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Identification
NameSufentanil
Accession NumberDB00708  (APRD00671)
TypeSmall Molecule
GroupsApproved, Investigational
Description

An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent. [PubChem]

Structure
Thumb
Synonyms
N-(4-(Methoxymethyl)-1-(2-(2-thienyl)ethyl)-4-piperidinyl)-N-phenylpropanamide
N-(4-(Methoxymethyl)-1-(2-(2-thienyl)ethyl)-4-piperidyl)propionanilide
Sufentanil
Sufentanilo
Sufentanilum
Sufentanyl
External Identifiers
  • R 30730
  • R 33800
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Sufenta Inj 50mcg/mlliquid50 mcgintravenousJanssen Pharmaceutica, Division Of Janssen Ortho Inc.1985-12-311996-09-10Canada
Sufenta Inj 50mcg/mlliquid50 mcgintravenous; epiduralJanssen Inc1985-12-312007-11-26Canada
Sufentanil Citrateinjection50 ug/mLepidural; intravenousAkorn, Inc.2010-12-01Not applicableUs
Sufentanil Citrate Injection USPsolution50 mcgintravenous; epiduralSandoz Canada Incorporated2001-08-01Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Sufentanil Citrateinjection, solution50 ug/mLepidural; intravenousHospira, Inc.1996-12-11Not applicableUs
Sufentanil Citrateinjection.05 mg/mLepidural; intravenousWest Ward Pharmaceutical Corp.1995-12-15Not applicableUs
Sufentanil Citrateinjection.05 mg/mLepidural; intravenousWest Ward Pharmaceutical Corp.1995-12-15Not applicableUs
Sufentanil Citrateinjection.05 mg/mLepidural; intravenousWest Ward Pharmaceutical Corp.1995-12-15Not applicableUs
Sufentanil Citrateinjection, solution50 ug/mLepidural; intravenousHospira, Inc.1996-12-11Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ChronogesicDURECT
DisufenAngenerico
FastfenCristália
SufentaJanssen
Sufenta ForteJanssen
Sufenta miteJanssen
SufentilClaris Lifesciences Ltd.
ZuftilPisa
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Sufentanil Citrate
Thumb
  • InChI Key: OJCZPLDERGDQRJ-UHFFFAOYSA-N
  • Monoisotopic Mass: 578.229801514
  • Average Mass: 578.674
DBSALT000275
Categories
UNIIAFE2YW0IIZ
CAS number56030-54-7
WeightAverage: 386.551
Monoisotopic: 386.202798904
Chemical FormulaC22H30N2O2S
InChI KeyInChIKey=GGCSSNBKKAUURC-UHFFFAOYSA-N
InChI
InChI=1S/C22H30N2O2S/c1-3-21(25)24(19-8-5-4-6-9-19)22(18-26-2)12-15-23(16-13-22)14-11-20-10-7-17-27-20/h4-10,17H,3,11-16,18H2,1-2H3
IUPAC Name
N-[4-(methoxymethyl)-1-[2-(thiophen-2-yl)ethyl]piperidin-4-yl]-N-phenylpropanamide
SMILES
CCC(=O)N(C1=CC=CC=C1)C1(COC)CCN(CCC2=CC=CS2)CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as anilides. These are organic heterocyclic compounds derived from oxoacids RkE(=O)l(OH)m (l not 0) by replacing an OH group by the NHPh group or derivative formed by ring substitution.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassAnilides
Direct ParentAnilides
Alternative Parents
Substituents
  • Anilide
  • Aralkylamine
  • 4-aminopiperidine
  • Piperidine
  • Heteroaromatic compound
  • Thiophene
  • Tertiary carboxylic acid amide
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationUsed as an analgesic adjunct in anesthesia and as a primary anesthetic drug in procedures requiring assisted ventilation and in the relief of pain.
PharmacodynamicsSufentanil is a synthetic opioid analgesic. Sufentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, sufentanil exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Sufentanil may increase the patient's tolerance for pain and decrease the perception of suffering, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Sufentanil depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
Mechanism of actionOpiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Sufentanil's analgesic activity is, most likely, due to its conversion to morphine. Opioids open calcium-dependent inwardly rectifying potassium channels (OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life265 minutes
ClearanceNot Available
ToxicityLD50: 18.7 mg/kg (IV in mice)
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Sufentanil Action PathwayDrug actionSMP00417
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9875
Blood Brain Barrier+0.9886
Caco-2 permeable+0.5201
P-glycoprotein substrateSubstrate0.6673
P-glycoprotein inhibitor IInhibitor0.8275
P-glycoprotein inhibitor IIInhibitor0.8387
Renal organic cation transporterNon-inhibitor0.5594
CYP450 2C9 substrateNon-substrate0.7923
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.713
CYP450 1A2 substrateNon-inhibitor0.8954
CYP450 2C9 inhibitorNon-inhibitor0.7839
CYP450 2D6 inhibitorNon-inhibitor0.8416
CYP450 2C19 inhibitorNon-inhibitor0.5438
CYP450 3A4 inhibitorInhibitor0.6293
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6401
Ames testNon AMES toxic0.7695
CarcinogenicityNon-carcinogens0.8861
BiodegradationNot ready biodegradable0.9724
Rat acute toxicity3.0968 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9793
hERG inhibition (predictor II)Inhibitor0.772
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Akorn inc
  • Baxter healthcare corp anesthesia and critical care
  • Hospira inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Liquidintravenous50 mcg
Liquidintravenous; epidural50 mcg
Injectionepidural; intravenous.05 mg/mL
Injectionepidural; intravenous50 ug/mL
Injection, solutionepidural; intravenous50 ug/mL
Solutionintravenous; epidural50 mcg
Prices
Unit descriptionCostUnit
Sufentanil citrate powder18927.0USD g
Sufenta 50 mcg/ml ampul5.38USD ml
Sufentanil 50 mcg/ml ampul3.92USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point97 °CPhysProp
water solubility76 mg/L (at 25 °C)ROY,SD & FLYNN,GL (1988)
logP3.95SANGSTER (1993)
logS-3.71ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.012 mg/mLALOGPS
logP3.4ALOGPS
logP3.61ChemAxon
logS-4.5ALOGPS
pKa (Strongest Basic)8.86ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.78 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity111.42 m3·mol-1ChemAxon
Polarizability43.85 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Jacob Mathew, J. Killgore, “New methods for the synthesis of alfentanil, sufentanil, and remifentanil.” U.S. Patent US20060149071, issued July 06, 2006.

US20060149071
General ReferencesNot Available
External Links
ATC CodesN01AH03
AHFS Codes
  • 28:08.08
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (47.6 KB)
Interactions
Drug Interactions
Drug
AcebutololSufentanil may increase the bradycardic activities of Acebutolol.
AcepromazineAcepromazine may increase the hypotensive activities of Sufentanil.
AcetazolamideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Acetazolamide.
AlvimopanThe risk or severity of adverse effects can be increased when Sufentanil is combined with Alvimopan.
AmilorideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Amiloride.
Ammonium chlorideAmmonium chloride may increase the excretion rate of Sufentanil which could result in a higher serum level.
AmphetamineAmphetamine may increase the analgesic activities of Sufentanil.
AprepitantThe serum concentration of Sufentanil can be increased when it is combined with Aprepitant.
AtenololSufentanil may increase the bradycardic activities of Atenolol.
AzelastineSufentanil 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 Sufentanil.
BendroflumethiazideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Bendroflumethiazide.
BepridilSufentanil may increase the bradycardic activities of Bepridil.
BetaxololSufentanil may increase the bradycardic activities of Betaxolol.
BisoprololSufentanil may increase the bradycardic activities of Bisoprolol.
BretyliumBretylium may increase the bradycardic activities of Sufentanil.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
BumetanideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Bumetanide.
ButorphanolButorphanol may decrease the analgesic activities of Sufentanil.
CarteololSufentanil may increase the bradycardic activities of Carteolol.
CarvedilolSufentanil may increase the bradycardic activities of Carvedilol.
CathinoneCathinone may increase the analgesic activities of Sufentanil.
CeritinibSufentanil may increase the bradycardic activities of Ceritinib.
ChlorothiazideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Chlorothiazide.
ChlorthalidoneThe risk or severity of adverse effects can be increased when Sufentanil is combined with Chlorthalidone.
ConivaptanThe serum concentration of Sufentanil can be increased when it is combined with Conivaptan.
CyclothiazideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Cyclothiazide.
DasatinibThe serum concentration of Sufentanil can be increased when it is combined with Dasatinib.
DesmopressinThe risk or severity of adverse effects can be increased when Sufentanil is combined with Desmopressin.
DiltiazemSufentanil may increase the bradycardic activities of Diltiazem.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
EluxadolineSufentanil may increase the activities of Eluxadoline.
EsmololSufentanil may increase the bradycardic activities of Esmolol.
Etacrynic acidThe risk or severity of adverse effects can be increased when Sufentanil is combined with Ethacrynic acid.
EthanolSufentanil may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthoxzolamideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Ethoxzolamide.
FluconazoleThe metabolism of Sufentanil can be decreased when combined with Fluconazole.
FosaprepitantThe serum concentration of Sufentanil can be increased when it is combined with Fosaprepitant.
FurosemideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Furosemide.
Fusidic AcidThe serum concentration of Sufentanil can be increased when it is combined with Fusidic Acid.
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Hydrochlorothiazide.
HydrocodoneSufentanil may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroflumethiazideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Hydroflumethiazide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
IdelalisibThe serum concentration of Sufentanil can be increased when it is combined with Idelalisib.
IndapamideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Indapamide.
IsocarboxazidSufentanil may increase the serotonergic activities of Isocarboxazid.
IvabradineSufentanil may increase the bradycardic activities of Ivabradine.
IvacaftorThe serum concentration of Sufentanil can be increased when it is combined with Ivacaftor.
LabetalolSufentanil may increase the bradycardic activities of Labetalol.
LacosamideSufentanil may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LevobunololSufentanil may increase the bradycardic activities of Levobunolol.
LinezolidSufentanil may increase the serotonergic activities of Linezolid.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Sufentanil.
LuliconazoleThe serum concentration of Sufentanil can be increased when it is combined with Luliconazole.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
MethotrimeprazineSufentanil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetipranololSufentanil may increase the bradycardic activities of Metipranolol.
MetolazoneThe risk or severity of adverse effects can be increased when Sufentanil is combined with Metolazone.
MetoprololSufentanil may increase the bradycardic activities of Metoprolol.
MetyrosineSufentanil may increase the sedative activities of Metyrosine.
MifepristoneThe serum concentration of Sufentanil can be increased when it is combined with Mifepristone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
MirtazapineSufentanil may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoclobemideSufentanil may increase the serotonergic activities of Moclobemide.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
NadololSufentanil may increase the bradycardic activities of Nadolol.
NaltrexoneThe therapeutic efficacy of Sufentanil can be decreased when used in combination with Naltrexone.
NebivololSufentanil may increase the bradycardic activities of Nebivolol.
NelfinavirThe metabolism of Sufentanil can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Sufentanil can be increased when it is combined with Netupitant.
OctreotideOctreotide may increase the bradycardic activities of Sufentanil.
OrphenadrineSufentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Sufentanil can be increased when it is combined with Palbociclib.
ParaldehydeSufentanil may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineSufentanil may increase the serotonergic activities of Paroxetine.
PegvisomantThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Sufentanil.
PenbutololSufentanil may increase the bradycardic activities of Penbutolol.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
PhenelzineSufentanil may increase the serotonergic activities of Phenelzine.
PindololSufentanil may increase the bradycardic activities of Pindolol.
PramipexoleSufentanil may increase the sedative activities of Pramipexole.
ProcarbazineSufentanil may increase the serotonergic activities of Procarbazine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Sufentanil.
PropranololSufentanil may increase the bradycardic activities of Propranolol.
RamosetronSufentanil may increase the activities of Ramosetron.
RasagilineSufentanil may increase the serotonergic activities of Rasagiline.
RopiniroleSufentanil may increase the sedative activities of Ropinirole.
RotigotineSufentanil may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Sufentanil.
RuxolitinibRuxolitinib may increase the bradycardic activities of Sufentanil.
SelegilineSufentanil may increase the serotonergic activities of Selegiline.
SimeprevirThe serum concentration of Sufentanil can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
SotalolSufentanil may increase the bradycardic activities of Sotalol.
SpironolactoneThe risk or severity of adverse effects can be increased when Sufentanil is combined with Spironolactone.
StiripentolThe serum concentration of Sufentanil can be increased when it is combined with Stiripentol.
SuccinylcholineSuccinylcholine may increase the bradycardic activities of Sufentanil.
SuvorexantSufentanil may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
Tedizolid PhosphateSufentanil may increase the serotonergic activities of Tedizolid Phosphate.
ThalidomideSufentanil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TicrynafenThe risk or severity of adverse effects can be increased when Sufentanil is combined with Ticrynafen.
TimololSufentanil may increase the bradycardic activities of Timolol.
TofacitinibTofacitinib may increase the bradycardic activities of Sufentanil.
TorasemideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Torasemide.
TranylcypromineSufentanil may increase the serotonergic activities of Tranylcypromine.
TriamtereneThe risk or severity of adverse effects can be increased when Sufentanil is combined with Triamterene.
TrichlormethiazideThe risk or severity of adverse effects can be increased when Sufentanil is combined with Trichlormethiazide.
VerapamilSufentanil may increase the bradycardic activities of Verapamil.
ZolpidemSufentanil may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
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. Hurle MA: Changes in the expression of G protein-coupled receptor kinases and beta-arrestin 2 in rat brain during opioid tolerance and supersensitivity. J Neurochem. 2001 Apr;77(2):486-92. [PubMed:11299311 ]
  2. Levron JC: [Pharmacokinetics and pharmacodynamics of morphinomimetics in the central nervous system]. Agressologie. 1991;32(6-7):318-20. [PubMed:1688220 ]
  3. Ilien B, Galzi JL, Mejean A, Goeldner M, Hirth C: A mu-opioid receptor-filter assay. Rapid estimation of binding affinity of ligands and reversibility of long-lasting ligand-receptor complexes. Biochem Pharmacol. 1988 Oct 15;37(20):3843-51. [PubMed:2847746 ]
  4. Colpaert FC, Leysen JE, Michiels M, van den Hoogen RH: Epidural and intravenous sufentanil in the rat: analgesia, opiate receptor binding, and drug concentrations in plasma and brain. Anesthesiology. 1986 Jul;65(1):41-9. [PubMed:3014923 ]
  5. Leysen JE, Gommeren W: In vitro binding properties of 3H-sufentanil, a superior ligand for the mu-opiate receptor. Arch Int Pharmacodyn Ther. 1982 Dec;260(2):287-9. [PubMed:6131653 ]
  6. 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
unknown
Actions
agonist
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. Freye E, Latasch L, Portoghese PS: The delta receptor is involved in sufentanil-induced respiratory depression--opioid subreceptors mediate different effects. Eur J Anaesthesiol. 1992 Nov;9(6):457-62. [PubMed:1330549 ]
  2. Zhu J, Xue JC, Law PY, Claude PA, Luo LY, Yin J, Chen C, Liu-Chen LY: The region in the mu opioid receptor conferring selectivity for sufentanil over the delta receptor is different from that over the kappa receptor. FEBS Lett. 1996 Apr 15;384(2):198-202. [PubMed:8612823 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other
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. Zhu J, Xue JC, Law PY, Claude PA, Luo LY, Yin J, Chen C, Liu-Chen LY: The region in the mu opioid receptor conferring selectivity for sufentanil over the delta receptor is different from that over the kappa receptor. FEBS Lett. 1996 Apr 15;384(2):198-202. [PubMed:8612823 ]
  2. Chang HM, Berde CB, Holz GG 4th, Steward GF, Kream RM: Sufentanil, morphine, met-enkephalin, and kappa-agonist (U-50,488H) inhibit substance P release from primary sensory neurons: a model for presynaptic spinal opioid actions. Anesthesiology. 1989 Apr;70(4):672-7. [PubMed:2467589 ]

Enzymes

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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23