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Identification
NameRamelteon
Accession NumberDB00980  (APRD01213)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Ramelteon is the first in a new class of sleep agents that selectively binds to the melatonin receptors in the suprachiasmatic nucleus (SCN). It is used for insomnia, particularly delayed sleep onset. Ramelteon has not been shown to produce dependence and has shown no potential for abuse.

Structure
Thumb
Synonyms
Rozerem
External Identifiers
  • TAK-375
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rozeremtablet, film coated8 mg/1oralRebel Distributors Corp2005-07-222016-04-05Us
Rozeremtablet, film coated8 mg/1oralAvera Mc Kennan Hospital2015-03-052016-04-05Us
Rozeremtablet, film coated8 mg/1oralTakeda Pharmaceuticals America, Inc.2005-07-222016-04-05Us
Rozeremtablet, film coated8 mg/1oralbryant ranch prepack2005-07-222016-04-05Us
Rozeremtablet, film coated8 mg/1oralPhysicians Total Care, Inc.2006-08-012016-04-05Us
Rozeremtablet, film coated8 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-05-182016-04-05Us
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII901AS54I69
CAS number196597-26-9
WeightAverage: 259.3434
Monoisotopic: 259.157228921
Chemical FormulaC16H21NO2
InChI KeyInChIKey=YLXDSYKOBKBWJQ-LBPRGKRZSA-N
InChI
InChI=1S/C16H21NO2/c1-2-15(18)17-9-7-12-4-3-11-5-6-14-13(16(11)12)8-10-19-14/h5-6,12H,2-4,7-10H2,1H3,(H,17,18)/t12-/m0/s1
IUPAC Name
N-{2-[(8S)-1H,2H,6H,7H,8H-indeno[5,4-b]furan-8-yl]ethyl}propanamide
SMILES
CCC(=O)NCC[C@@H]1CCC2=C1C1=C(OCC1)C=C2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzofurans. These are organic compounds containing a benzene ring fused to a furan. Furan is a five-membered aromatic ring with four carbon atoms and one oxygen atom.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzofurans
Sub ClassNot Available
Direct ParentBenzofurans
Alternative Parents
Substituents
  • Indane
  • Benzofuran
  • Alkyl aryl ether
  • Benzenoid
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Oxacycle
  • Ether
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of insomnia characterized by difficulty with sleep onset.
PharmacodynamicsRamelteon is the first selective melatonin agonist. It works by mimicking melatonin (MT), a naturally occuring hormone that is produced during the sleep period and thought to be responsible for the regulation of circadian rhythm underlying the normal sleep-wake cycle. Ramelteon has a high affinity for the MT1 and MT2 receptors. The MT1 and MT2 receptors are located in the brain's suprachiasmatic nuclei (SCN),which is known as the body's "master clock" because it regulates the 24-hour sleep-wake cycle. Ramelteon has an active metabolite that is less potent but circulates in higher concentrations than the parent compound. The metabolite also has weak affinity for the 5HT2b receptor.
Mechanism of actionRamelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors, and lower selectivity for the MT3 receptor. Melatonin production is concurrent with nocturnal sleep, meaning that an increase in melatonin levels is related to the onset of self-reported sleepiness and an increase in sleep propensity. MT1 receptors are believed to be responsible for regulation of sleepiness and facilitation of sleep onset, and MT2 receptors are believed to mediate phase-shifting effects of melatonin on the circadian rhythm. While MT1 and MT2 receptors are associated with the sleep-wake cycle, MT3 has a completely different profile, and therefore is not likely to be involved in the sleep-wake cycle. Remelteon has no appreciable affinity for the gamma-aminobutyric acid (GABA) receptor complex or receptors that bind neuropeptides, cytokines, serotonin, dopamine, norepinephrine, acetylcholine, or opiates.
Related Articles
AbsorptionRapid, total absorption is at least 84%.
Volume of distribution
  • 73.6 L
Protein binding~82% (in human serum)
Metabolism

Hepatic

Route of eliminationFollowing oral administration of radiolabeled ramelteon, 84% of total radioactivity was excreted in urine and approximately 4% in feces, resulting in a mean recovery of 88%. Less than 0.1% of the dose was excreted in urine and feces as the parent compound.
Half life~1-2.6 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9934
Caco-2 permeable+0.5893
P-glycoprotein substrateSubstrate0.5211
P-glycoprotein inhibitor INon-inhibitor0.8548
P-glycoprotein inhibitor IINon-inhibitor0.7877
Renal organic cation transporterNon-inhibitor0.6381
CYP450 2C9 substrateNon-substrate0.7876
CYP450 2D6 substrateNon-substrate0.6392
CYP450 3A4 substrateSubstrate0.512
CYP450 1A2 substrateInhibitor0.7314
CYP450 2C9 inhibitorNon-inhibitor0.6471
CYP450 2D6 inhibitorNon-inhibitor0.5916
CYP450 2C19 inhibitorInhibitor0.8314
CYP450 3A4 inhibitorNon-inhibitor0.9196
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7763
Ames testNon AMES toxic0.7016
CarcinogenicityNon-carcinogens0.8206
BiodegradationReady biodegradable0.6635
Rat acute toxicity2.1034 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7898
hERG inhibition (predictor II)Inhibitor0.5
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Takeda global research development center inc
Packagers
Dosage forms
FormRouteStrength
Tablet, film coatedoral8 mg/1
Prices
Unit descriptionCostUnit
Rozerem 8 mg tablet5.17USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6034239 No1999-07-222019-07-22Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP2.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0164 mg/mLALOGPS
logP3.03ALOGPS
logP2.57ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)15.82ChemAxon
pKa (Strongest Basic)-0.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area38.33 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity75.52 m3·mol-1ChemAxon
Polarizability29.99 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Vinod Kumar Kansal, Dhirenkumar N. Mistry, Sanjay L. Vasoya, “Intermediates and processes for the synthesis of Ramelteon.” U.S. Patent US20080242877, issued October 02, 2008.

US20080242877
General References
  1. Karim A, Tolbert D, Cao C: Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia. J Clin Pharmacol. 2006 Feb;46(2):140-8. [PubMed:16432265 ]
  2. Miyamoto M: Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders. CNS Neurosci Ther. 2009 Winter;15(1):32-51. doi: 10.1111/j.1755-5949.2008.00066.x. [PubMed:19228178 ]
  3. Pandi-Perumal SR, Srinivasan V, Spence DW, Moscovitch A, Hardeland R, Brown GM, Cardinali DP: Ramelteon: a review of its therapeutic potential in sleep disorders. Adv Ther. 2009 Jun;26(6):613-26. doi: 10.1007/s12325-009-0041-6. Epub 2009 Jun 30. [PubMed:19568703 ]
  4. Borja NL, Daniel KL: Ramelteon for the treatment of insomnia. Clin Ther. 2006 Oct;28(10):1540-55. [PubMed:17157111 ]
  5. Roth T, Stubbs C, Walsh JK: Ramelteon (TAK-375), a selective MT1/MT2-receptor agonist, reduces latency to persistent sleep in a model of transient insomnia related to a novel sleep environment. Sleep. 2005 Mar;28(3):303-7. [PubMed:16173650 ]
  6. Simpson D, Curran MP: Ramelteon: a review of its use in insomnia. Drugs. 2008;68(13):1901-19. [PubMed:18729542 ]
External Links
ATC CodesN05CH02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (2.36 MB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Ramelteon can be increased when it is combined with Abiraterone.
AtazanavirThe serum concentration of Ramelteon can be increased when it is combined with Atazanavir.
AzelastineRamelteon may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Ramelteon.
BoceprevirThe serum concentration of Ramelteon can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Ramelteon can be decreased when combined with Bortezomib.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
BuprenorphineRamelteon may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CapecitabineThe serum concentration of Ramelteon can be increased when it is combined with Capecitabine.
CeritinibThe serum concentration of Ramelteon can be increased when it is combined with Ceritinib.
ClarithromycinThe serum concentration of Ramelteon can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Ramelteon can be increased when it is combined with Cobicistat.
DarunavirThe serum concentration of Ramelteon can be increased when it is combined with Darunavir.
DeferasiroxThe serum concentration of Ramelteon can be increased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Ramelteon can be increased when it is combined with Delavirdine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
EthanolRamelteon may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FloxuridineThe serum concentration of Ramelteon can be increased when it is combined with Floxuridine.
FluconazoleThe serum concentration of Ramelteon can be increased when it is combined with Fluconazole.
FluorouracilThe serum concentration of Ramelteon can be increased when it is combined with Fluorouracil.
FluvoxamineThe serum concentration of Ramelteon can be increased when it is combined with Fluvoxamine.
GemfibrozilThe serum concentration of Ramelteon can be increased when it is combined with Gemfibrozil.
HydrocodoneRamelteon may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
IdelalisibThe serum concentration of Ramelteon can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Ramelteon can be increased when it is combined with Indinavir.
ItraconazoleThe serum concentration of Ramelteon can be increased when it is combined with Itraconazole.
KetoconazoleThe serum concentration of Ramelteon can be increased when it is combined with Ketoconazole.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Ramelteon.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
MethotrimeprazineRamelteon may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineRamelteon may increase the sedative activities of Metyrosine.
MexiletineThe metabolism of Ramelteon can be decreased when combined with Mexiletine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
MirtazapineRamelteon may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
NefazodoneThe serum concentration of Ramelteon can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Ramelteon can be increased when it is combined with Nelfinavir.
NicardipineThe serum concentration of Ramelteon can be increased when it is combined with Nicardipine.
OrphenadrineRamelteon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeRamelteon may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Ramelteon is combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Ramelteon can be increased when it is combined with Peginterferon alfa-2b.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
PosaconazoleThe serum concentration of Ramelteon can be increased when it is combined with Posaconazole.
PramipexoleRamelteon may increase the sedative activities of Pramipexole.
RifabutinThe metabolism of Ramelteon can be increased when combined with Rifabutin.
RifampicinThe metabolism of Ramelteon can be increased when combined with Rifampicin.
RifapentineThe metabolism of Ramelteon can be increased when combined with Rifapentine.
RitonavirThe serum concentration of Ramelteon can be increased when it is combined with Ritonavir.
RopiniroleRamelteon may increase the sedative activities of Ropinirole.
RotigotineRamelteon may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ramelteon.
SaquinavirThe serum concentration of Ramelteon can be increased when it is combined with Saquinavir.
Sodium oxybateRamelteon may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
SulfadiazineThe serum concentration of Ramelteon can be increased when it is combined with Sulfadiazine.
SulfisoxazoleThe serum concentration of Ramelteon can be increased when it is combined with Sulfisoxazole.
SuvorexantRamelteon may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
TelaprevirThe serum concentration of Ramelteon can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Ramelteon can be increased when it is combined with Telithromycin.
ThalidomideRamelteon may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TolbutamideThe serum concentration of Ramelteon can be increased when it is combined with Tolbutamide.
VemurafenibThe serum concentration of Ramelteon can be increased when it is combined with Vemurafenib.
VoriconazoleThe serum concentration of Ramelteon can be increased when it is combined with Voriconazole.
ZolpidemRamelteon may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Do not take with or immediately after a high-fat meal.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
multitarget
General Function:
Melatonin receptor activity
Specific Function:
High affinity receptor for melatonin. Likely to mediates the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity.
Gene Name:
MTNR1B
Uniprot ID:
P49286
Molecular Weight:
40187.895 Da
References
  1. Kato K, Hirai K, Nishiyama K, Uchikawa O, Fukatsu K, Ohkawa S, Kawamata Y, Hinuma S, Miyamoto M: Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology. 2005 Feb;48(2):301-10. [PubMed:15695169 ]
  2. Karim A, Tolbert D, Cao C: Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia. J Clin Pharmacol. 2006 Feb;46(2):140-8. [PubMed:16432265 ]
  3. Greenblatt DJ, Harmatz JS, Karim A: Age and gender effects on the pharmacokinetics and pharmacodynamics of ramelteon, a hypnotic agent acting via melatonin receptors MT1 and MT2. J Clin Pharmacol. 2007 Apr;47(4):485-96. [PubMed:17389558 ]
  4. Roth T, Stubbs C, Walsh JK: Ramelteon (TAK-375), a selective MT1/MT2-receptor agonist, reduces latency to persistent sleep in a model of transient insomnia related to a novel sleep environment. Sleep. 2005 Mar;28(3):303-7. [PubMed:16173650 ]
  5. Miyamoto M: Effect of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist, on motor performance in mice. Neurosci Lett. 2006 Jul 24;402(3):201-4. Epub 2006 May 24. [PubMed:16730121 ]
  6. Authors unspecified: Ramelteon: TAK 375. Drugs R D. 2005;6(3):186-8. [PubMed:15869323 ]
  7. Miyamoto M: Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders. CNS Neurosci Ther. 2009 Winter;15(1):32-51. doi: 10.1111/j.1755-5949.2008.00066.x. [PubMed:19228178 ]
  8. Miyamoto M: [A novel therapeutic drug: ramelteon]. Nihon Rinsho. 2009 Aug;67(8):1595-600. [PubMed:19768947 ]
  9. Pandi-Perumal SR, Srinivasan V, Spence DW, Moscovitch A, Hardeland R, Brown GM, Cardinali DP: Ramelteon: a review of its therapeutic potential in sleep disorders. Adv Ther. 2009 Jun;26(6):613-26. doi: 10.1007/s12325-009-0041-6. Epub 2009 Jun 30. [PubMed:19568703 ]
  10. Borja NL, Daniel KL: Ramelteon for the treatment of insomnia. Clin Ther. 2006 Oct;28(10):1540-55. [PubMed:17157111 ]
  11. Johnson MW, Suess PE, Griffiths RR: Ramelteon: a novel hypnotic lacking abuse liability and sedative adverse effects. Arch Gen Psychiatry. 2006 Oct;63(10):1149-57. [PubMed:17015817 ]
  12. Zammit G, Erman M, Wang-Weigand S, Sainati S, Zhang J, Roth T: Evaluation of the efficacy and safety of ramelteon in subjects with chronic insomnia. J Clin Sleep Med. 2007 Aug 15;3(5):495-504. [PubMed:17803013 ]
  13. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
multitarget
General Function:
Organic cyclic compound binding
Specific Function:
High affinity receptor for melatonin. Likely to mediates the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity.
Gene Name:
MTNR1A
Uniprot ID:
P48039
Molecular Weight:
39374.315 Da
References
  1. Kato K, Hirai K, Nishiyama K, Uchikawa O, Fukatsu K, Ohkawa S, Kawamata Y, Hinuma S, Miyamoto M: Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology. 2005 Feb;48(2):301-10. [PubMed:15695169 ]
  2. Karim A, Tolbert D, Cao C: Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia. J Clin Pharmacol. 2006 Feb;46(2):140-8. [PubMed:16432265 ]
  3. Greenblatt DJ, Harmatz JS, Karim A: Age and gender effects on the pharmacokinetics and pharmacodynamics of ramelteon, a hypnotic agent acting via melatonin receptors MT1 and MT2. J Clin Pharmacol. 2007 Apr;47(4):485-96. [PubMed:17389558 ]
  4. Roth T, Stubbs C, Walsh JK: Ramelteon (TAK-375), a selective MT1/MT2-receptor agonist, reduces latency to persistent sleep in a model of transient insomnia related to a novel sleep environment. Sleep. 2005 Mar;28(3):303-7. [PubMed:16173650 ]
  5. Miyamoto M: Effect of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist, on motor performance in mice. Neurosci Lett. 2006 Jul 24;402(3):201-4. Epub 2006 May 24. [PubMed:16730121 ]
  6. Authors unspecified: Ramelteon: TAK 375. Drugs R D. 2005;6(3):186-8. [PubMed:15869323 ]
  7. Miyamoto M: Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders. CNS Neurosci Ther. 2009 Winter;15(1):32-51. doi: 10.1111/j.1755-5949.2008.00066.x. [PubMed:19228178 ]
  8. Miyamoto M: [A novel therapeutic drug: ramelteon]. Nihon Rinsho. 2009 Aug;67(8):1595-600. [PubMed:19768947 ]
  9. Pandi-Perumal SR, Srinivasan V, Spence DW, Moscovitch A, Hardeland R, Brown GM, Cardinali DP: Ramelteon: a review of its therapeutic potential in sleep disorders. Adv Ther. 2009 Jun;26(6):613-26. doi: 10.1007/s12325-009-0041-6. Epub 2009 Jun 30. [PubMed:19568703 ]
  10. Borja NL, Daniel KL: Ramelteon for the treatment of insomnia. Clin Ther. 2006 Oct;28(10):1540-55. [PubMed:17157111 ]
  11. Johnson MW, Suess PE, Griffiths RR: Ramelteon: a novel hypnotic lacking abuse liability and sedative adverse effects. Arch Gen Psychiatry. 2006 Oct;63(10):1149-57. [PubMed:17015817 ]
  12. Zammit G, Erman M, Wang-Weigand S, Sainati S, Zhang J, Roth T: Evaluation of the efficacy and safety of ramelteon in subjects with chronic insomnia. J Clin Sleep Med. 2007 Aug 15;3(5):495-504. [PubMed:17803013 ]
  13. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Obach RS, Ryder TF: Metabolism of ramelteon in human liver microsomes and correlation with the effect of fluvoxamine on ramelteon pharmacokinetics. Drug Metab Dispos. 2010 Aug;38(8):1381-91. doi: 10.1124/dmd.110.034009. Epub 2010 May 17. [PubMed:20478852 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Obach RS, Ryder TF: Metabolism of ramelteon in human liver microsomes and correlation with the effect of fluvoxamine on ramelteon pharmacokinetics. Drug Metab Dispos. 2010 Aug;38(8):1381-91. doi: 10.1124/dmd.110.034009. Epub 2010 May 17. [PubMed:20478852 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Obach RS, Ryder TF: Metabolism of ramelteon in human liver microsomes and correlation with the effect of fluvoxamine on ramelteon pharmacokinetics. Drug Metab Dispos. 2010 Aug;38(8):1381-91. doi: 10.1124/dmd.110.034009. Epub 2010 May 17. [PubMed:20478852 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on May 04, 2016 02:30