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Showing drug card for Caffeine (DB00201)

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Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:04:12
Primary Accession Number DB00201
Secondary Accession Number
  • APRD00673
Name Caffeine
Drug Type
  • Approved
  • Small Molecule
Description A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes smooth muscle, stimulates cardiac muscle, stimulates diuresis, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide phosphodiesterases, antagonism of adenosine receptors, and modulation of intracellular calcium handling. [PubChem]
Synonyms
  1. CFF
  2. Cafeina
  3. Caffein
  4. Caffeine Pure
  5. Caffeine, Anhydrous
  6. Caffeine, Monohydrate
  7. Caffeine, Synthetic
  8. Compound 65
  9. Methyltheobromide
  10. Methyltheobromine
  11. Monomethyl Derivative of Theophylline
  12. Theobromine ME
  13. Theophylline ME
Brand Names
  1. Alert-Pep
  2. Anoquan
  3. Cafamil
  4. Cafcit
  5. Cafecon
  6. Cafergot
  7. Caffedrine
  8. Caffedrine Caplets
  9. Caffine
  10. Cafipel
  11. Coffein
  12. Coffeine
  13. Darvon Compound
  14. Darvon Compound-65
  15. Dasin
  16. Dexitac
  17. Dexitac Stay Alert Stimulant
  18. Dhc Plus
  19. Diurex
  20. Durvitan
  21. Eldiatric C
  22. Enerjets
  23. Ercatab
  24. Esgic
  25. Esgic-Plus
  26. Femcet
  27. Fioricet
  28. Fiorinal
  29. Guaranine
  30. Hycomine
  31. Invagesic
  32. Invagesic Forte
  33. Keep Alert
  34. Kofein
  35. Koffein
  36. Lanorinal
  37. Mateina
  38. Maximum Strength Snapback Stimulant Powders
  39. Medigesic Plus
  40. Migergot
  41. Miudol
  42. Natural Caffeinum
  43. Nix Nap
  44. No-Doz
  45. Nodaca
  46. Nodoz Maximum Strength Caplets
  47. Norgesic
  48. Norgesic Forte
  49. Organex
  50. Orphengesic
  51. Orphengesic Forte
  52. Pep-Back
  53. Phensal
  54. Propoxyphene Compound 65
  55. Propoxyphene Compound-65
  56. Quick Pep
  57. Refresh'n
  58. SK 65 Compound
  59. Stim
  60. Synalgos-Dc
  61. Thein
  62. Theine
  63. Triad
  64. Ultra Pep-Back
  65. Vivarin
  66. Wake-Up
  67. Wigraine
Brand Mixtures
  1. 217 (Acetylsalicylic Acid + Caffeine Citrate)
  2. 217 Strong Tab (Acetylsalicylic Acid + Caffeine Citrate)
  3. 222 Tablet (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  4. 282 Mep (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate + Meprobamate)
  5. 282 Mep Tab (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate + Meprobamate)
  6. 282 Tab (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  7. 282 Tablets (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  8. 292 Tab (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  9. 292 Tablets (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  10. 692 Tab (Acetylsalicylic Acid + Caffeine + Dextropropoxyphene Hydrochloride)
  11. 692 Tablet (Acetylsalicylic Acid + Caffeine + Dextropropoxyphene Hydrochloride)
  12. A & C Tablets with Codeine 15mg (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  13. A & C Tablets with Codeine 30mg (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  14. A C and C Tab 0.125gr (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  15. A.C. & C 8mg Tab (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  16. A.C. & C Tablets (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  17. AC and C Tab 1/8gr (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  18. AC&C Tablets (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  19. ASA, Caffeine & 8mg Codeine Phosphate (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  20. Acet 2 (Acetaminophen + Caffeine + Codeine Phosphate)
  21. Acet 3 (Acetaminophen + Caffeine + Codeine Phosphate)
  22. Acetaminophen 300 Mg with Caffeine & Codeine Caplet (Acetaminophen + Caffeine + Codeine Phosphate)
  23. Acetaminophen 500mg Cmpd Tab with Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  24. Acetaminophen Caffeine & 8mg Cod Phos Tab (Acetaminophen + Caffeine + Codeine (Codeine Phosphate))
  25. Acetaminophen Caffeine & 8mg Cod. Phos. Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  26. Acetaminophen Compound Caplets with Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  27. Acetaminophen Compound Tablets with Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  28. Acetaminophen Compound Tablets with Codeine 8mg (Acetaminophen + Caffeine + Codeine Phosphate)
  29. Acetaminophen Extra Strength with Caf & Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  30. Acetaminophen with Caffeine and Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  31. Acetaminophen with Codeine - Caplet (Acetaminophen + Caffeine + Codeine Phosphate)
  32. Acetaminophen with Codeine Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  33. Acetaminophen, Caffeine & 8mg Codeine Phosphate (Acetaminophen + Caffeine + Codeine Phosphate)
  34. Acetaminophen, Caffeine & 8mg Codeine Phosphate Tablets (Acetaminophen + Caffeine + Codeine Phosphate)
  35. Acetaminophen, Caffeine and 8 Mg of Codeine Phosphate Tablets (Acetaminophen + Caffeine + Codeine Phosphate)
  36. Acetaminophen, Caffeine, and 8mg of Codeine Phosphate Tablets (Acetaminophen + Caffeine + Codeine Phosphate)
  37. Acetylsalicylic Acid Caffeine & 8mg Cod Phos (Acetylsalicylic Acid + Caffeine + Codeine (Codeine Phosphate))
  38. Acetylsalicylic Acid, Caffeine & 8 Mg Codeine Phosphate Tablets (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  39. Acetylsalicylic Acid, Caffeine and 8mg Codeine Phosphate (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  40. Alka-Seltzer Morning Relief (Acetylsalicylic Acid + Caffeine)
  41. Anacin Caplet (Acetylsalicylic Acid + Caffeine)
  42. Anacin Caplets (Acetylsalicylic Acid + Caffeine)
  43. Anacin Extra Strength Caplet (Acetylsalicylic Acid + Caffeine)
  44. Anacin Extra Strength Tablet (Acetylsalicylic Acid + Caffeine)
  45. Anacin Tab (Acetylsalicylic Acid + Caffeine)
  46. Anacin Tablet (Acetylsalicylic Acid + Caffeine)
  47. Anacin with Codeine Tab (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  48. Antidol Tablets (Acetylsalicylic Acid + Caffeine)
  49. Arco Pain Tab (Acetylsalicylic Acid + Caffeine Citrate)
  50. Astone Cap (Acetylsalicylic Acid + Caffeine)
  51. Atasol 15 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  52. Atasol 30 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  53. Atasol 8 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  54. C T Acetylsalicylic Acid Codeine and Caf Tab (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  55. C-2 Buffered with Codeine (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  56. C2 Buffered Tab (Acetylsalicylic Acid + Aluminum Hydroxide + Caffeine + Magnesium Hydroxide)
  57. C2 Buffered with Codeine Tab (Acetylsalicylic Acid + Aluminum Hydroxide + Caffeine + Codeine Phosphate + Magnesium Hydroxide)
  58. C2 Tab with Codeine (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  59. Cafergot PB Sup (Belladonna + Caffeine + Ergotamine (Ergotamine Tartrate) + Pentobarbital)
  60. Cafergot PB Tab (Belladonna + Caffeine + Ergotamine (Ergotamine Tartrate) + Pentobarbital Sodium)
  61. Cafergot Sup (Caffeine + Ergotamine Tartrate)
  62. Cafergot Tab (Caffeine + Ergotamine Tartrate)
  63. Calmine Tab (Acetylsalicylic Acid + Caffeine)
  64. Codamin No2 (Acetaminophen + Caffeine + Codeine Phosphate)
  65. Codamin No3 (Acetaminophen + Caffeine + Codeine Phosphate)
  66. Codaminophen Tab 1/8gr (Acetaminophen + Caffeine + Codeine Phosphate)
  67. Corytab (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride)
  68. Cotabs (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  69. Darvon N Compound Pulvule 405 (Acetylsalicylic Acid + Caffeine + Dextropropoxyphene Napsylate)
  70. Dolomine 37 (Acetylsalicylic Acid + Caffeine)
  71. Dristan Capsules (Acetylsalicylic Acid + Caffeine + Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  72. Emercidin D Tab (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride + Phenylpropanolamine Hydrochloride)
  73. Emertabs Tab (Acetaminophen + Caffeine + Phenylpropanolamine Hydrochloride)
  74. Ergodryl Cap (Caffeine Citrate + Diphenhydramine Hydrochloride + Ergotamine Tartrate)
  75. Excedrin (Acetaminophen + Caffeine)
  76. Excedrin Extra-Strength (Acetaminophen + Caffeine)
  77. Excedrin Tab (Acetaminophen + Caffeine)
  78. Exdol 15tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  79. Exdol 30tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  80. Exdol 8 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  81. Exdol-15 Tablets (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  82. Exdol-30 Tablets (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  83. Exdol-8 Tablets (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  84. Extra Strength Acetaminophen, Caffeine & 8mg Codeine Phosphate Caplets (Acetaminophen + Caffeine + Codeine Phosphate)
  85. Extra Strength Midol (Acetylsalicylic Acid + Caffeine)
  86. Fiorinal C1/2 Cap (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  87. Fiorinal C1/4 Cap (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  88. Fiorinal Cap (Acetylsalicylic Acid + Butalbital + Caffeine)
  89. Fiorinal Tab (Acetylsalicylic Acid + Butalbital + Caffeine)
  90. Gravergol Capsules (Caffeine + Dimenhydrinate + Ergotamine Tartrate)
  91. Herbopyrine Tab 325mg (Acetylsalicylic Acid + Caffeine Citrate)
  92. Instantine - Tab (Acetylsalicylic Acid + Caffeine)
  93. Instantine - Tablets (Acetylsalicylic Acid + Caffeine)
  94. Instantine Tab (Acetylsalicylic Acid + Caffeine)
  95. Madelon (Acetylsalicylic Acid + Caffeine)
  96. Megral Tabs (Caffeine + Cyclizine Hydrochloride + Ergotamine Tartrate)
  97. Midol - Caplet (Acetylsalicylic Acid + Caffeine + Cinnamedrine)
  98. Midol Extra Strength Gelcaps (Acetaminophen + Caffeine + Pyrilamine Maleate)
  99. Midol Extra Strength Menstrual (Acetaminophen + Caffeine + Pyrilamine Maleate)
  100. Midol Menstrual Formula - Caplet (Acetylsalicylic Acid + Caffeine)
  101. Midol Multi-Symptom Caplets Extra Strength (Acetaminophen + Caffeine + Pyrilamine Maleate)
  102. Midol Multi-Symptom Gelcap Extra Strength (Acetaminophen + Caffeine + Pyrilamine Maleate)
  103. Midol Regular (Acetylsalicylic Acid + Caffeine)
  104. Midol Tab (Acetylsalicylic Acid + Caffeine + Cinnamedrine)
  105. Neo Tigol Tab (Acetylsalicylic Acid + Aluminum Hydroxide + Caffeine + Magnesium Hydroxide + Passion Flower + Valerian)
  106. Nervine (Acetylsalicylic Acid + Caffeine)
  107. Nervine Tab (Acetylsalicylic Acid + Caffeine)
  108. Norgesic Forte Tab (Acetylsalicylic Acid + Caffeine + Orphenadrine Citrate)
  109. Norgesic Tab (Acetylsalicylic Acid + Caffeine + Orphenadrine Citrate)
  110. Novo AC and C 8mg Tab (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  111. Novo-Gesic C15 (Acetaminophen + Caffeine + Codeine Phosphate)
  112. Novo-Gesic C30 (Acetaminophen + Caffeine + Codeine Phosphate)
  113. Novo-Gesic-C8 (Acetaminophen + Caffeine + Codeine Phosphate)
  114. Novo-Propoxyn Compound Cap (Acetylsalicylic Acid + Caffeine + Dextropropoxyphene Hydrochloride)
  115. Oradrine 2 Tab (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride + Phenylpropanolamine Hydrochloride)
  116. Oradrine Tablets (Acetaminophen + Caffeine + Codeine Phosphate + Diphenylpyraline Hydrochloride + Phenylpropanolamine Hydrochloride)
  117. Oradrine-2 Tab (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride + Phenylpropanolamine Hydrochloride)
  118. Pain Aid (Acetylsalicylic Acid + Caffeine)
  119. Painex Tab 0.25gr (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  120. Painex Tab 0.5gr (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  121. Ratio-Lenoltec No 1 (Acetaminophen + Caffeine + Codeine Phosphate)
  122. Ratio-Lenoltec No 2 (Acetaminophen + Caffeine + Codeine Phosphate)
  123. Ratio-Lenoltec No 3 (Acetaminophen + Caffeine + Codeine Phosphate)
  124. Ratio-Tecnal (Acetylsalicylic Acid + Butalbital + Caffeine)
  125. Ratio-Tecnal C 1/2 (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  126. Ratio-Tecnal C1/4 (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  127. Sinugex 38 (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride)
  128. Triaminicin Colds & Flu Caplets (Acetaminophen + Caffeine + Pheniramine Maleate + Phenylpropanolamine Hydrochloride + Pyrilamine Maleate)
  129. Trianal Capsules (Acetylsalicylic Acid + Butalbital + Caffeine)
  130. Trianal Tablet (Acetylsalicylic Acid + Butalbital + Caffeine)
  131. Trianal-C 1/2 Capsule (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  132. Triatec-8 Fort Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  133. Triatec-8 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  134. Tylenol No 1 Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  135. Tylenol No.1 Caplets (Acetaminophen + Caffeine + Codeine Phosphate)
  136. Tylenol No.1 Forte Caplets (Acetaminophen + Caffeine + Codeine Phosphate)
  137. Tylenol No1 Forte Tablets with Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  138. Tylenol Ultra Relief (Acetaminophen + Caffeine)
  139. Tylenol with Codeine No. 2 - Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  140. Tylenol with Codeine No. 3 - Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  141. Tylenol with Codeine No2 Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  142. Tylenol with Codeine No3 Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  143. Ultra Headache Relief (Acetaminophen + Caffeine)
  144. Wigraine Suppositories (Belladonna + Caffeine + Ergotamine Tartrate)
  145. Wigraine Tab (Belladonna + Caffeine + Ergotamine Tartrate)
Chemical IUPAC Name 1,3,7-trimethylpurine-2,6-dione
Chemical Formula C8H10N4O2
Chemical Structure Structure
CAS Registry Number 58-08-2
InChI Identifier InChI=1/C8H10N4O2/c1-10-4-9-6-5(10)7(13)12(3)8(14)11(6)2/h4H,1-3H3
InChI Key RYYVLZVUVIJVGH-UHFFFAOYAW
KEGG Drug D00528 Link Image
KEGG Compound C07481 Link Image
PubChem Compound 2519 Link Image
PubChem Substance 148854 Link Image
ChEBI ID 27732 Link Image
PharmGKB ID PA448710 Link Image
HET ID CFF Link Image
GenBank ID Not Available
Drug ID Number [DIN] 02241831 Link Image
RxList Link http://www.rxlist.com/cgi/generic3/caffeine.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Caffeine Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference U.S. Pat. 2,508,545 (1950)
Average Molecular Weight 194.1906
Monoisotopic Molecular Weight 194.0804
State Solid
Melting Point 238 oC
Experimental Water Solubility 22 mg/ml Source: PhysProp
Predicted Water Solubility 1.10e+01 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity -0.5 Source: PhysProp
Predicted LogP -0.23 Calculated using ALOGPS
Experimental LogS -0.97 [ADME Research, USCD]
Predicted LogS -1.25 Calculated using ALOGPS
Experimental Caco2 Permeability -4.41 [ADME Research, USCD]
pKa/Isoelectric Point 10.4
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 CN1C=NC2=C1C(=O)N(C)C(=O)N2C
Canonical SMILES CN1C=NC2=C1C(=O)N(C)C(=O)N2C
Drug Category
  • Anorexigenic Agents
  • Central Nervous System Stimulants
  • Phosphodiesterase Inhibitors
ATC Codes
AHFS Codes
  • 28:08.92
  • 28:20.00
  • 28:20.92
  • 92:02.00*
Indication For management of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in infants.
Pharmacology Caffeine, a naturally occurring xanthine derivative like theobromine and the bronchodilator theophylline, is used as a CNS stimulant, mild diuretic, and respiratory stimulant (in neonates with apnea of prematurity). Often combined with analgesics or with ergot alkaloids, caffeine is used to treat migraine and other headache types. Over the counter, caffeine is available to treat drowsiness or mild water-weight gain.
Mechanism of Action Caffeine stimulates medullary, vagal, vasomotor, and respiratory centers, promoting bradycardia, vasoconstriction, and increased respiratory rate. This action was previously believed to be due primarily to increased intracellular cyclic 3′,5′-adenosine monophosphate (cyclic AMP) following inhibition of phosphodiesterase, the enzyme that degrades cyclic AMP. It is now thought that xanthines such as caffeine act as agonists at adenosine-receptors within the plasma membrane of virtually every cell. As adenosine acts as an autocoid, inhibiting the release of neurotransmitters from presynaptic sites but augmenting the actions of norepinephrine or angiotensin, antagonism of adenosine receptors promotes neurotransmitter release. This explains the stimulatory effects of caffeine. Blockade of the adenosine A1 receptor in the heart leads to the accelerated, pronounced "pounding" of the heart upon caffeine intake.
Absorption Readily absorbed after oral or parenteral administration. The peak plasma level for caffeine range from 6-10mg/L and the mean time to reach peak concentration ranged from 30 minutes to 2 hours.
Toxicity LD50=127 mg/kg (orally in mice)
Protein Binding Low (25 to 36%).
Biotransformation Hepatic cytochrome P450 1A2 (CYP 1A2) is involved in caffeine biotransformation. About 80% of a dose of caffeine is metabolized to paraxanthine (1,7-dimethylxanthine), 10% to theobromine (3,7-dimethylxanthine), and 4% to theophylline (1,3-dimethylxanthine).
Half Life 3 to 7 hours in adults, 65 to 130 hours in neonates
Dosage Forms
Form Route
Capsule Oral
Elixir Oral
Liquid Oral
Pill Oral
Solution Oral
Solution / drops Oral
Suppository Rectal
Suspension Oral
Syrup Oral
Tablet Oral
Tablet, extended release 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. Nehlig A, Daval JL, Debry G: Caffeine and the central nervous system: mechanisms of action, biochemical, metabolic and psychostimulant effects. Brain Res Brain Res Rev. 1992 May-Aug;17(2):139-70. [PubMed Link Image]
  2. Smit HJ, Gaffan EA, Rogers PJ: Methylxanthines are the psycho-pharmacologically active constituents of chocolate. Psychopharmacology (Berl). 2004 Nov;176(3-4):412-9. Epub 2004 May 5. [PubMed Link Image]
  3. Haskell CF, Kennedy DO, Wesnes KA, Milne AL, Scholey AB: A double-blind, placebo-controlled, multi-dose evaluation of the acute behavioural effects of guarana in humans. J Psychopharmacol. 2007 Jan;21(1):65-70. Epub 2006 Mar 13. [PubMed Link Image]
  4. Benjamin LT Jr, Rogers AM, Rosenbaum A: Coca-Cola, caffeine, and mental deficiency: Harry Hollingworth and the Chattanooga trial of 1911. J Hist Behav Sci. 1991 Jan;27(1):42-55. [PubMed Link Image]
  5. Nathanson JA: Caffeine and related methylxanthines: possible naturally occurring pesticides. Science. 1984 Oct 12;226(4671):184-7. [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 1A2 (CYP1A2)
Targets
  1. Adenosine A1 receptor
  2. cAMP-specific 3',5'-cyclic phosphodiesterase 4B
  3. Adenosine A2a receptor
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 1A2 (CYP1A2)
Enzyme 1 Gene Name CYP1A2
Enzyme 1 SwissProt ID P05177 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >P05177|CP1A2_HUMAN Cytochrome P450 1A2 - Homo sapiens (Human). 
MALSQSVPFSATELLLASAIFCLVFWVLKGLRPRVPKGLKSPPEPWGWPLLGHVLTLGKN
PHLALSRMSQRYGDVLQIRIGSTPVLVLSRLDTIRQALVRQGDDFKGRPDLYTSTLITDG
QSLTFSTDSGPVWAARRRLAQNALNTFSIASDPASSSSCYLEEHVSKEAKALISRLQELM
AGPGHFDPYNQVVVSVANVIGAMCFGQHFPESSDEMLSLVKNTHEFVETASSGNPLDFFP
ILRYLPNPALQRFKAFNQRFLWFLQKTVQEHYQDFDKNSVRDITGALFKHSKKGPRASGN
LIPQEKIVNLVNDIFGAGFDTVTTAISWSLMYLVTKPEIQRKIQKELDTVIGRERRPRLS
DRPQLPYLEAFILETFRHSSFLPFTIPHSTTRDTTLNGFYIPKKCCVFVNQWQVNHDPEL
WEDPSEFRPERFLTADGTAINKPLSEKMMLFGMGKRRCIGEVLAKWEIFLFLAILLQQLE
FSVPPGVKVDLTPIYGLTMKHARCEHVQARRFSIN
Drug Target 1 [top]
Target 1 ID 16
Target 1 Name Adenosine A1 receptor
Target 1 Synonyms Not Available
Target 1 Gene Name ADORA1
Target 1 Protein Sequence >Adenosine A1 receptor 
MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGA
LVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVT
PRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYM
VYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALIL
FLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFL
KIWNDHFRCQPAPPIDEDLPEERPDD
Target 1 Number of Residues 331
Target 1 Molecular Weight 36512
Target 1 Theoretical pI 8.75
Target 1 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
nucleotide receptor activity, G-protein coupled
purinergic nucleotide receptor activity, G-protein coupled
adenosine receptor activity, G-protein coupled
A1 adenosine receptor activity, G-protein coupled
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 A1 adenosine receptor activity, G-protein coupled
Target 1 Specific Function Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 11-33
  • 47-69
  • 81-102
  • 124-146
  • 177-201
  • 236-259
  • 268-292
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 256155 Link Image
Target 1 UniProtKB/Swiss-Prot ID P30542 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name AA1R_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >981 bp 
ATGCCGCCCTCCATCTCAGCTTTCCAGGCCGCCTACATCGGCATCGAGGTGCTCATCGCC
CTGGTCTCTGTGCCCGGGAACGTGCTGGTGATCTGGGCGGTGAAGGTGAACCAGGCGCTG
CGGGATGCCACCTTCTGCTTCATCGTGTCGCTGGCGGTGGCTGATGTGGCCGTGGGTGCC
CTGGTCATCCCCCTCGCCATCCTCATCAACATTGGGCCACAGACCTACTTCCACACCTGC
CTCATGGTTGCCTGTCCGGTCCTCATCCTCACCCAGAGCTCCATCCTGGCCCTGCTGGCA
ATTGCGGTGGACCGCTACCTCCGGGTCAAGATCCCTCTCCGGTACAAGATGGTGGTGACC
CCCCGGAGGGCGGCGGTGGCCATAGCCGGCTGCTGGATCCTCTCCTTCGTGGTGGGACTG
ACCCCTATGTTTGGCTGGAACAATCTGAGTGCGGTGGAGCGGGCCTGGGCAGCCAACGGC
AGCATGGGGGAGCCCGTGATCAAGTGCGAGTTCGAGAAGGTCATCAGCATGGAGTACATG
GTCTACTTCAACTTCTTTGTGTGGGTGCTCCCCCCGCTTCTCCTCATGGTCCTCATCTAC
CTGGAGGTCTTCTACCTAATCCGCAAGCAGCTCAACAAGAAGGTGTCGGCCTCCTCCGGC
GACCCGCAGAAGTACTATGGGAAGGAGCTGAAGATCGCCAAGTCGCTGGCCCTCATCCTC
TTCCTCTTTGCCCTCAGCTGGCTGCCTTTGCACATCCTCAACTGCATCACCCTCTTCTGC
CCGTCCTGCCACAAGCCCAGCATCCTTACCTACATTGCCATCTTCCTCACGCACGGCAAC
TCGGCCATGAACCCCATTGTCTATGCCTTCCGCATCCAGAAGTTCCGCGTCACCTTCCTT
AAGATTTGGAATGACCATTTCCGCTGCCAGCCTGCACCTCCCATTGACGAGGATCTCCCA
GAAGAGAGGCCTGATGACTAG
Target 1 GenBank Gene ID
Target 1 GeneCard ID ADORA1 Link Image
Target 1 GenAtlas ID ADORA1 Link Image
Target 1 HGNC ID HGNC:262 Link Image
Target 1 Chromosome Location 1
Target 1 Locus 1q32.1
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Townsend-Nicholson A, Shine J: Molecular cloning and characterisation of a human brain A1 adenosine receptor cDNA. Brain Res Mol Brain Res. 1992 Dec;16(3-4):365-70. [PubMed Link Image]
  2. Libert F, Van Sande J, Lefort A, Czernilofsky A, Dumont JE, Vassart G, Ensinger HA, Mendla KD: Cloning and functional characterization of a human A1 adenosine receptor. Biochem Biophys Res Commun. 1992 Sep 16;187(2):919-26. [PubMed Link Image]
  3. Ren H, Stiles GL: Characterization of the human A1 adenosine receptor gene. Evidence for alternative splicing. J Biol Chem. 1994 Jan 28;269(4):3104-10. [PubMed Link Image]
Target 1 Drug References
  1. Gaytan SP, Saadani-Makki F, Bodineau L, Frugiere A, Larnicol N, Pasaro R: Effect of postnatal exposure to caffeine on the pattern of adenosine A1 receptor distribution in respiration-related nuclei of the rat brainstem. Auton Neurosci. 2006 Jun 30;126-127:339-46. Epub 2006 May 15. [PubMed Link Image]
  2. Listos J, Malec D, Fidecka S: Adenosine receptor antagonists intensify the benzodiazepine withdrawal signs in mice. Pharmacol Rep. 2006 Sep-Oct;58(5):643-51. [PubMed Link Image]
  3. Rieg T, Schnermann J, Vallon V: Adenosine A1 receptors determine effects of caffeine on total fluid intake but not caffeine appetite. Eur J Pharmacol. 2007 Jan 26;555(2-3):174-7. Epub 2006 Oct 25. [PubMed Link Image]
  4. Mustafa S, Venkatesh P, Pasha K, Mullangi R, Srinivas NR: Altered intravenous pharmacokinetics of topotecan in rats with acute renal failure (ARF) induced by uranyl nitrate: do adenosine A1 antagonists (selective/non-selective) normalize the altered topotecan kinetics in ARF? Xenobiotica. 2006 Dec;36(12):1239-58. [PubMed Link Image]
  5. Wang SJ: Caffeine facilitation of glutamate release from rat cerebral cortex nerve terminals (synaptosomes) through activation protein kinase C pathway: an interaction with presynaptic adenosine A1 receptors. Synapse. 2007 Jun;61(6):401-11. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 541
Target 2 Name cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Target 2 Synonyms
  1. DPDE4
  2. EC 3.1.4.17
  3. PDE32
Target 2 Gene Name PDE4B
Target 2 Protein Sequence >cAMP-specific 3',5'-cyclic phosphodiesterase 4B 
MKKSRSVMTVMADDNVKDYFECSLSKSYSSSSNTLGIDLWRGRRCCSGNLQLPPLSQRQS
ERARTPEGDGISRPTTLPLTTLPSIAITTVSQECFDVENGPSPGRSPLDPQASSSAGLVL
HATFPGHSQRRESFLYRSDSDYDLSPKAMSRNSSLPSEQHGDDLIVTPFAQVLASLRSVR
NNFTILTNLHGTSNKRSPAASQPPVSRVNPQEESYQKLAMETLEELDWCLDQLETIQTYR
SVSEMASNKFKRMLNRELTHLSEMSRSGNQVSEYISNTFLDKQNDVEIPSPTQKDREKKK
KQQLMTQISGVKKLMHSSSLNNTSISRFGVNTENEDHLAKELEDLNKWGLNIFNVAGYSH
NRPLTCIMYAIFQERDLLKTFRISSDTFITYMMTLEDHYHSDVAYHNSLHAADVAQSTHV
LLSTPALDAVFTDLEILAAIFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHL
AVGFKLLQEEHCDIFMNLTKKQRQTLRKMVIDMVLATDMSKHMSLLADLKTMVETKKVTS
SGVLLLDNYTDRIQVLRNMVHCADLSNPTKSLELYRQWTDRIMEEFFQQGDKERERGMEI
SPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVQPDAQDILDTLEDNRNWYQSMIPQSP
SPPLDEQNRDCQGLMEKFQFELTLDEEDSEGPEKEGEGHSYFSSTKTLCVIDPENRDSLG
ETDIDIATEDKSPVDT
Target 2 Number of Residues 748
Target 2 Molecular Weight 83344
Target 2 Theoretical pI 4.89
Target 2 GO Classification
Function
hydrolase activity
hydrolase activity, acting on ester bonds
phosphoric ester hydrolase activity
phosphoric diester hydrolase activity
cyclic-nucleotide phosphodiesterase activity
3',5'-cyclic-nucleotide phosphodiesterase activity
catalytic activity
Process
cellular process
cell communication
signal transduction
Component
Not Available
Target 2 General Function Involved in cAMP phosphodiesterase activity
Target 2 Specific Function May be involved in mediating central nervous system effects of therapeutic agents ranging from antidepressants to antiasthmatic and anti-inflammatory agents
Target 2 Pathways
Name SMPDB Link KEGG Link
Purine metabolism SMP00050 Link Image map00230 Link Image
Target 2 Reactions
  • nucleoside 3',5'-cyclic phosphate + H2O = nucleoside 5'-phosphate
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 347122 Link Image
Target 2 UniProtKB/Swiss-Prot ID Q07343 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name PDE4B_HUMAN Link Image
Target 2 PDB ID 1TB5 Link Image
Target 2 PDB File Show
Target 2 3D Structure
Target 2 Cellular Location
  • Cytoplasmic
Target 2 Gene Sequence >2211 bp 
ATGAAGAAAAGCAGGAGTGTGATGACGGTGATGGCTGATGATAATGTTAAAGATTATTTT
GAATGTAGCTTGAGTAAATCCTACAGTTCTTCCAGTAACACACTTGGGATCGACCTCTGG
AGAGGGAGAAGGTGTTGCTCAGGAAACTTACAGTTACCACCACTGTCTCAAAGACAGAGT
GAAAGGGCAAGGACTCCTGAGGGAGATGGTATTTCCAGGCCGACCACACTGCCTTTGACA
ACGCTTCCAAGCATTGCTATTACAACTGTAAGCCAGGAGTGCTTTGATGTGGAAAATGGC
CCTTCCCCAGGTCGGAGTCCACTGGATCCCCAGGCCAGCTCTTCCGCTGGGCTGGTACTT
CACGCCACCTTTCCTGGGCACAGCCAGCGCAGAGAGTCATTTCTCTACAGATCAGACAGC
GACTATGACTTGTCACCAAAGGCGATGTCGAGAAACTCTTCTCTTCCAAGCGAGCAACAC
GGCGATGACTTGATTGTAACTCCTTTTGCCCAGGTCCTTGCCAGCTTGCGAAGTGTGAGA
AACAACTTCACTATACTGACAAACCTTCATGGTACATCTAACAAGAGGTCCCCAGCTGCT
AGTCAGCCTCCTGTCTCCAGAGTCAACCCACAAGAAGAATCTTATCAAAAATTAGCAATG
GAAACGCTGGAGGAATTAGACTGGTGTTTAGACCAGCTAGAGACCATACAGACCTACCGG
TCTGTCAGTGAGATGGCTTCTAACAAGTTCAAAAGAATGCTGAACCGGGAGCTGACACAC
CTCTCAGAGATGAGCCGATCAGGGAACCAGGTGTCTGAATACATTTCAAATACTTTCTTA
GACAAGCAGAATGATGTGGAGATCCCATCTCCTACCCAGAAAGACAGGGAGAAAAAGAAA
AAGCAGCAGCTCATGACCCAGATAAGTGGAGTGAAGAAATTAATGCATAGTTCAAGCCTA
AACAATACAAGCATCTCACGCTTTGGAGTCAACACTGAAAATGAAGATCACCTGGCCAAG
GAGCTGGAAGACCTGAACAAATGGGGTCTTAACATCTTTAATGTGGCTGGATATTCTCAC
AATAGACCCCTAACATGCATCATGTATGCTATATTCCAGGAAAGAGACCTCCTAAAGACA
TTCAGAATCTCATCTGACACATTTATAACCTACATGATGACTTTAGAAGACCATTACCAT
TCTGACGTGGCATATCACAACAGCCTGCACGCTGCTGATGTAGCCCAGTCGACCCATGTT
CTCCTTTCTACACCAGCATTAGACGCTGTCTTCACAGATTTGGAGATCCTGGCTGCCATT
TTTGCAGCTGCCATCCATGACGTTGATCATCCTGGAGTCTCCAATCAGTTTCTCATCAAC
ACAAATTCAGAACTTGCTTTGATGTATAATGATGAATCTGTGTTGGAAAATCATCACCTT
GCTGTGGGTTTCAAACTGCTGCAAGAAGAACACTGTGACATCTTCATGAATCTCACCAAG
AAGCAGCGTCAGACACTCAGGAAGATGGTTATTGACATGGTGTTAGCAACTGATATGTCT
AAACATATGAGCCTGCTGGCAGACCTGAAGACAATGGTAGAAACGAAGAAAGTTACAAGT
TCAGGCGTTCTTCTCCTAGACAACTATACCGATCGCATTCAGGTCCTTCGCAACATGGTA
CACTGTGCAGACCTGAGCAACCCCACCAAGTCCTTGGAATTGTATCGGCAATGGACAGAC
CGCATCATGGAGGAATTTTTCCAGCAGGGAGACAAAGAGCGGGAGAGGGGAATGGAAATT
AGCCCAATGTGTGATAAACACACAGCTTCTGTGGAAAAATCCCAGGTTGGTTTCATCGAC
TACATTGTCCATCCATTGTGGGAGACATGGGCAGATTTGGTACAGCCTGATGCTCAGGAC
ATTCTCGATACCTTAGAAGATAACAGGAACTGGTATCAGAGCATGATACCTCAAAGTCCC
TCACCACCACTGGACGAGCAGAACAGGGACTGCCAGGGTCTGATGGAGAAGTTTCAGTTT
GAACTGACTCTCGATGAGGAAGATTCTGAAGGACCTGAGAAGGAGGGAGAGGGACACAGC
TATTTCAGCAGCACAAAGACGCTTTGTGTGATTGATCCAGAAAACAGAGATTCCCTGGGA
GAGACTGACATAGACATTGCAACAGAAGACAAGTCCCCCGTGGATACATAA
Target 2 GenBank Gene ID
Target 2 GeneCard ID PDE4B Link Image
Target 2 GenAtlas ID PDE4B Link Image
Target 2 HGNC ID HGNC:8781 Link Image
Target 2 Chromosome Location 1
Target 2 Locus 1p31
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. McLaughlin MM, Cieslinski LB, Burman M, Torphy TJ, Livi GP: A low-Km, rolipram-sensitive, cAMP-specific phosphodiesterase from human brain. Cloning and expression of cDNA, biochemical characterization of recombinant protein, and tissue distribution of mRNA. J Biol Chem. 1993 Mar 25;268(9):6470-6. [PubMed Link Image]
  2. Bolger G, Michaeli T, Martins T, St John T, Steiner B, Rodgers L, Riggs M, Wigler M, Ferguson K: A family of human phosphodiesterases homologous to the dunce learning and memory gene product of Drosophila melanogaster are potential targets for antidepressant drugs. Mol Cell Biol. 1993 Oct;13(10):6558-71. [PubMed Link Image]
  3. Huston E, Lumb S, Russell A, Catterall C, Ross AH, Steele MR, Bolger GB, Perry MJ, Owens RJ, Houslay MD: Molecular cloning and transient expression in COS7 cells of a novel human PDE4B cAMP-specific phosphodiesterase, HSPDE4B3. Biochem J. 1997 Dec 1;328 ( Pt 2):549-58. [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 1178
Target 3 Name Adenosine A2a receptor
Target 3 Synonyms Not Available
Target 3 Gene Name ADORA2A
Target 3 Protein Sequence >Adenosine A2a receptor 
MPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAAADIAVGVLAI
PFAITISTGFCAACHGCLFIACFVLVLTQSSIFSLLAIAIDRYIAIRIPLRYNGLVTGTR
AKGIIAICWVLSFAIGLTPMLGWNNCGQPKEGKNHSQGCGEGQVACLFEDVVPMNYMVYF
NFFACVLVPLLLMLGVYLRIFLAARRQLKQMESQPLPGERARSTLQKEVHAAKSLAIIVG
LFALCWLPLHIINCFTFFCPDCSHAPLWLMYLAIVLSHTNSVVNPFIYAYRIREFRQTFR
KIIRSHVLRQQEPFKAAGTSARVLAAHGSDGEQVSLRLNGHPPGVWANGSAPHPERRPNG
YALGLVSGGSAQESQGNTGLPDVELLSHELKGVCPEPPGLDDPLAQDGAGVS
Target 3 Number of Residues 418
Target 3 Molecular Weight 44708
Target 3 Theoretical pI 8.05
Target 3 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
nucleotide receptor activity, G-protein coupled
purinergic nucleotide receptor activity, G-protein coupled
adenosine receptor activity, G-protein coupled
A2A adenosine receptor activity, G-protein coupled
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 A2A adenosine receptor activity, G-protein coupled
Target 3 Specific Function Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 8-30
  • 44-66
  • 78-100
  • 121-143
  • 174-198
  • 235-258
  • 267-290
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 177892 Link Image
Target 3 UniProtKB/Swiss-Prot ID P29274 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name AA2AR_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >1230 bp 
ATGGGCTCCTCGGTGTACATCACGGTGGAGCTGGCCATTGCTGTGCTGGCCATCCTGGGC
AATGTGCTGGTGTGCTGGGCCGTGTGGCTCAACAGCAACCTGCAGAACGTCACCAACTAC
TTTGTGGTGTCACTGGCGGCGGCCGACATCGCAGTGGGTGTGCTCGCCATCCCCTTTGCC
ATCACCATCAGCACCGGGTTCTGCGCTGCCTGCCACGGCTGCCTCTTCATTGCCTGCTTC
GTCCTGGTCCTCACGCAGAGCTCCATCTTCAGTCTCCTGGCCATCGCCATTGACCGCTAC
ATTGCCATCCGCATCCCGCTCCGGTACAATGGCTTGGTGACCGGCACGAGGGCTAAGGGC
ATCATTGCCATCTGCTGGGTGCTGTCGTTTGCCATCGGCCTGACTCCCATGCTAGGTTGG
AACAACTGCGGTCAGCCAAAGGAGGGCAAGAACCACTCCCAGGGCTGCGGGGAGGGCCAA
GTGGCCTGTCTCTTTGAGGATGTGGTCCCCATGAACTACATGGTGTACTTCAACTTCTTT
GCCTGTGTGCTGGTGCCCCTGCTGCTCATGCTGGGTGTCTATTTGCGGATCTTCCTGGCG
GCGCGACGACAGCTGAAGCAGATGGAGAGCCAGCCTCTGCCGGGGGAGCGGGCACGGTCC
ACACTGCAGAAGGAGGTCCATGCTGCCAAGTCACTGGCCATCATTGTGGGGCTCTTTGCC
CTCTGCTGGCTGCCCCTACACATCATCAACTGCTTCACTTTCTTCTGCCCCGACTGCAGC
CACGCCCCTCTCTGGCTCATGTACCTGGCCATCGTCCTCTCCCACACCAATTCGGTTGTG
AATCCCTTCATCTACGCCTACCGTATCCGCGAGTTCCGCCAGACCTTCCGCAAGATCATT
CGCAGCCACGTCCTGAGGCAGCAAGAACCTTTCAAGGCAGCTGGCACCAGTGCCCGGGTC
TTGGCAGCTCATGGCAGTGACGGAGAGCAGGTCAGCCTCCGTCTCAACGGCCACCCGCCA
GGAGTGTGGGCCAACGGCAGTGCTCCCCACCCTGAGCGGAGGCCCAATGGCTATGCCCTG
GGGCTGGTGAGTGGAGGGAGTGCCCAAGAGTCCCAGGGGAACACGGGCCTCCCAGACGTG
GAGCTCCTTAGCCATGAGCTCAAGGGAGTGTGCCCAGAGCCCCCTGGCCTAGATGACCCC
CTGGCCCAGGATGGAGCAGGAGTGTCCTGA
Target 3 GenBank Gene ID
Target 3 GeneCard ID ADORA2A Link Image
Target 3 GenAtlas ID ADORA2A Link Image
Target 3 HGNC ID HGNC:263 Link Image
Target 3 Chromosome Location 22
Target 3 Locus 22q11.23
Target 3 SNPs SNPJam Report Link Image
Target 3 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. Furlong TJ, Pierce KD, Selbie LA, Shine J: Molecular characterization of a human brain adenosine A2 receptor. Brain Res Mol Brain Res. 1992 Sep;15(1-2):62-6. [PubMed Link Image]
  3. Kim J, Wess J, van Rhee AM, Schoneberg T, Jacobson KA: Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem. 1995 Jun 9;270(23):13987-97. [PubMed Link Image]
  4. Le F, Townsend-Nicholson A, Baker E, Sutherland GR, Schofield PR: Characterization and chromosomal localization of the human A2a adenosine receptor gene: ADORA2A. Biochem Biophys Res Commun. 1996 Jun 14;223(2):461-7. [PubMed Link Image]
Target 3 Drug References
  1. Riksen NP, Franke B, van den Broek P, Smits P, Rongen GA: The 1976C>T polymorphism in the adenosine A2A receptor gene does not affect the vasodilator response to adenosine in humans in vivo. Pharmacogenet Genomics. 2007 Jul;17(7):551-4. [PubMed Link Image]
  2. Zhao G, Messina E, Xu X, Ochoa M, Sun HL, Leung K, Shryock J, Belardinelli L, Hintze TH: Caffeine attenuates the duration of coronary vasodilation and changes in hemodynamics induced by regadenoson (CVT-3146), a novel adenosine A2A receptor agonist. J Cardiovasc Pharmacol. 2007 Jun;49(6):369-75. [PubMed Link Image]
  3. Cornelis MC, El-Sohemy A, Campos H: Genetic polymorphism of the adenosine A2A receptor is associated with habitual caffeine consumption. Am J Clin Nutr. 2007 Jul;86(1):240-4. [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.