You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameNaltrexone
Accession NumberDB00704  (APRD00005, DB05067)
TypeSmall Molecule
GroupsApproved, Investigational, Vet Approved
Description

Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of naloxone. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence. [PubChem]

Structure
Thumb
Synonyms
17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one
17-(Cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan-6-one
N-Cyclopropylmethyl-14-hydroxydihydromorphinone
N-Cyclopropylmethylnoroxymorphone
Naltrexon
Naltrexona
Naltrexone
Naltrexonum
External Identifiers
  • EN-1639 A
  • UM 792
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Naltrexone Hydrochloride Tablets USPtablet50 mgoralSterinova IncNot applicableNot applicableCanada
Revia - Tab 50mgtablet50 mgoralDupont Merck Pharma Inc.1995-12-311998-08-13Canada
VivitrolkitAlkermes, Inc.2006-06-132016-04-05Us
VivitrolkitAlkermes, Inc.2006-06-132016-02-13Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-naltrexonetablet50 mgoralTeva Canada Limited1997-10-23Not applicableCanada
Apo-naltrexonetablet50 mgoralApotex Inc2015-11-10Not applicableCanada
Naltrexone Hydrochloridetablet, film coated50 mg/1oralTAGI Pharma Inc.2013-09-232016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralMallinckrodt, Inc.2009-07-292016-04-23Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralUnit Dose Services1998-05-082016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralSun Pharma Global FZE2012-02-292016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralPrecision Dose Inc.2014-10-292016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralPd Rx Pharmaceuticals, Inc.2009-07-292016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralAmerican Health Packaging2012-01-022016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralPd Rx Pharmaceuticals, Inc.1998-05-082016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralbryant ranch prepack1998-05-082016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralAv Kare, Inc.2015-03-262016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralPhysicians Total Care, Inc.2006-04-192016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralAccord Healthcare, Inc.2011-10-012016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralREMEDYREPACK INC.2013-10-072016-04-05Us
Naltrexone Hydrochloridetablet, film coated50 mg/1oralBarr Laboratories Inc.1998-05-082017-08-31Us
Over the Counter ProductsNot Available
International Brands
NameCompany
AbernilMedochemie
AdependAOP Orphan
AntaxonZambon
AntaxonePharmazam
ArropQuimico
CelupanNot Available
DepadeNot Available
DependexAmomed
MorVivaNot Available
NaleronaABL Pharma
NalorexBristol-Myers Squibb
NaltaxNavana
NaltreksonWyeth
NarcoralSirton
NeksiGMP
NemexinBristol-Myers Squibb
OpizoneBritannia
RevezSoubeiran Chobet
TrexanDu Pont
VivitrexNot Available
Brand mixtures
NameLabellerIngredients
ContraveTakeda Pharmaceuticals America, Inc.
EmbedaSTAT Rx USA LLC
Salts
Name/CASStructureProperties
Naltrexone Hydrochloride
Thumb
  • InChI Key: RHBRMCOKKKZVRY-ITLPAZOVSA-N
  • Monoisotopic Mass: 377.139385968
  • Average Mass: 377.862
DBSALT000670
Categories
UNII5S6W795CQM
CAS number16590-41-3
WeightAverage: 341.4009
Monoisotopic: 341.162708229
Chemical FormulaC20H23NO4
InChI KeyInChIKey=DQCKKXVULJGBQN-XFWGSAIBSA-N
InChI
InChI=1S/C20H23NO4/c22-13-4-3-12-9-15-20(24)6-5-14(23)18-19(20,16(12)17(13)25-18)7-8-21(15)10-11-1-2-11/h3-4,11,15,18,22,24H,1-2,5-10H2/t15-,18+,19+,20-/m1/s1
IUPAC Name
(1S,5R,13R,17S)-4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0¹,¹³.0⁵,¹⁷.0⁷,¹⁸]octadeca-7(18),8,10-trien-14-one
SMILES
[H][C@@]12OC3=C(O)C=CC4=C3[C@@]11CCN(CC3CC3)[C@]([H])(C4)[C@]1(O)CCC2=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as morphinans. These are polycyclic compounds with a four-ring skeleton with three condensed six-member rings forming a partially hydrogenated phenanthrene moiety, one of which is aromatic while the two others are alicyclic.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassMorphinans
Sub ClassNot Available
Direct ParentMorphinans
Alternative Parents
Substituents
  • Morphinan
  • Benzylisoquinoline
  • Phenanthrene
  • Isoquinolone
  • Tetralin
  • Benzofuran
  • Aralkylamine
  • Cyclohexanone
  • Alkyl aryl ether
  • Benzenoid
  • Piperidine
  • Tertiary alcohol
  • Cyclic alcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ketone
  • 1,2-aminoalcohol
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed as an adjunct to a medically supervised behaviour modification program in the maintenance of opiate cessation in individuals who were formerly physically dependent on opiates and who have successfully undergone detoxification. Also used for the management of alcohol dependence in conjunction with a behavioural modification program.
PharmacodynamicsNaltrexone, a pure opioid antagonist, is a synthetic congener of oxymorphone with no opioid agonist properties. Naltrexone is indicated in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids. It markedly attenuates or completely blocks, reversibly, the subjective effects of intravenously administered opioids. When co-administered with morphine, on a chronic basis, naltrexone blocks the physical dependence to morphine, heroin and other opioids. In subjects physically dependent on opioids, naltrexone will precipitate withdrawal symptomatology.
Mechanism of actionNaltrexone is a pure opiate antagonist and has little or no agonist activity. The mechanism of action of naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone is thought to act as a competitive antagonist at mc, κ, and δ receptors in the CNS, with the highest affintiy for the μ receptor. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. This leads to the antagonization of most of the subjective and objective effects of opiates, including respiratory depression, miosis, euphoria, and drug craving. The major metabolite of naltrexone, 6-β-naltrexol, is also an opiate antagonist and may contribute to the antagonistic activity of the drug.
Related Articles
AbsorptionAlthough well absorbed orally, naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5 to 40%.
Volume of distribution
  • 1350 L [intravenous administration]
Protein binding21% bound to plasma proteins over the therapeutic dose range.
Metabolism

Hepatic. When administered orally, naltrexone undergoes extensive biotransformation and is metabolized to 6 beta-naltrexol (which may contribute to the therapeutic effect) and other minor metabolites.

SubstrateEnzymesProduct
Naltrexone
Not Available
6-beta-naltrexolDetails
Route of eliminationBoth parent drug and metabolites are excreted primarily by the kidney (53% to 79% of the dose), however, urinary excretion of unchanged naltrexone accounts for less than 2% of an oral dose and fecal excretion is a minor elimination pathway. The renal clearance for naltrexone ranges from 30 to 127 mL/min and suggests that renal elimination is primarily by glomerular filtration.
Half life4 hours for naltrexone and 13 hours for the active metabolite 6 beta-naltrexol.
Clearance
  • ~ 3.5 L/min [after IV administration]
ToxicityIn the mouse, rat and guinea pig, the oral LD50s were 1,100-1,550 mg/kg; 1,450 mg/kg; and 1,490 mg/kg; respectively. High doses of naltrexone (generally ≥1,000 mg/kg) produce salivation, depression/reduced activity, tremors, and convulsions.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Naltrexone Action PathwayDrug actionSMP00687
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Mu-type opioid receptor
Gene symbol: OPRM1
UniProt: P35372
rs1799971 Not AvailableA > GThose with the AG genotype respond better to therapy (increase number of abstinent days)18250251
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9769
Blood Brain Barrier+0.9671
Caco-2 permeable+0.7471
P-glycoprotein substrateSubstrate0.8685
P-glycoprotein inhibitor INon-inhibitor0.8867
P-glycoprotein inhibitor IINon-inhibitor0.8718
Renal organic cation transporterNon-inhibitor0.5189
CYP450 2C9 substrateNon-substrate0.8336
CYP450 2D6 substrateSubstrate0.5925
CYP450 3A4 substrateSubstrate0.5981
CYP450 1A2 substrateInhibitor0.6656
CYP450 2C9 inhibitorNon-inhibitor0.9355
CYP450 2D6 inhibitorNon-inhibitor0.5686
CYP450 2C19 inhibitorNon-inhibitor0.9354
CYP450 3A4 inhibitorNon-inhibitor0.8993
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9483
Ames testNon AMES toxic0.6324
CarcinogenicityNon-carcinogens0.96
BiodegradationNot ready biodegradable0.9939
Rat acute toxicity2.7174 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.861
hERG inhibition (predictor II)Non-inhibitor0.8446
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Alkermes inc
  • Actavis totowa llc
  • Barr laboratories inc
  • Mallinckrodt inc
  • Sandoz inc
  • Duramed pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseoral
Capsule, extended releaseoral
Tablet, film coatedoral50 mg/1
Tabletoral50 mg
Kit
Prices
Unit descriptionCostUnit
Vivitrol injectable suspension960.0USD each
ReVia 30 50 mg tablet Bottle291.73USD bottle
Naltrexone hcl powder172.54USD g
Naltrexone powder69.0USD g
Revia 50 mg tablet9.35USD tablet
Naltrexone 50 mg tablet4.57USD tablet
Naltrexone HCl 50 mg tablet4.45USD tablet
Depade 50 mg tablet4.28USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5792477 No1997-05-022017-05-02Us
US5916598 No1997-05-022017-05-02Us
US6194006 No1998-12-302018-12-30Us
US6264987 No2000-05-192020-05-19Us
US6331317 No1999-11-122019-11-12Us
US6379703 No1998-12-302018-12-30Us
US6379704 No2000-05-192020-05-19Us
US6395304 No1999-11-122019-11-12Us
US6403114 No1997-05-022017-05-02Us
US6495164 No2000-05-252020-05-25Us
US6495166 No1999-11-122019-11-12Us
US6534092 No2000-05-192020-05-19Us
US6537586 No1999-11-122019-11-12Us
US6596316 No1998-12-302018-12-30Us
US6667061 No2000-05-252020-05-25Us
US6713090 No1999-11-122019-11-12Us
US6939033 No1999-11-122019-11-12Us
US7375111 No2005-03-262025-03-26Us
US7462626 No2004-07-202024-07-20Us
US7682633 No2007-06-192027-06-19Us
US7682634 No2007-06-192027-06-19Us
US7799345 No2000-05-252020-05-25Us
US7815934 No2007-12-122027-12-12Us
US7919499 No2009-10-152029-10-15Us
US8088786 No2009-02-032029-02-03Us
US8158156 No2007-06-192027-06-19Us
US8318788 No2007-11-082027-11-08Us
US8623418 No2009-11-072029-11-07Us
US8685443 No2005-07-032025-07-03Us
US8685444 No2005-07-032025-07-03Us
US8722085 No2007-11-082027-11-08Us
US8815889 No2004-07-202024-07-20Us
US8846104 No2007-06-192027-06-19Us
US8877247 No2007-06-192027-06-19Us
US8916195 No2010-02-022030-02-02Us
US9107837 No2007-06-042027-06-04Us
US9125868 No2007-11-082027-11-08Us
US9248123 No2012-01-132032-01-13Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point168-170 °CPhysProp
water solubility100 mg/mL (as hydrochloride salt)Not Available
logP1.92HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility3.07 mg/mLALOGPS
logP2.07ALOGPS
logP1.36ChemAxon
logS-2ALOGPS
pKa (Strongest Acidic)7.39ChemAxon
pKa (Strongest Basic)11.54ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area70 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity91.5 m3·mol-1ChemAxon
Polarizability35.97 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Bao-Shan Huang, Yansong Lu, Ben-Yi Ji, Aris P Christodoulou, “Preparation of naltrexone from codeine and 3-benzylmorphine.” U.S. Patent US6013796, issued March, 1990.

US6013796
General References
  1. Schmitz JM, Stotts AL, Rhoades HM, Grabowski J: Naltrexone and relapse prevention treatment for cocaine-dependent patients. Addict Behav. 2001 Mar-Apr;26(2):167-80. [PubMed:11316375 ]
  2. Krystal JH, Gueorguieva R, Cramer J, Collins J, Rosenheck R: Naltrexone is associated with reduced drinking by alcohol dependent patients receiving antidepressants for mood and anxiety symptoms: results from VA Cooperative Study No. 425, "Naltrexone in the treatment of alcoholism". Alcohol Clin Exp Res. 2008 Jan;32(1):85-91. Epub 2007 Dec 7. [PubMed:18070245 ]
  3. Ray LA, Chin PF, Miotto K: Naltrexone for the treatment of alcoholism: clinical findings, mechanisms of action, and pharmacogenetics. CNS Neurol Disord Drug Targets. 2010 Mar;9(1):13-22. [PubMed:20201811 ]
External Links
ATC CodesA08AA62N07BB04
AHFS Codes
  • 28:10.00
PDB EntriesNot Available
FDA labelDownload (1.83 MB)
MSDSDownload (73.9 KB)
Interactions
Drug Interactions
Drug
AlfentanilThe therapeutic efficacy of Alfentanil can be decreased when used in combination with Naltrexone.
BuprenorphineThe therapeutic efficacy of Buprenorphine can be decreased when used in combination with Naltrexone.
ButorphanolThe therapeutic efficacy of Butorphanol can be decreased when used in combination with Naltrexone.
FentanylThe therapeutic efficacy of Fentanyl can be decreased when used in combination with Naltrexone.
HydrocodoneThe therapeutic efficacy of Hydrocodone can be decreased when used in combination with Naltrexone.
HydromorphoneThe therapeutic efficacy of Hydromorphone can be decreased when used in combination with Naltrexone.
LevorphanolThe therapeutic efficacy of Levorphanol can be decreased when used in combination with Naltrexone.
MethadoneThe therapeutic efficacy of Methadone can be decreased when used in combination with Naltrexone.
MethylnaltrexoneThe risk or severity of adverse effects can be increased when Methylnaltrexone is combined with Naltrexone.
MorphineThe therapeutic efficacy of Morphine can be decreased when used in combination with Naltrexone.
NalbuphineThe therapeutic efficacy of Nalbuphine can be decreased when used in combination with Naltrexone.
NaloxegolThe risk or severity of adverse effects can be increased when Naltrexone is combined with Naloxegol.
OxycodoneThe therapeutic efficacy of Oxycodone can be decreased when used in combination with Naltrexone.
OxymorphoneThe therapeutic efficacy of Oxymorphone can be decreased when used in combination with Naltrexone.
PentazocineThe therapeutic efficacy of Pentazocine can be decreased when used in combination with Naltrexone.
PethidineThe therapeutic efficacy of Pethidine can be decreased when used in combination with Naltrexone.
RemifentanilThe therapeutic efficacy of Remifentanil can be decreased when used in combination with Naltrexone.
SufentanilThe therapeutic efficacy of Sufentanil can be decreased when used in combination with Naltrexone.
TapentadolThe therapeutic efficacy of Tapentadol can be decreased when used in combination with Naltrexone.
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Naltrexone.
Food Interactions
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Voltage-gated calcium channel activity
Specific Function:
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44778.855 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Kato H: [Pharmacological effects of a mu-opioid receptor antagonist naltrexone on alcohol dependence]. Nihon Arukoru Yakubutsu Igakkai Zasshi. 2008 Oct;43(5):697-704. [PubMed:19068776 ]
  3. Helm S, Trescot AM, Colson J, Sehgal N, Silverman S: Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification. Pain Physician. 2008 Mar-Apr;11(2):225-35. [PubMed:18354714 ]
  4. Goodman AJ, Le Bourdonnec B, Dolle RE: Mu opioid receptor antagonists: recent developments. ChemMedChem. 2007 Nov;2(11):1552-70. [PubMed:17918759 ]
  5. Barrios de Tomasi E, Juarez-Gonzalez J: [Opioid antagonists and alcohol consumption]. Rev Neurol. 2007 Aug 1-15;45(3):155-62. [PubMed:17661275 ]
  6. Weerts EM, Kim YK, Wand GS, Dannals RF, Lee JS, Frost JJ, McCaul ME: Differences in delta- and mu-opioid receptor blockade measured by positron emission tomography in naltrexone-treated recently abstinent alcohol-dependent subjects. Neuropsychopharmacology. 2008 Feb;33(3):653-65. Epub 2007 May 9. [PubMed:17487229 ]
  7. Herz A: Opioid reward mechanisms: a key role in drug abuse? Can J Physiol Pharmacol. 1998 Mar;76(3):252-8. [PubMed:9673788 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates th...
Gene Name:
OPRK1
Uniprot ID:
P41145
Molecular Weight:
42644.665 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Helm S, Trescot AM, Colson J, Sehgal N, Silverman S: Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification. Pain Physician. 2008 Mar-Apr;11(2):225-35. [PubMed:18354714 ]
  3. Herz A: Endogenous opioid systems and alcohol addiction. Psychopharmacology (Berl). 1997 Jan;129(2):99-111. [PubMed:9040115 ]
  4. Barrios de Tomasi E, Juarez-Gonzalez J: [Opioid antagonists and alcohol consumption]. Rev Neurol. 2007 Aug 1-15;45(3):155-62. [PubMed:17661275 ]
  5. Wee S, Orio L, Ghirmai S, Cashman JR, Koob GF: Inhibition of kappa opioid receptors attenuated increased cocaine intake in rats with extended access to cocaine. Psychopharmacology (Berl). 2009 Sep;205(4):565-75. doi: 10.1007/s00213-009-1563-y. Epub 2009 May 30. [PubMed:19484223 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurot...
Gene Name:
OPRD1
Uniprot ID:
P41143
Molecular Weight:
40368.235 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Roy S, Guo X, Kelschenbach J, Liu Y, Loh HH: In vivo activation of a mutant mu-opioid receptor by naltrexone produces a potent analgesic effect but no tolerance: role of mu-receptor activation and delta-receptor blockade in morphine tolerance. J Neurosci. 2005 Mar 23;25(12):3229-33. [PubMed:15788780 ]
  3. Barrios de Tomasi E, Juarez-Gonzalez J: [Opioid antagonists and alcohol consumption]. Rev Neurol. 2007 Aug 1-15;45(3):155-62. [PubMed:17661275 ]
  4. Weerts EM, Kim YK, Wand GS, Dannals RF, Lee JS, Frost JJ, McCaul ME: Differences in delta- and mu-opioid receptor blockade measured by positron emission tomography in naltrexone-treated recently abstinent alcohol-dependent subjects. Neuropsychopharmacology. 2008 Feb;33(3):653-65. Epub 2007 May 9. [PubMed:17487229 ]
  5. Herz A: Opioid reward mechanisms: a key role in drug abuse? Can J Physiol Pharmacol. 1998 Mar;76(3):252-8. [PubMed:9673788 ]
  6. Herz A: Endogenous opioid systems and alcohol addiction. Psychopharmacology (Berl). 1997 Jan;129(2):99-111. [PubMed:9040115 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Not Available
Specific Function:
Not Available
Gene Name:
SIGMAR1
Uniprot ID:
Q5T1J1
Molecular Weight:
14852.655 Da
References
  1. Helm S, Trescot AM, Colson J, Sehgal N, Silverman S: Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification. Pain Physician. 2008 Mar-Apr;11(2):225-35. [PubMed:18354714 ]
  2. Wee S, Orio L, Ghirmai S, Cashman JR, Koob GF: Inhibition of kappa opioid receptors attenuated increased cocaine intake in rats with extended access to cocaine. Psychopharmacology (Berl). 2009 Sep;205(4):565-75. doi: 10.1007/s00213-009-1563-y. Epub 2009 May 30. [PubMed:19484223 ]
  3. Herz A: Endogenous opioid systems and alcohol addiction. Psychopharmacology (Berl). 1997 Jan;129(2):99-111. [PubMed:9040115 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da
References
  1. Antonilli L, Brusadin V, Milella MS, Sobrero F, Badiani A, Nencini P: In vivo chronic exposure to heroin or naltrexone selectively inhibits liver microsome formation of estradiol-3-glucuronide in the rat. Biochem Pharmacol. 2008 Sep 1;76(5):672-9. doi: 10.1016/j.bcp.2008.06.011. Epub 2008 Jul 1. [PubMed:18639530 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on May 04, 2016 02:37