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Identification
NameNaloxone
Accession NumberDB01183  (APRD00025)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.

Structure
Thumb
Synonyms
1-N-Allyl-14-hydroxynordihydromorphinone
17-Allyl-3,14-dihydroxy-4,5alpha-epoxymorphinan-6-one
EN 1530 Base
L-Naloxone
N-Allylnoroxymorphone
Nalossone
Naloxona
Naloxone
Naloxonum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Evzioinjection, solution.4 mg/1intramuscular; subcutaneouskaleo, Inc.2014-04-03Not applicableUs
Naloxone HCl Injection - 0.4mg/ml USPliquid0.4 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated1995-12-31Not applicableCanada
Naloxone HCl Injection - 1mg/ml USPliquid1 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated1995-12-31Not applicableCanada
Naloxone Hydrochloride Injectionsolution1 mgintramuscular; intravenous; subcutaneousOmega Laboratories Ltd2013-10-10Not applicableCanada
Naloxone Hydrochloride Injectionsolution0.4 mgintramuscular; intravenous; subcutaneousOmega Laboratories Ltd2013-10-03Not applicableCanada
Naloxone Hydrochloride Injection Sdz Preservative Freesolution0.4 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated2013-07-10Not applicableCanada
Naloxone Hydrochloride Injection USPsolution0.4 mgintramuscular; intravenous; subcutaneousAlveda Pharmaceuticals Inc2014-01-09Not applicableCanada
Narcanspray4 mg/.1mLnasalAdapt Pharma, Inc.2015-11-18Not applicableUs
Narcan Injection 0.02mg/mlliquid0.02 mgintramuscular; intravenous; subcutaneousBristol Myers Squibb Canada1993-12-312004-08-05Canada
Narcan Injection 0.4mg/mlsolution0.4 mgintramuscular; intravenous; subcutaneousBristol Myers Squibb Canada1992-12-312004-08-05Canada
Narcan Injection 1mg/mlliquid1 mgintramuscular; intravenous; subcutaneousBristol Myers Squibb Canada1992-12-312004-08-04Canada
S.O.S. Naloxone Hydrochloride Injectionsolution1 mgintramuscular; intravenous; subcutaneousSandoz Canada IncorporatedNot applicableNot applicableCanada
S.O.S. Naloxone Hydrochloride Injectionsolution0.4 mgintramuscular; intravenous; subcutaneousSandoz Canada IncorporatedNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Naloxone Hydrochlorideinjection1 mg/mLparenteralCardinal Health2001-06-01Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLparenteralGeneral Injectables & Vaccines, Inc2012-08-29Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1987-01-07Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousSina Health Inc1987-01-07Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousCardinal Health2011-07-08Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLparenteralInternational Medication Systems, Limited2001-06-01Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLparenteralPhysicians Total Care, Inc.2011-05-05Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLparenteralREMEDYREPACK INC.2013-06-122016-04-05Us
Naloxone Hydrochlorideinjection1 mg/mLparenteralInternational Medication Systems, Limited1988-04-01Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousPhysicians Total Care, Inc.2000-06-15Not applicableUs
Naloxone Hydrochlorideinjection.4 mg/mLintramuscular; intravenous; subcutaneousWest Ward Pharmaceuticals Corp.1986-09-24Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousTYA Pharmaceuticals1986-09-24Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLparenteralGeneral Injectables & Vaccines, Inc2013-12-06Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLparenteralAmphastar Pharmaceuticals, Inc.2001-06-01Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2010-05-03Not applicableUs
Naloxone Hydrochlorideinjection.4 mg/mLintramuscular; intravenous; subcutaneousGeneral Injectables & Vaccines, Inc2010-03-01Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLparenteralAmphastar Pharmaceuticals, Inc.1988-04-01Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLparenteralREMEDYREPACK INC.2015-03-07Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLparenteralGeneral Injectables & Vaccines, Inc.2010-12-27Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1986-09-24Not applicableUs
Naloxone Hydrochlorideinjection1 mg/mLintramuscular; intravenous; subcutaneousGeneral Injectables & Vaccines, Inc.2014-05-07Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1987-01-07Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousMylan Institutional LLC2014-12-17Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousCardinal Health2012-03-06Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousGeneral Injectables & Vaccines, Inc2010-08-01Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1987-01-07Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousMylan Institutional LLC2014-03-06Not applicableUs
Naloxone Hydrochlorideinjection, solution.4 mg/mLintramuscular; intravenous; subcutaneousCardinal Health2011-07-08Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
NaloneNot Available
NarcanNot Available
NarcantiNot Available
NarconNot Available
Brand mixtures
NameLabellerIngredients
Act Buprenorphine/naloxoneActavis Pharma Company
BunavailBio Delivery Sciences International, Inc.
Buprenorphine and NaloxoneTeva Pharmaceuticals USA Inc
Buprenorphine HCl and Naloxone HClMallinckrodt, Inc.
Buprenorphine Hydrochloride and Naloxone Hydrochloride DihydrateRoxane Laboratories, Inc.
Mylan-buprenorphine/naloxoneMylan Pharmaceuticals Ulc
Pentazocine and NaloxoneActavis Pharma, Inc.
Pentazocine HCl and Naloxone HClSTAT Rx USA LLC
Pentazocine Hydrochloride and Naloxone HydrochlorideGAVIS Pharmaceuticals, LLC
SuboxoneIndivior Inc.
TarginPurdue Pharma
Teva-buprenorphine/naloxoneTeva Canada Limited
ZubsolvOrexo Us, Inc.
Salts
Name/CASStructureProperties
Naloxone Hydrochloride
Thumb
  • InChI Key: RGPDIGOSVORSAK-STHHAXOLSA-N
  • Monoisotopic Mass: 363.123735904
  • Average Mass: 363.835
DBSALT000126
Naloxone hydrochloride dihydrate
ThumbNot applicableDBSALT001497
Categories
UNII36B82AMQ7N
CAS number465-65-6
WeightAverage: 327.3743
Monoisotopic: 327.147058165
Chemical FormulaC19H21NO4
InChI KeyInChIKey=UZHSEJADLWPNLE-GRGSLBFTSA-N
InChI
InChI=1S/C19H21NO4/c1-2-8-20-9-7-18-15-11-3-4-12(21)16(15)24-17(18)13(22)5-6-19(18,23)14(20)10-11/h2-4,14,17,21,23H,1,5-10H2/t14-,17+,18+,19-/m1/s1
IUPAC Name
(1S,5R,13R,17S)-10,17-dihydroxy-4-(prop-2-en-1-yl)-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(CC=C)[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
IndicationFor the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids including natural and synthetic narcotics, propoxyphene, methadone and the narcotic-antagonist analgesics: nalbuphine, pentazocine and butorphanol. It is also indicated for the diagnosis of suspected acute opioid overdose. It may also be used as an adjunctive agent to increase blood pressure in the management of septic shock.
PharmacodynamicsNaloxone is an opiate antagonist and prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine. Naloxone is an essentially pure narcotic antagonist, i.e., it does not possess the "agonistic" or morphine-like properties characteristic of other narcotic antagonists; naloxone does not produce respiratory depression, psychotomimetic effects or pupillary constriction. In the absence of narcotics or agonistic effects of other narcotic antagonists, it exhibits essentially no pharmacologic activity. When given intravenously, the onset of action is apparent within 2 minutes. The onset of action is slower if given subcutaneously or intramuscularly. The duration of action also differs between sites of injection and dose.
Mechanism of actionWhile the mechanism of action of naloxone is not fully understood, the preponderance of evidence suggests that naloxone antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor. Recently, naloxone has been shown to bind all three opioid receptors (mu, kappa and gamma) but the strongest binding is to the mu receptor.
Related Articles
AbsorptionWell absorbed following intramuscular injection.
Volume of distribution

Following parenteral administration naloxone hydrochloride is rapidly distributed in the body. Naloxone is also very lipophillic and easily crosses the blood-brain-barrier. It can also cross the placenta.

Protein bindingPlasma protein binding occurs but is relatively weak. Plasma albumin is the major binding constituent but significant binding of naloxone also occurs to plasma constituents other than albumin.
Metabolism

Naloxone is hepatically metabolized and primarily undergoes glucuronidation to form naloxone-3-glucuronide.

Route of eliminationUrine (25%- 40% is excreted as metabolites within 6 hours)
Half lifeAdults = 30-81 minutes; Neonates = 3.1 ± 0.5 hours.
ClearanceNot Available
ToxicityLD50, IV administration, mouse = 150 ± 5 mg/kg; LD50, IV administration, rat = 109 ± 4 mg/kg;
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Naloxone Action PathwayDrug actionSMP00688
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9729
Blood Brain Barrier+0.9787
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.8788
P-glycoprotein inhibitor INon-inhibitor0.7922
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterInhibitor0.5
CYP450 2C9 substrateNon-substrate0.8522
CYP450 2D6 substrateSubstrate0.5296
CYP450 3A4 substrateSubstrate0.6107
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9303
CYP450 2D6 inhibitorNon-inhibitor0.7886
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9153
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9523
Ames testNon AMES toxic0.7182
CarcinogenicityNon-carcinogens0.9583
BiodegradationNot ready biodegradable0.9968
Rat acute toxicity2.7231 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7798
hERG inhibition (predictor II)Non-inhibitor0.8641
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Filmbuccal
Tabletsublingual
Injection, solutionintramuscular; subcutaneous.4 mg/1
Liquidintramuscular; intravenous; subcutaneous0.4 mg
Liquidintramuscular; intravenous; subcutaneous1 mg
Injectionintramuscular; intravenous; subcutaneous.4 mg/mL
Injectionintramuscular; intravenous; subcutaneous1 mg/mL
Injectionparenteral1 mg/mL
Injection, solutionintramuscular; intravenous; subcutaneous.4 mg/mL
Solutionintramuscular; intravenous; subcutaneous1 mg
Solutionintramuscular; intravenous; subcutaneous0.4 mg
Spraynasal4 mg/.1mL
Liquidintramuscular; intravenous; subcutaneous0.02 mg
Tabletoral
Film, solublebuccal; sublingual
Film, solublesublingual
Tablet (extended-release)oral
Tablet, orally disintegratingsublingual
Prices
Unit descriptionCostUnit
Naloxone hcl powder70.9USD g
Naloxone 0.4 mg/ml vial7.07USD ml
Naloxone 0.4 mg/ml ampul4.78USD ml
Narcan 0.4 mg/ml ampul4.58USD ml
Naloxone 0.02 mg/ml vial0.84USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6159498 No1996-10-182016-10-18Us
US6277384 No1998-12-222018-12-22Us
US6696066 No1998-12-222018-12-22Us
US7579019 No2000-01-222020-01-22Us
US7674799 No2005-03-302025-03-30Us
US7674800 No2005-03-302025-03-30Us
US7683072 No2005-03-302025-03-30Us
US7731686 No2006-06-102026-06-10Us
US7731690 No2005-01-152025-01-15Us
US7749194 No2008-10-302028-10-30Us
US7918823 No2004-11-232024-11-23Us
US7947017 No2008-03-122028-03-12Us
US8016788 No2005-03-212025-03-21Us
US8017150 No2003-02-132023-02-13Us
US8021344 No2009-11-022029-11-02Us
US8147866 No2007-07-232027-07-23Us
US8206360 No2007-02-272027-02-27Us
US8226610 No2009-04-102029-04-10Us
US8231573 No2008-11-252028-11-25Us
US8313466 No2004-11-232024-11-23Us
US8361029 No2004-11-232024-11-23Us
US8425462 No2004-11-232024-11-23Us
US8454996 No1999-09-242019-09-24Us
US8470361 No2010-05-222030-05-22Us
US8475832 No2010-03-262030-03-26Us
US8603514 No2004-04-032024-04-03Us
US8608698 No2004-11-232024-11-23Us
US8627816 No2012-02-042032-02-04Us
US8658198 No2007-12-032027-12-03Us
US8673355 No1998-12-222018-12-22Us
US8703177 No2012-08-202032-08-20Us
US8822487 No1998-12-222018-12-22Us
US8846090 No2003-04-042023-04-04Us
US8846091 No2003-04-042023-04-04Us
US8926594 No2006-03-312026-03-31Us
US8939943 No2011-02-282031-02-28Us
US8940330 No2012-09-182032-09-18Us
US8969369 No2002-05-102022-05-10Us
US9022022 No2011-02-282031-02-28Us
US9056051 No2002-05-102022-05-10Us
US9056170 No2004-11-232024-11-23Us
US9073933 No2005-03-302025-03-30Us
US9084729 No2002-05-102022-05-10Us
US9161937 No2002-05-102022-05-10Us
US9168252 No2002-05-102022-05-10Us
US9205082 No2002-05-102022-05-10Us
US9211253 No2015-03-162035-03-16Us
US9238108 No2007-01-222027-01-22Us
US9259421 No2012-09-182032-09-18Us
US9278182 No2006-02-012026-02-01Us
US9283216 No2002-05-102022-05-10Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point200-205 °CNot Available
water solubilitySolubleNot Available
logP2.09HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility5.64 mg/mLALOGPS
logP1.47ALOGPS
logP1.62ChemAxon
logS-1.8ALOGPS
pKa (Strongest Acidic)7.27ChemAxon
pKa (Strongest Basic)10.63ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area70 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity88.72 m3·mol-1ChemAxon
Polarizability33.8 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Bianca Brogmann, Silke Muhlau, Christof Spitzley, “Pharmaceutical preparation containing oxycodone and naloxone.” U.S. Patent US20050245556, issued November 03, 2005.

US20050245556
General References
  1. Link [Link]
External Links
ATC CodesV03AB15
AHFS Codes
  • 28:10.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (74 KB)
Interactions
Drug Interactions
Drug
MethylnaltrexoneThe risk or severity of adverse effects can be increased when Methylnaltrexone is combined with Naloxone.
NaloxegolThe risk or severity of adverse effects can be increased when Naloxone is combined with Naloxegol.
Food InteractionsNot Available

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. Narita M, Suzuki M, Mizoguchi H, Narita M, Yajima Y, Sakurada S, Tseng LF, Suzuki T: Up-regulation of mu-opioid receptor-mediated G-protein activation in protein kinase Cgamma knockout mice following repeated naloxone treatment. Neurosci Lett. 2003 Feb 27;338(2):103-6. [PubMed:12566163 ]
  2. Freye E, Latasch L, Von Bredow G, Neruda B: [The opioid tramadol demonstrates excitatory properties of non-opioid character--a preclinical study using alfentanil as a comparison]. Schmerz. 1998 Feb 28;12(1):19-24. [PubMed:12799988 ]
  3. Neal CR Jr, Owens CE, Taylor LP, Hoversten MT, Akil H, Watson SJ Jr: Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors. J Chem Neuroanat. 2003 Jul;25(4):233-47. [PubMed:12842269 ]
  4. Spetea M, Toth F, Schutz J, Otvos F, Toth G, Benyhe S, Borsodi A, Schmidhammer H: Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist. Eur J Neurosci. 2003 Jul;18(2):290-5. [PubMed:12887410 ]
  5. Marek GJ: Behavioral evidence for mu-opioid and 5-HT2A receptor interactions. Eur J Pharmacol. 2003 Aug 1;474(1):77-83. [PubMed:12909198 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. 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 ]
  8. Goodman AJ, Le Bourdonnec B, Dolle RE: Mu opioid receptor antagonists: recent developments. ChemMedChem. 2007 Nov;2(11):1552-70. [PubMed:17918759 ]
  9. van Dorp E, Yassen A, Dahan A: Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32. [PubMed:17367258 ]
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. Moncada A, Cendan CM, Baeyens JM, Del Pozo E: Effects of serine/threonine protein phosphatase inhibitors on morphine-induced antinociception in the tail flick test in mice. Eur J Pharmacol. 2003 Mar 28;465(1-2):53-60. [PubMed:12650833 ]
  2. Kakinohana M, Marsala M, Carter C, Davison JK, Yaksh TL: Neuraxial morphine may trigger transient motor dysfunction after a noninjurious interval of spinal cord ischemia: a clinical and experimental study. Anesthesiology. 2003 Apr;98(4):862-70. [PubMed:12657847 ]
  3. Breljak D, Boranic M, Horvat S: Oligopeptide fragments of the enkephalin molecule interfere with hematopoietic cell colony formation. Int J Immunopathol Pharmacol. 2000 Jan-Apr;13(1):13-19. [PubMed:12749773 ]
  4. Chudapongse N, Kim SY, Kramer RE, Ho IK: Nonspecific effects of the selective kappa-opioid receptor agonist U-50,488H on dopamine uptake and release in PC12 cells. J Pharmacol Sci. 2003 Nov;93(3):372-5. [PubMed:14646257 ]
  5. Osman AM, Gomma M, Saad AH: A possible role for an enkephalinergic system in the internal defense mechanism of Biomphalaria alexandrina exposed to Schistosoma mansoni. J Egypt Soc Parasitol. 2003 Dec;33(3):841-61. [PubMed:14708857 ]
  6. 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 ]
  7. van Dorp E, Yassen A, Dahan A: Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32. [PubMed:17367258 ]
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. Peng X, Neumeyer JL: Kappa receptor bivalent ligands. Curr Top Med Chem. 2007;7(4):363-73. [PubMed:17305578 ]
  2. van Dorp E, Yassen A, Dahan A: Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32. [PubMed:17367258 ]
  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 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
other/unknown
General Function:
Transcriptional activator activity, rna polymerase ii transcription factor binding
Specific Function:
Phosphorylation-dependent transcription factor that stimulates transcription upon binding to the DNA cAMP response element (CRE), a sequence present in many viral and cellular promoters. Transcription activation is enhanced by the TORC coactivators which act independently of Ser-133 phosphorylation. Involved in different cellular processes including the synchronization of circadian rhythmicity ...
Gene Name:
CREB1
Uniprot ID:
P16220
Molecular Weight:
36687.86 Da
References
  1. Li J, Li YH, Yuan XR: Changes of phosphorylation of cAMP response element binding protein in rat nucleus accumbens after chronic ethanol intake: naloxone reversal. Acta Pharmacol Sin. 2003 Sep;24(9):930-6. [PubMed:12956944 ]
  2. Chartoff EH, Papadopoulou M, Konradi C, Carlezon WA Jr: Dopamine-dependent increases in phosphorylation of cAMP response element binding protein (CREB) during precipitated morphine withdrawal in primary cultures of rat striatum. J Neurochem. 2003 Oct;87(1):107-18. [PubMed:12969258 ]
  3. Gao C, Chen LW, Tao YM, Chen J, Xu XJ, Chi ZQ: Effects of ohmefentanyl stereoisomers on phosphorylation of cAMP- response element binding protein in cultured rat hippocampal neurons. Acta Pharmacol Sin. 2003 Dec;24(12):1253-8. [PubMed:14653953 ]
  4. Walters CL, Cleck JN, Kuo YC, Blendy JA: Mu-opioid receptor and CREB activation are required for nicotine reward. Neuron. 2005 Jun 16;46(6):933-43. [PubMed:15953421 ]
  5. Hawes JJ, Narasimhaiah R, Picciotto MR: Galanin attenuates cyclic AMP regulatory element-binding protein (CREB) phosphorylation induced by chronic morphine and naloxone challenge in Cath.a cells and primary striatal cultures. J Neurochem. 2006 Feb;96(4):1160-8. Epub 2006 Jan 17. [PubMed:16417577 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonistother/unknown
General Function:
Zinc ion binding
Specific Function:
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription fact...
Gene Name:
ESR1
Uniprot ID:
P03372
Molecular Weight:
66215.45 Da
References
  1. Farooqui M, Geng ZH, Stephenson EJ, Zaveri N, Yee D, Gupta K: Naloxone acts as an antagonist of estrogen receptor activity in MCF-7 cells. Mol Cancer Ther. 2006 Mar;5(3):611-20. [PubMed:16546975 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transmembrane signaling receptor activity
Specific Function:
Cooperates with LY96 and CD14 to mediate the innate immune response to bacterial lipopolysaccharide (LPS). Acts via MYD88, TIRAP and TRAF6, leading to NF-kappa-B activation, cytokine secretion and the inflammatory response (PubMed:9237759, PubMed:10835634). Also involved in LPS-independent inflammatory responses triggered by free fatty acids, such as palmitate, and Ni(2+). Responses triggered b...
Gene Name:
TLR4
Uniprot ID:
O00206
Molecular Weight:
95679.19 Da
References
  1. Lewis SS, Loram LC, Hutchinson MR, Li CM, Zhang Y, Maier SF, Huang Y, Rice KC, Watkins LR: (+)-naloxone, an opioid-inactive toll-like receptor 4 signaling inhibitor, reverses multiple models of chronic neuropathic pain in rats. J Pain. 2012 May;13(5):498-506. doi: 10.1016/j.jpain.2012.02.005. Epub 2012 Apr 20. [PubMed:22520687 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. Gao B, Hagenbuch B, Kullak-Ublick GA, Benke D, Aguzzi A, Meier PJ: Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. J Pharmacol Exp Ther. 2000 Jul;294(1):73-9. [PubMed:10871297 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 ]
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Drug created on June 13, 2005 07:24 / Updated on June 29, 2016 02:25