotopic Molecular Weight 271.1936
State Solid
Melting Point Not Available
Experimental Water Solubility 74.7 mg/L Source: PhysProp
Predicted Water Solubility 8.51e-03 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 3.6 Source: PhysProp
Predicted LogP 3.76 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -4.50 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 COC1=CC2=C(C[C@H]3[C@H]4CCCC[C@@]24CCN3C)C=C1
Canonical SMILES COC1=CC2=C(CC3C4CCCCC24CCN3C)C=C1
Drug Category
  • Analgesics, Opioid
  • Antitussive Agents
  • Excitatory Amino Acid Antagonists
ATC Codes
AHFS Codes
  • 48:08.00
  • 48:16.00
Indication For treatment and relief of dry cough.
Pharmacology Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity.
Mechanism of Action Dextromethorphan is an opioid-like drug that binds to and acts as antagonist to the NMDA glutamatergic receptor, it is an agonist to the opioid sigma 1 and sigma 2 receptors, it is also an alpha3/beta4 nicotinic receptor antagonist and targets the serotonin reuptake pump. Dextromethorphan is rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier. The first-pass through the hepatic portal vein results in some of the drug being metabolized into an active metabolite of dextromethorphan, dextrorphan, the 3-hydroxy derivative of dextromethorphan.
Absorption Rapidly absorbed from the gastrointestinal tract.
Toxicity Not Available
Protein Binding Not Available
Biotransformation Hepatic. Rapidly and extensively metabolized to dextrorphan (active metabolite). One well known metabolic catalyst involved is a specific cytochrome P450 enzyme known as 2D6, or CYP2D6.
Half Life 3-6 hours
Dosage Forms
Form Route
Capsule Oral
Liquid Oral
Lozenge Oral
Strip Oral
Suspension Oral
Syrup Oral
Tablet Oral
Patient Information Not Available
Contraindications Not Available
Interactions Not Available
Drug Interactions
Drug Interaction
Dihydroquinidine barbiturate Quinidine increases the toxicity of dextromethorphan
Fluoxetine Combination associated with possible serotoninergic syndrome
Isocarboxazid Possible severe adverse reaction
Memantine Increased risk of CNS adverse effects
Moclobemide Increased CNS toxicity
Paroxetine Combination associated with possible serotoninergic syndrome
Phenelzine Possible severe adverse reaction
Quinidine Quinidine increases the toxicity of dextromethorphan
Quinidine barbiturate Quinidine increases the toxicity of dextromethorphan
Rasagiline Possible severe adverse reaction
Selegiline Combination associated with possible serotoninergic syndrome
Sibutramine Combination associated with possible serotoninergic syndrome
Terbinafine Terbinafine increases dextromethorphan levels
Tranylcypromine Possible severe adverse reaction
Food Interactions
  • Take without regard to meals.
Pathways Not Available
General References
  1. Hernandez SC, Bertolino M, Xiao Y, Pringle KE, Caruso FS, Kellar KJ: Dextromethorphan and its metabolite dextrorphan block alpha3beta4 neuronal nicotinic receptors. J Pharmacol Exp Ther. 2000 Jun;293(3):962-7. [PubMed Link Image]
  2. Brooks BR, Thisted RA, Appel SH, Bradley WG, Olney RK, Berg JE, Pope LE, Smith RA: Treatment of pseudobulbar affect in ALS with dextromethorphan/quinidine: a randomized trial. Neurology. 2004 Oct 26;63(8):1364-70. [PubMed Link Image]
  3. Carliss RD, Radovsky A, Chengelis CP, O'Neill TP, Shuey DL: Oral administration of dextromethorphan does not produce neuronal vacuolation in the rat brain. Neurotoxicology. 2007 Jul;28(4):813-8. Epub 2007 Apr 6. [PubMed Link Image]
  4. Olney JW, Labruyere J, Price MT: Pathological changes induced in cerebrocortical neurons by phencyclidine and related drugs. Science. 1989 Jun 16;244(4910):1360-2. [PubMed Link Image]
  5. Hargreaves RJ, Hill RG, Iversen LL: Neuroprotective NMDA antagonists: the controversy over their potential for adverse effects on cortical neuronal morphology. Acta Neurochir Suppl (Wien). 1994;60:15-9. [PubMed Link Image]
  6. Drugs.com Link Image
  7. Wikipedia Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 2D6 (CYP2D6)
Targets
  1. Sigma 1-type opioid receptor
  2. Opioid receptor, sigma 1
  3. Glutamate [NMDA] receptor subunit 3A
  4. Neuronal acetylcholine receptor subunit alpha-2
  5. Sodium-dependent serotonin transporter
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 2D6 (CYP2D6)
Enzyme 1 Gene Name CYP2D6
Enzyme 1 SwissProt ID P10635 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P10635|CP2D6_HUMAN Cytochrome P450 2D6 (EC 1.14.14.1) 
MGLEALVPLAVIVAIFLLLVDLMHRRQRWAARYPPGPLPLPGLGNLLHVDFQNTPYCFDQ
LRRRFGDVFSLQLAWTPVVVLNGLAAVREALVTHGEDTADRPPVPITQILGFGPRSQGVF
LARYGPAWREQRRFSVSTLRNLGLGKKSLEQWVTEEAACLCAAFANHSGRPFRPNGLLDK
AVSNVIASLTCGRRFEYDDPRFLRLLDLAQEGLKEESGFLREVLNAVPVLLHIPALAGKV
LRFQKAFLTQLDELLTEHRMTWDPAQPPRDLTEAFLAEMEKAKGNPESSFNDENLRIVVA
DLFSAGMVTTSTTLAWGLLLMILHPDVQRRVQQEIDDVIGQVRRPEMGDQAHMPYTTAVI
HEVQRFGDIVPLGMTHMTSRDIEVQGFRIPKGTTLITNLSSVLKDEAVWEKPFRFHPEHF
LDAQGHFVKPEAFLPFSAGRRACLGEPLARMELFLFFTSLLQHFSFSVPTGQPRPSHHGV
FAFLVSPSPYELCAVPR
Drug Target 1 [top]
Target 1 ID 174
Target 1 Name Sigma 1-type opioid receptor
Target 1 Synonyms
  1. Aging-associated gene 8 protein
  2. SIG-1R
  3. SR-BP
  4. SR31747-binding protein
  5. Sigma1-receptor
  6. Sigma1R
  7. hSigmaR1
Target 1 Gene Name OPRS1
Target 1 Protein Sequence >Sigma receptor 
MQWAVGRRWAWAALLLAVAAVLTQVVWLWLGTQSFVFQREEIAQLARQYAGLDHELAFSR
LIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCLLHASLSEYVLLFGTALGSRGHSGRY
WAEISDTIISGTFHQWREGTTKSEVFYPGETVVHGPGEATAVEWGPNTWMVEYGRGVIPS
TLAFALADTVFSTQDFLTLFYTLRSYARGLRLELTTYLFGQDP
Target 1 Number of Residues 226
Target 1 Molecular Weight 25128
Target 1 Theoretical pI 5.87
Target 1 GO Classification
Function
catalytic activity
isomerase activity
intramolecular oxidoreductase activity
intramolecular oxidoreductase activity, transposing C=C bonds
C-8 sterol isomerase activity
Process
physiological process
metabolism
cellular metabolism
alcohol metabolism
sterol metabolism
ergosterol metabolism
ergosterol biosynthesis
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
endoplasmic reticulum
Target 1 General Function Involved in C-8 sterol isomerase activity
Target 1 Specific Function Not Available
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 9-31
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 1783387 Link Image
Target 1 UniProtKB/Swiss-Prot ID Q99720 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name Q99720_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location Not Available
Target 1 Gene Sequence >672 bp 
ATGCAGTGGGCCGTGGGCCGGCGGTGGGCGTGGGCCGCGCTGCTCCTGGCTGTCGCAGCG
GTGCTGACCCAGGTCGTCTGGCTCTGGCTGGGTACGCAGAGCTTCGTCTTCCAGCGCGAA
GAGATAGCGCAGTTGGCGCGGCAGTACGCTGGGCTGGACCACGAGCTGGCCTTCTCTCGT
CTGATCGTGGAGCTGCGGCGGCTGCACCCAGGCCACGTGCTGCCCGACGAGGAGCTGCAG
TGGGTGTTCGTGAATGCGGGTGGCTGGATGGGCGCCATGTGCCTTCTGCACGCCTCGCTG
TCCGAGTATGTGCTGCTCTTCGGCACCGCCTTGGGCTCCCGCGGCCACTCGGGGCGCTAC
TGGGCTGAGATCTCGGATACCATCATCTCTGGCACCTTCCACCAGTGGAGAGAGGGCACC
ACCAAAAGTGAGGTCTTCTACCCAGGGGAGACGGTAGTACACGGGCCTGGTGAGGCAACA
GCTGTGGAGTGGGGGCCAAACACATGGATGGTGGAGTACGGCCGGGGCGTCATCCCATCC
ACCCTGGCCTTCGCGCTGGCCGACACTGTCTTCAGCACCCAGGACTTCCTCACCCTCTTC
TATACTCTTCGCTCCTATGCTCGGGGCCTCCGGCTTGAGCTCACCACCTACCTCTTTGGC
CAGGACCCTTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID OPRS1 Link Image
Target 1 GenAtlas ID OPRS1 Link Image
Target 1 HGNC ID HGNC:8157 Link Image
Target 1 Chromosome Location 9
Target 1 Locus 9p13.3
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Strausberg RL, Feingold EA, Grouse LH, Derge JG, Klausner RD, Collins FS, Wagner L, Shenmen CM, Schuler GD, Altschul SF, Zeeberg B, Buetow KH, Schaefer CF, Bhat NK, Hopkins RF, Jordan H, Moore T, Max SI, Wang J, Hsieh F, Diatchenko L, Marusina K, Farmer AA, Rubin GM, Hong L, Stapleton M, Soares MB, Bonaldo MF, Casavant TL, Scheetz TE, Brownstein MJ, Usdin TB, Toshiyuki S, Carninci P, Prange C, Raha SS, Loquellano NA, Peters GJ, Abramson RD, Mullahy SJ, Bosak SA, McEwan PJ, McKernan KJ, Malek JA, Gunaratne PH, Richards S, Worley KC, Hale S, Garcia AM, Gay LJ, Hulyk SW, Villalon DK, Muzny DM, Sodergren EJ, Lu X, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madan A, Young AC, Shevchenko Y, Bouffard GG, Blakesley RW, Touchman JW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Krzywinski MI, Skalska U, Smailus DE, Schnerch A, Schein JE, Jones SJ, Marra MA: Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences. Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):16899-903. Epub 2002 Dec 11. [PubMed Link Image]
  2. Kekuda R, Prasad PD, Fei YJ, Leibach FH, Ganapathy V: Cloning and functional expression of the human type 1 sigma receptor (hSigmaR1). Biochem Biophys Res Commun. 1996 Dec 13;229(2):553-8. [PubMed Link Image]
  3. Prasad PD, Li HW, Fei YJ, Ganapathy ME, Fujita T, Plumley LH, Yang-Feng TL, Leibach FH, Ganapathy V: Exon-intron structure, analysis of promoter region, and chromosomal localization of the human type 1 sigma receptor gene. J Neurochem. 1998 Feb;70(2):443-51. [PubMed Link Image]
Target 1 Drug References
  1. Church AJ, Andrew RD: Spreading depression expands traumatic injury in neocortical brain slices. J Neurotrauma. 2005 Feb;22(2):277-90. [PubMed Link Image]
  2. Shin EJ, Nah SY, Kim WK, Ko KH, Jhoo WK, Lim YK, Cha JY, Chen CF, Kim HC: The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan. Br J Pharmacol. 2005 Apr;144(7):908-18. [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. Shin EJ, Nah SY, Chae JS, Bing G, Shin SW, Yen TP, Baek IH, Kim WK, Maurice T, Nabeshima T, Kim HC: Dextromethorphan attenuates trimethyltin-induced neurotoxicity via sigma1 receptor activation in rats. Neurochem Int. 2007 May;50(6):791-9. Epub 2007 Feb 4. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 319
Target 2 Name Opioid receptor, sigma 1
Target 2 Synonyms Not Available
Target 2 Gene Name OPRS1
Target 2 Protein Sequence >Opioid receptor, sigma 1 
MGAMCLLHASLSEYVLLFGTALGSRGHSGRYWAEISDTIISGTFHQWREGTTKSEVFYPG
ETVVHGPGEATAVEWGPNTWMVEYGRGVIPSTLAFALADTVFSTQDFLTLFYTLRSYARG
LRLELTTYLFGQDP
Target 2 Number of Residues 136
Target 2 Molecular Weight 14853
Target 2 Theoretical pI 5.07
Target 2 GO Classification
Function
catalytic activity
isomerase activity
intramolecular oxidoreductase activity
intramolecular oxidoreductase activity, transposing C=C bonds
C-8 sterol isomerase activity
Process
physiological process
metabolism
cellular metabolism
alcohol metabolism
sterol metabolism
ergosterol metabolism
ergosterol biosynthesis
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
endoplasmic reticulum
Target 2 General Function Involved in C-8 sterol isomerase activity
Target 2 Specific Function Not Available
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 123231939 Link Image
Target 2 UniProtKB/Swiss-Prot ID Q5T1J1 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name Q5T1J1_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location Not Available
Target 2 Gene Sequence >405 bp 
ATGGGCGCCATGTGCCTTCTGCACGCCTCGCTGTCCGAGTATGTGCTGCTCTTCGGCACC
GCCTTGGGCTCCCGCGGCCACTCGGGGCGCTACTGGGCTGAGATCTCGGATACCATCATC
TCTGGCACCTTCCACCAGTGGAGAGAGGGCACCACCAAAAGTGAGGTCTTCTACCCAGGG
GAGACGGTAGTACACGGGCCTGGTGAGGCAACAGCTGTGGAGTGGGGGCCAAACACATGG
ATGGTGGAGTACGGCCGGGGCGTCATCCCATCCACCCTGGCCTTCGCGCTGGCCGACACT
GTCTTCAGCACCCAGGACTTCCTCACCCTCTTCTATACTCTTCGCTCCTATGCTCGGGGC
CTCCGGCTTGAGCTCACCACCTACCTCTTTGGCCAGGACCCTTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID OPRS1 Link Image
Target 2 GenAtlas ID OPRS1 Link Image
Target 2 HGNC ID HGNC:8157 Link Image
Target 2 Chromosome Location 9
Target 2 Locus 9p13.3
Target 2 SNPs SNPJam Report Link Image
Target 2 General References Not Available
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 706
Target 3 Name Glutamate [NMDA] receptor subunit 3A
Target 3 Synonyms
  1. Glutamate receptor subunit 3A precursor
  2. N-methyl-D-aspartate receptor subtype NR3A
  3. NMDAR-L
Target 3 Gene Name GRIN3A
Target 3 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 3 Number of Residues 1133
Target 3 Molecular Weight 125597
Target 3 Theoretical pI 7.81
Target 3 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 3 General Function Involved in ionotropic glutamate receptor activity
Target 3 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 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • 1-23
Target 3 Transmembrane Regions
  • 675-695
  • 749-769
  • 931-951
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 20372905 Link Image
Target 3 UniProtKB/Swiss-Prot ID Q8TCU5 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name NMD3A_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Cell membrane
  • multi-pass membrane protein. Enriched in post-synaptic plasma membrane and post-synap
Target 3 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 3 GenBank Gene ID
Target 3 GeneCard ID GRIN3A Link Image
Target 3 GenAtlas ID GRIN3A Link Image
Target 3 HGNC ID HGNC:16767 Link Image
Target 3 Chromosome Location 9
Target 3 Locus 9q31.1
Target 3 SNPs SNPJam Report Link Image
Target 3 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 3 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 4 [top]
Target 4 ID 813
Target 4 Name Neuronal acetylcholine receptor subunit alpha-2
Target 4 Synonyms
  1. Neuronal acetylcholine receptor subunit alpha-2 precursor
Target 4 Gene Name CHRNA2
Target 4 Protein Sequence >Neuronal acetylcholine receptor protein subunit alpha-2 precursor 
MGPSCPVFLSFTKLSLWWLLLTPAGGEEAKRPPPRAPGDPLSSPSPTALPQGGSHTETED
RLFKHLFRGYNRWARPVPNTSDVVIVRFGLSIAQLIDVDEKNQMMTTNVWLKQEWSDYKL
RWNPADFGNITSLRVPSEMIWIPDIVLYNNADGEFAVTHMTKAHLFSTGTVHWVPPAIYK
SSCSIDVTFFPFDQQNCKMKFGSWTYDKAKIDLEQMEQTVDLKDYWESGEWAIVNATGTY
NSKKYDCCAEIYPDVTYAFVIRRLPLFYTINLIIPCLLISCLTVLVFYLPSDCGEKITLC
ISVLLSLTVFLLLITEIIPSTSLVIPLIGEYLLFTMIFVTLSIVITVFVLNVHHRSPSTH
TMPHWVRGALLGCVPRWLLMNRPPPPVELCHPLRLKLSPSYHWLESNVDAEEREVVVEEE
DRWACAGHVAPSVGTLCSHGHLHSGASGPKAEALLQEGELLLSPHMQKALEGVHYIADHL
RSEDADSSVKEDWKYVAMVIDRIFLWLFIIVCFLGTIGLFLPPFLAGMI
Target 4 Number of Residues 537
Target 4 Molecular Weight 59736
Target 4 Theoretical pI 6.02
Target 4 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 4 General Function Involved in neurotransmitter receptor activity
Target 4 Specific Function After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • 1-26
Target 4 Transmembrane Regions
  • 265-289
  • 297-315
  • 331-352
  • 503-521
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 1458110 Link Image
Target 4 UniProtKB/Swiss-Prot ID Q15822 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name ACHA2_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 4 Gene Sequence >1590 bp 
ATGGGCCCCTCCTGTCCTGTGTTCCTGTCCTTCACAAAGCTCAGCCTGTGGTGGCTCCTT
CTGACCCCAGCAGGTGGAGAGGAAGCTAAGCGCCCACCTCCCAGGGCTCCTGGAGACCCA
CTCTCCTCTCCCAGTCCCACGGCATTGCCGCAGGGAGGCTCGCATACCGAGACTGAGGAC
CGGCTCTTCAAACACCTCTTCCGGGGCTACAACCGCTGGGCGCGCCCGGTGCCCAACACT
TCAGACGTGGTGATTGTGCGCTTTGGACTGTCCATCGCTCAGCTCATCGATGTGGATGAG
AAGAACCAAATGATGACCACCAACGTCTGGCTAAAACAGGAGTGGAGCGACTACAAACTG
CGCTGGAACCCCGCTGATTTTGGCAACATCACATCTCTCAGGGTCCCTTCTGAGATGATC
TGGATCCCCGACATTGTTCTCTACAACAATGCAGATGGGGAGTTTGCAGTGACCCACATG
ACCAAGGCCCACCTCTTCTCCACGGGCACTGTGCACTGGGTGCCCCCGGCCATCTACAAG
AGCTCCTGCAGCATCGACGTCACCTTCTTCCCCTTCGACCAGCAGAACTGCAAGATGAAG
TTTGGCTCCTGGACTTATGACAAGGCCAAGATCGACCTGGAGCAGATGGAGCAGACTGTG
GACCTGAAGGACTACTGGGAGAGCGGCGAGTGGGCCATCGTCAATGCCACGGGCACCTAC
AACAGCAAGAAGTACGACTGCTGCGCCGAGATCTACCCCGACGTCACCTACGCCTTCGTC
ATCCGGCGGCTGCCGCTCTTCTACACCATCAACCTCATCATCCCCTGCCTGCTCATCTCC
TGCCTCACTGTGCTGGTCTTCTACCTGCCCTCCGACTGCGGCGAGAAGATCACGCTGTGC
ATTTCGGTGCTGCTGTCACTCACCGTCTTCCTGCTGCTCATCACTGAGATCATCCCGTCC
ACCTCGCTGGTCATCCCGCTCATCGGCGAGTACCTGCTGTTCACCATGATCTTCGTCACC
CTGTCCATCGTCATCACCGTCTTCGTGCTCAATGTGCACCACCGCTCCCCCAGCACCCAC
ACCATGCCCCACTGGGTGCGGGGGGCCCTTCTGGGCTGTGTGCCCCGGTGGCTTCTGATG
AACCGGCCCCCACCACCCGTGGAGCTCTGCCACCCCCTACGCCTGAAGCTCAGCCCCTCT
TATCACTGGCTGGAGAGCAACGTGGATGCCGAGGAGAGGGAGGTGGTGGTGGAGGAGGAG
GACAGATGGGCATGTGCAGGTCATGTGGCCCCCTCTGTGGGCACCCTCTGCAGCCACGGC
CACCTGCACTCTGGGGCCTCAGGTCCCAAGGCTGAGGCTCTGCTGCAGGAGGGTGAGCTG
CTGCTATCACCCCACATGCAGAAGGCACTGGAAGGTGTGCACTACATTGCCGACCACCTG
CGGTCTGAGGATGCTGACTCTTCGGTGAAGGAGGACTGGAAGTATGTTGCCATGGTCATC
GACAGGATCTTCCTCTGGCTGTTTATCATCGTCTGCTTCCTGGGGACCATCGGCCTCTTT
CTGCCTCCGTTCCTAGCTGGAATGATCTGA
Target 4 GenBank Gene ID
Target 4 GeneCard ID CHRNA2 Link Image
Target 4 GenAtlas ID CHRNA2 Link Image
Target 4 HGNC ID HGNC:1956 Link Image
Target 4 Chromosome Location 8
Target 4 Locus 8p21
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Elliott KJ, Ellis SB, Berckhan KJ, Urrutia A, Chavez-Noriega LE, Johnson EC, Velicelebi G, Harpold MM: Comparative structure of human neuronal alpha 2-alpha 7 and beta 2-beta 4 nicotinic acetylcholine receptor subunits and functional expression of the alpha 2, alpha 3, alpha 4, alpha 7, beta 2, and beta 4 subunits. J Mol Neurosci. 1996 Fall;7(3):217-28. [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 824
Target 5 Name Sodium-dependent serotonin transporter
Target 5 Synonyms
  1. 5HT transporter
  2. 5HTT
Target 5 Gene Name SLC6A4
Target 5 Protein Sequence >Sodium-dependent serotonin transporter 
METTPLNSQKQLSACEDGEDCQENGVLQKVVPTPGDKVESGQISNGYSAVPSPGAGDDTR
HSIPATTTTLVAELHQGERETWGKKVDFLLSVIGYAVDLGNVWRFPYICYQNGGGAFLLP
YTIMAIFGGIPLFYMELALGQYHRNGCISIWRKICPIFKGIGYAICIIAFYIASYYNTIM
AWALYYLISSFTDQLPWTSCKNSWNTGNCTNYFSEDNITWTLHSTSPAEEFYTRHVLQIH
RSKGLQDLGGISWQLALCIMLIFTVIYFSIWKGVKTSGKVVWVTATFPYIILSVLLVRGA
TLPGAWRGVLFYLKPNWQKLLETGVWIDAAAQIFFSLGPGFGVLLAFASYNKFNNNCYQD
ALVTSVVNCMTSFVSGFVIFTVLGYMAEMRNEDVSEVAKDAGPSLLFITYAEAIANMPAS
TFFAIIFFLMLITLGLDSTFAGLEGVITAVLDEFPHVWAKRRERFVLAVVITCFFGSLVT
LTFGGAYVVKLLEEYATGPAVLTVALIEAVAVSWFYGITQFCRDVKEMLGFSPGWFWRIC
WVAISPLFLLFIICSFLMSPPQLRLFQYNYPYWSIILGYCIGTSSFICIPTYIAYRLIIT
PGTFKERIIKSITPETPTEIPCGDIRLNAV
Target 5 Number of Residues 640
Target 5 Molecular Weight 70325
Target 5 Theoretical pI 6.17
Target 5 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 5 General Function Involved in serotonin:sodium symporter activity
Target 5 Specific Function Terminates the action of serotonine by its high affinity sodium-dependent reuptake into presynaptic terminals
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • 88-108
  • 116-135
  • 160-180
  • 253-271
  • 280-297
  • 333-350
  • 362-383
  • 417-436
  • 464-482
  • 498-518
  • 539-558
  • 577-595
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 36433 Link Image
Target 5 UniProtKB/Swiss-Prot ID P31645 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name SC6A4_HUMAN Link Image
Target 5 PDB ID Not Available
Target 5 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 5 Gene Sequence >1893 bp 
ATGGAGACGACGCCCTTGAATTCTCAGAAGCAGCTATCAGCGTGTGAAGATGGAGAAGAT
TGTCAGGAAAACGGAGTTCTACAGAAGGTTGTTCCCACCCCAGGGGACAAAGTGGAGTCC
GGGCAAATATCCAATGGGTACTCAGCAGTTCCAAGTCCTGGTGCGGGAGATGACACACGG
CACTCTATCCCAGCGACCACCACCACCCTAGTGGCTGAGCTTCATCAAGGGGAACGGGAG
ACCTGGGGCAAGAAGGTGGATTTCCTTCTCTCAGTGATTGGCTATGCTGTGGACCTGGGC
AATGTCTGGCGCTTCCCCTACATATGTTACCAGAATGGAGGGGGGGCATTCCTCCTCCCC
TACACCATCATGGCCATTTTTGGGGGAATCCCGCTCTTTTACATGGAGCTCGCACTGGGA
CAGTACCACCGAAATGGATGCATTTCAATATGGAGGAAAATCTGCCCGATTTTCAAAGGG
ATTGGTTATGCCATCTGCATCATTGCCTTTTACATTGCTTCCTACTACAACACCATCATG
GCCTGGGCGCTATACTACCTCATCTCCTCCTTCACGGACCAGCTGCCCTGGACCAGCTGC
AAGAACTCCTGGAACACTGGCAACTGCACCAATTACTTCTCCGAGGACAACATCACCTGG
ACCCTCCATTCCACGTCCCCTGCTGAAGAATTTTACACGCGCCACGTCCTGCAGATCCAC
CGGTCTAAGGGGCTCCAGGACCTGGGGGGCATCAGCTGGCAGCTGGCCCTCTGCATCATG
CTGATCTTCACTGTTATCTACTTCAGCATCTGGAAAGGCGTCAAGACCTCTGGCAAGGTG
GTGTGGGTGACAGCCACCTTCCCTTATATCATCCTTTCTGTCCTGCTGGTGAGGGGTGCC
ACCCTCCCTGGAGCCTGGAGGGGTGTTCTCTTCTACTTGAAACCCAATTGGCAGAAACTC
CTGGAGACAGGGGTGTGGATAGATGCAGCCGCTCAGATCTTCTTCTCTCTTGGTCCGGGC
TTTGGGGTCCTGCTGGCTTTTGCTAGCTACAACAAGTTCAACAACAACTGCTACCAAGAT
GCCCTGGTGACCAGCGTGGTGAACTGCATGACGAGCTTCGTTTCGGGATTTGTCATCTTC
ACAGTGCTCGGTTACATGGCTGAGATGAGGAATGAAGATGTGTCTGAGGTGGCCAAAGAC
GCAGGTCCCAGCCTCCTCTTCATCACGTATGCAGAAGCGATAGCCAACATGCCAGCGTCC
ACTTTCTTTGCCATCATCTTCTTTCTGATGTTAATCACGCTGGGCTTGGACAGCACGTTT
GCAGGCTTGGAGGGGGTGATCACGGCTGTGCTGGATGAGTTCCCACACGTCTGGGCCAAG
CGCCGGGAGCGGTTCGTGCTCGCCGTGGTCATCACCTGCTTCTTTGGATCCCTGGTCACC
CTGACTTTTGGAGGGGCCTACGTGGTGAAGCTGCTGGAGGAGTATGCCACGGGGCCCGCA
GTGCTCACTGTCGCGCTGATCGAAGCAGTCGCTGTGTCTTGGTTCTATGGCATCACTCAG
TTCTGCAGGGACGTGAAGGAAATGCTCGGCTTCAGCCCGGGGTGGTTCTGGAGGATCTGC
TGGGTGGCCATCAGCCCTCTGTTTCTCCTGTTCATCATTTGCAGTTTTCTGATGAGCCCG
CCACAACTACGACTTTTCCAATATAATTATCCTTACTGGAGTATCATCTTGGGTTACTGC
ATAGGAACCTCATCTTTCATTTGCATCCCCACATATATAGCTTATCGGTTGATCATCACT
CCAGGGACATTTAAAGAGCGTATTATTAAAAGTATTACCCCGGAGACACCAACAGAAATT
CCTTGTGGGGACATCCGCTTGAATGCTGTGTAA
Target 5 GenBank Gene ID
Target 5 GeneCard ID SLC6A4 Link Image
Target 5 GenAtlas ID SLC6A4 Link Image
Target 5 HGNC ID HGNC:11050 Link Image
Target 5 Chromosome Location 17
Target 5 Locus 17q11.1-q12
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, Shaw N, Lane CR, Lim EP, Kalyanaraman N, Nemesh J, Ziaugra L, Friedland L, Rolfe A, Warrington J, Lipshutz R, Daley GQ, Lander ES: Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat Genet. 1999 Jul;22(3):231-8. [PubMed Link Image]
  2. Caspi A, Sugden K, Moffitt TE, Taylor A, Craig IW, Harrington H, McClay J, Mill J, Martin J, Braithwaite A, Poulton R: Influence of life stress on depression: moderation by a polymorphism in the 5-HTT gene. Science. 2003 Jul 18;301(5631):386-9. [PubMed Link Image]
  3. Ramamoorthy S, Bauman AL, Moore KR, Han H, Yang-Feng T, Chang AS, Ganapathy V, Blakely RD: Antidepressant- and cocaine-sensitive human serotonin transporter: molecular cloning, expression, and chromosomal localization. Proc Natl Acad Sci U S A. 1993 Mar 15;90(6):2542-6. [PubMed Link Image]
  4. Lesch KP, Wolozin BL, Murphy DL, Reiderer P: Primary structure of the human platelet serotonin uptake site: identity with the brain serotonin transporter. J Neurochem. 1993 Jun;60(6):2319-22. [PubMed Link Image]
  5. Lesch KP, Wolozin BL, Estler HC, Murphy DL, Riederer P: Isolation of a cDNA encoding the human brain serotonin transporter. J Neural Transm Gen Sect. 1993;91(1):67-72. [PubMed Link Image]
Target 5 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.