Identification

Name
Sufentanil
Accession Number
DB00708  (APRD00671, DB05563)
Type
Small Molecule
Groups
Approved, 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 IDs
IDS-NS-001 / R 30730 / R 33800
Product Ingredients
IngredientUNIICASInChI Key
Sufentanil CitrateS9ZFX8403R60561-17-3OJCZPLDERGDQRJ-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SufentaSolution50 ug/1mLIntravenousTaylor Pharmaceuticals2008-07-02Not applicableUs
Sufenta Inj 50mcg/mlLiquid50 mcgIntravenousJanssen Pharmaceutica, Division Of Janssen Ortho Inc.1985-12-311996-09-10Canada
Sufenta Inj 50mcg/mlLiquid50 mcgEpidural; IntravenousJanssen Pharmaceuticals1985-12-312007-11-26Canada
Sufentanil CitrateInjection50 ug/1mLEpidural; IntravenousAkorn2010-12-01Not applicableUs
Sufentanil CitrateInjection, solution50 ug/1mLEpidural; IntravenousHospira, Inc.2006-10-062006-10-06Us
Sufentanil Citrate Injection USPSolution50 mcgEpidural; IntravenousSandoz Canada Incorporated2001-08-01Not applicableCanada
Sufentanil Citrate Injection, USPSolution50 mcgEpidural; IntravenousSterimax Inc2016-10-18Not applicableCanada
ZalvisoTablet15 μgSublingualGrunenthal Gmb H2015-09-18Not applicableEu
ZalvisoTablet15 μgSublingualGrunenthal Gmb H2015-09-18Not applicableEu
ZalvisoTablet15 μgSublingualGrunenthal Gmb H2015-09-18Not applicableEu
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Sufentanil CitrateInjection0.05 mg/1mLEpidural; IntravenousWest-Ward Pharmaceuticals Corp.1995-12-15Not applicableUs
Sufentanil CitrateInjection0.05 mg/1mLEpidural; IntravenousBaxter Laboratories2002-12-022014-03-31Us
Sufentanil CitrateInjection0.05 mg/1mLEpidural; IntravenousWest-Ward Pharmaceuticals Corp.1995-12-15Not applicableUs
Sufentanil CitrateInjection0.05 mg/1mLEpidural; IntravenousWest-Ward Pharmaceuticals Corp.1995-12-15Not applicableUs
Sufentanil CitrateInjection, solution50 ug/1mLEpidural; IntravenousHospira, Inc.2005-07-26Not applicableUs
International/Other Brands
Chronogesic (DURECT) / Disufen (Angenerico) / Fastfen (Cristália) / Sufenta (Janssen) / Sufenta Forte (Janssen) / Sufenta mite (Janssen) / Sufentil (Claris Lifesciences Ltd.) / Zuftil (Pisa)
Categories
UNII
AFE2YW0IIZ
CAS number
56030-54-7
Weight
Average: 386.551
Monoisotopic: 386.202798904
Chemical Formula
C22H30N2O2S
InChI Key
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

Pharmacology

Indication

Used as an analgesic adjunct in anesthesia and as a primary anesthetic drug in procedures requiring assisted ventilation and in the relief of pain.

Associated Therapies
Pharmacodynamics

Sufentanil 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 action

Opiate 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.

TargetActionsOrganism
AMu-type opioid receptor
agonist
Human
UDelta-type opioid receptor
agonist
Human
UKappa-type opioid receptor
other
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

265 minutes

Clearance
Not Available
Toxicity

LD50: 18.7 mg/kg (IV in mice)

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Sufentanil Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(2-benzhydryloxyethyl)diethyl-methylammonium iodideThe risk or severity of adverse effects can be increased when (2-benzhydryloxyethyl)diethyl-methylammonium iodide is combined with Sufentanil.
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Sufentanil.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Sufentanil.
16-BromoepiandrosteroneThe metabolism of 16-Bromoepiandrosterone can be decreased when combined with Sufentanil.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Sufentanil is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when Sufentanil is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of serotonin syndrome can be increased when Sufentanil is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Sufentanil.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of serotonin syndrome can be increased when Sufentanil is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Sufentanil.
Food Interactions
Not 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 References
Not Available
External Links
Human Metabolome Database
HMDB0014846
KEGG Drug
D05938
KEGG Compound
C08022
PubChem Compound
41693
PubChem Substance
46504737
ChemSpider
38043
BindingDB
94503
ChEBI
9316
ChEMBL
CHEMBL658
Therapeutic Targets Database
DAP000357
PharmGKB
PA451527
IUPHAR
3534
Guide to Pharmacology
GtP Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Sufentanil
ATC Codes
N01AH03 — Sufentanil
AHFS Codes
  • 28:08.08 — Opiate Agonists
MSDS
Download (47.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic SciencePlasma Concentrations1
1, 2TerminatedTreatmentOpioids / Pain1
2CompletedTreatmentAnaesthesia therapy1
2CompletedTreatmentMajor Upper or Lower Abdominal Surgery1
2CompletedTreatmentPain1
2CompletedTreatmentPregnant Women1
2Not Yet RecruitingTreatmentHead Trauma1
2RecruitingTreatmentPrenatal Diagnosis1
2WithdrawnTreatmentPain, Chronic1
2, 3Active Not RecruitingTreatmentCerebral Hypoperfusion / Intubation, Endotracheal / Premedication1
2, 3Active Not RecruitingTreatmentIntubation, Endotracheal / Premedication1
2, 3Active Not RecruitingTreatmentMyocardial Injury1
2, 3CompletedSupportive CareHealthy Volunteers / Pelvic Floor Disorders / Prolonged Labour1
3CompletedPreventionNormal Pregnancies1
3CompletedTreatmentChild Comfort / Intensive Care Units / Morphine / Pediatric1
3CompletedTreatmentModerate-to-severe Acute Pain1
3CompletedTreatmentPain, Acute1
3CompletedTreatmentPost Operative Pain1
3CompletedTreatmentPost-Operative Pain3
3CompletedTreatmentPostoperative pain1
3Not Yet RecruitingTreatmentObstetric Pain / Other Complications of Obstetric Anesthesia - Delivered1
3RecruitingTreatmentLumbar epidural anesthesia therapy1
4Active Not RecruitingTreatmentDriving Performance After Minor Ambulatory Surgery / Minor Surgical Procedures With Monitored Anesthesia Care1
4Active Not RecruitingTreatmentTrigeminal Neuralgia (TN)1
4CompletedNot AvailableAortic Aneurysms1
4CompletedBasic ScienceAnaesthesia therapy1
4CompletedPreventionAortic Valve Stenosis / Ischaemic Heart Diseases1
4CompletedSupportive CarePain1
4CompletedSupportive CarePost-Operative Nausea and Vomiting (PONV) / Postoperative pain1
4CompletedTreatmentAnalgesics / Pain, Chronic / Postoperative pain1
4CompletedTreatmentNumeric Pain Rating Scale > 5 / 10 / Severe Traumatic Pain1
4CompletedTreatmentPain3
4CompletedTreatmentPostoperative pain2
4CompletedTreatmentSingle Traumatic Limb Injury With Severe Pain (Score > 5/10 on Numerical Pain Scale)1
4Enrolling by InvitationSupportive CarePostoperative; Dysfunction Following Cardiac Surgery1
4Not Yet RecruitingPreventionPostoperative Cognitive Dysfunction / Postoperative Delirium1
4Not Yet RecruitingTreatmentAnalgesia, Patient-Controlled1
4Not Yet RecruitingTreatmentAnesthesia; Functional1
4RecruitingPreventionCoronary Artery Bypass Graft Redo / General Anesthetic Drug Adverse Reaction1
4RecruitingSupportive CarePregnancy1
4RecruitingTreatmentAnalgesia, Patient-Controlled / Anesthesia; Spinal / Intravenous Drug Delivery Systems / Lumbar epidural anesthesia / Morphine / Surgery, Colorectal1
4RecruitingTreatmentArteriovenous Malformations1
4RecruitingTreatmentLabour Pain1
4RecruitingTreatmentLabour Pain / Lumbar epidural anesthesia therapy / Opioids1
4RecruitingTreatmentPain, Acute1
4RecruitingTreatmentPatients Ongoing Elective Abdominal Laparoscopy1
4RecruitingTreatmentPostoperative pain1
4TerminatedTreatmentAnalgesia / Sedation therapy1
4TerminatedTreatmentThoracic Surgery1
4Unknown StatusTreatmentAdrenal Suppression / Hemodynamics Instability1
4Unknown StatusTreatmentAnalgesia, Patient-Controlled / Arthroplasty / Gastric Resection1
Not AvailableCompletedNot AvailableAdequate Anesthesia With Unimpaired Motor Strength1
Not AvailableCompletedDiagnosticProstate Cancer1
Not AvailableCompletedOtherLoss of Consciousness1
Not AvailableCompletedPreventionAnaesthesia therapy / Pain1
Not AvailableCompletedPreventionKidney Donation/Transplantation1
Not AvailableCompletedPreventionPost-Operative Nausea and Vomiting (PONV)1
Not AvailableCompletedScreeningKnee Surgery With Tourniquet1
Not AvailableCompletedSupportive CareEpidural Block / Malignant Neoplasm of Esophagus / Oesophagectomy1
Not AvailableCompletedSupportive CareInstrumental Delivery / Lumbar epidural anesthesia / Maternal Outcome / Neonatal Outcome1
Not AvailableCompletedSupportive CareTotal Knee Arthroplasty (TKA)1
Not AvailableCompletedTreatmentAnaesthesia therapy1
Not AvailableCompletedTreatmentAnesthesia Complications1
Not AvailableCompletedTreatmentBalanced Anesthesia1
Not AvailableCompletedTreatmentIschaemic Heart Diseases1
Not AvailableCompletedTreatmentLabour Pain1
Not AvailableCompletedTreatmentNeoplasms, Pancreatic1
Not AvailableCompletedTreatmentPediatric Ventricular Septal Defects1
Not AvailableCompletedTreatmentPost Operative Pain Management1
Not AvailableNot Yet RecruitingSupportive CareCardiovascular Disease (CVD)1
Not AvailableNot Yet RecruitingTreatmentAdult Disease / Liver Diseases1
Not AvailableNot Yet RecruitingTreatmentC.Delivery; Surgery (Previous), Gynecological1
Not AvailableNot Yet RecruitingTreatmentGeneral Surgery / Hallux Valgus1
Not AvailableNot Yet RecruitingTreatmentLiver Diseases / Neoplasms, Hepatic / Secondary Malignant Neoplasm of Liver1
Not AvailableRecruitingNot AvailableAnalgesic Quality / Mobility1
Not AvailableRecruitingTreatmentLabor Analgesia1
Not AvailableRecruitingTreatmentLabour Pain1
Not AvailableRecruitingTreatmentPostoperative Complications1
Not AvailableTerminatedDiagnosticLabour Pain1
Not AvailableUnknown StatusHealth Services ResearchPregnancy1
Not AvailableUnknown StatusSupportive CareAdjunct to general anesthesia therapy1
Not AvailableUnknown StatusTreatmentHaemodynamic Fluctuations During Off-pump CABG1

Pharmacoeconomics

Manufacturers
  • Akorn inc
  • Baxter healthcare corp anesthesia and critical care
  • Hospira inc
  • Watson laboratories inc
Packagers
  • Akorn Inc.
  • Baxter International Inc.
  • Generamedix Inc.
  • Hospira Inc.
  • Mallinckrodt Inc.
  • Taylor Pharmaceuticals
Dosage forms
FormRouteStrength
SolutionIntravenous50 ug/1mL
LiquidEpidural; Intravenous50 mcg
LiquidIntravenous50 mcg
InjectionEpidural; Intravenous0.05 mg/1mL
InjectionEpidural; Intravenous50 ug/1mL
Injection, solutionEpidural; Intravenous50 ug/1mL
SolutionEpidural; Intravenous50 mcg
TabletSublingual15 μg
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.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)97 °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
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0009000000-0f9e477eb2153eb20409
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0096000000-73641c83c08b872641cd
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-06ri-1981000000-b5f4aaab095cc6fc533c
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-03di-1900000000-2fdfd1d5fa6e43fa1604
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-03di-4900000000-bd92c052347dc0822a01

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Anilides
Direct Parent
Anilides
Alternative Parents
Aralkylamines / Piperidines / Thiophenes / Tertiary carboxylic acid amides / Heteroaromatic compounds / Trialkylamines / Amino acids and derivatives / Dialkyl ethers / Azacyclic compounds / Organopnictogen compounds
show 3 more
Substituents
Anilide / Aralkylamine / Piperidine / Tertiary carboxylic acid amide / Heteroaromatic compound / Thiophene / Amino acid or derivatives / Carboxamide group / Tertiary amine / Tertiary aliphatic amine
show 15 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
piperidines, thiophenes, ether, anilide (CHEBI:9316)

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...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
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 n...
Gene Name
OPRD1
Uniprot ID
P41143
Uniprot Name
Delta-type opioid receptor
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 synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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]

Drug created on June 13, 2005 07:24 / Updated on October 16, 2018 08:30