Identification

Name
Dantrolene
Accession Number
DB01219  (APRD00901)
Type
Small Molecule
Groups
Approved
Description

Chemically, dantrolene is a hydantoin derivative, but does not exhibit antiepileptic activity like other hydantoin derivates such as phenytoin.

Structure
Thumb
Synonyms
  • Dantamacrin
  • Dantrolene
  • Dantroleno
  • Dantrolenum
  • F-368
Product Ingredients
IngredientUNIICASInChI Key
Dantrolene Sodium287M0347EV24868-20-0OZOMQRBLCMDCEG-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DantriumInjection20 mg/60mLIntravenousPar Pharmaceutical2008-08-01Not applicableUs
DantriumCapsule50 mg/1OralPar Pharmaceutical2008-08-01Not applicableUs
DantriumCapsule25 mg/1OralPar Pharmaceutical2008-08-01Not applicableUs
DantriumCapsule100 mg/1OralPar Pharmaceutical2008-08-012017-05-10Us
Dantrium Cap 100mgCapsule100 mgOralNorwich Eaton Canada Inc.1979-12-311996-09-16Canada
Dantrium Cap 25mgCapsule25 mgOralNorwich Eaton Canada Inc.1979-12-311996-09-16Canada
Dantrium CapsulesCapsule25 mgOralPar Pharmaceutical Companies1993-12-31Not applicableCanada
Dantrium CapsulesCapsule100 mgOralPar Pharmaceutical Companies1993-12-31Not applicableCanada
Dantrium IntravenousPowder, for solution20 mgIntravenousPar Pharmaceutical Companies1993-12-31Not applicableCanada
Dantrolene SodiumCapsule50 mg/1OralPar Pharmaceutical2016-02-19Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dantrolene SodiumCapsule25 mg/1OralAmerincan Health Packaging2008-09-25Not applicableUs
Dantrolene SodiumCapsule25 mg/1OralImpax Generics2005-03-01Not applicableUs
Dantrolene SodiumCapsule100 mg/1OralImpax Generics2005-03-01Not applicableUs
Dantrolene SodiumCapsule25 mg/1OralCarilion Materials Management2005-03-01Not applicableUs
Dantrolene SodiumCapsule25 mg/1OralCardinal Health2008-09-25Not applicableUs
Dantrolene SodiumCapsule50 mg/1OralImpax Generics2005-03-01Not applicableUs
Dantrolene SodiumCapsule25 mg/1OralAvera Mc Kennan Hospital2016-09-13Not applicableUs
RevontoInjection, powder, lyophilized, for solution20 mg/60mLIntravenousUs World Meds, Llc2012-06-042017-03-31Us
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DantroleneInjection, powder, for solution20 mg/1IntravenousWest Ward Pharmaceutical2017-06-19Not applicableUs
International/Other Brands
Dantamacrin (Spepharm) / Dantrium
Categories
UNII
F64QU97QCR
CAS number
7261-97-4
Weight
Average: 314.253
Monoisotopic: 314.06511945
Chemical Formula
C14H10N4O5
InChI Key
OZOMQRBLCMDCEG-VIZOYTHASA-N
InChI
InChI=1S/C14H10N4O5/c19-13-8-17(14(20)16-13)15-7-11-5-6-12(23-11)9-1-3-10(4-2-9)18(21)22/h1-7H,8H2,(H,16,19,20)/b15-7+
IUPAC Name
1-({[5-(4-nitrophenyl)furan-2-yl]methylidene}amino)imidazolidine-2,4-dione
SMILES
[O-][N+](=O)C1=CC=C(C=C1)C1=CC=C(O1)C=NN1CC(=O)NC1=O

Pharmacology

Indication

For use, along with appropriate supportive measures, for the management of the fulminant hypermetabolism of skeletal muscle characteristic of malignant hyperthermia crises in patients of all ages. Also used preoperatively, and sometimes postoperatively, to prevent or attenuate the development of clinical and laboratory signs of malignant hyperthermia in individuals judged to be malignant hyperthermia susceptible.

Structured Indications
Pharmacodynamics

Dantrolene is classified as a direct-acting skeletal muscle relaxant. It is currently the only specific and effective treatment for malignant hyperthermia. In isolated nerve-muscle preparation, Dantrium has been shown to produce relaxation by affecting the contractile response of the muscle at a site beyond the myoneural junction. In skeletal muscle, Dantrium dissociates excitation-contraction coupling, probably by interfering with the release of Ca2+ from the sarcoplasmic reticulum. In the anesthetic-induced malignant hyperthermia syndrome, evidence points to an intrinsic abnormality of skeletal muscle tissue. In selected humans, it has been postulated that “triggering agents” (e.g.,general anesthetics and depolarizing neuromuscular blocking agents) produce a change within the cell which results in an elevated myoplasmic calcium. This elevated myoplasmic calcium activates acute cellular catabolic processes that cascade to the malignant hyperthermia crisis. It is hypothesized that addition of Dantrium to the “triggered” malignant hyperthermic muscle cell reestablishes a normal level of ionized calcium in the myoplasm.

Mechanism of action

Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1, and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction.

TargetActionsOrganism
ARyanodine receptor 1
antagonist
Human
Absorption

Bioavailability is 70%.

Volume of distribution
Not Available
Protein binding

Significant, mostly to albumin.

Metabolism

Hepatic, most likely by hepatic microsomal enzymes. Its major metabolites in body fluids are 5-hydroxydantrolene and an acetylamino metabolite of dantrolene. Another metabolite with an unknown structure appears related to the latter. Dantrium may also undergo hydrolysis and subsequent oxidation forming nitrophenylfuroic acid.

Route of elimination
Not Available
Half life

The mean biologic half-life after intravenous administration is variable, between 4 to 8 hours under most experimental conditions, while oral is 8.7 hours for a 100mg dose.

Clearance
Not Available
Toxicity

Oral LD50 in rats is 7400 mg/kg. Symptoms which may occur in case of overdose include, but are not limited to, muscular weakness and alterations in the state of consciousness (e.g., lethargy, coma), vomiting, diarrhea, and crystalluria.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AmiodaroneThe metabolism of Dantrolene can be decreased when combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Dantrolene can be increased when it is combined with Aprepitant.Approved, Investigational
AtazanavirThe metabolism of Dantrolene can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Dantrolene can be decreased when combined with Atomoxetine.Approved
BoceprevirThe metabolism of Dantrolene can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Dantrolene can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Dantrolene can be decreased when it is combined with Bosentan.Approved, Investigational
CarbamazepineThe metabolism of Dantrolene can be increased when combined with Carbamazepine.Approved, Investigational
CeritinibThe serum concentration of Dantrolene can be increased when it is combined with Ceritinib.Approved
ClarithromycinThe metabolism of Dantrolene can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Dantrolene can be decreased when combined with Clemastine.Approved
ClotrimazoleThe metabolism of Dantrolene can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Dantrolene can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Dantrolene.Approved, Investigational
CrizotinibThe metabolism of Dantrolene can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Dantrolene can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Dantrolene can be decreased when it is combined with Dabrafenib.Approved
DarunavirThe metabolism of Dantrolene can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Dantrolene can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Dantrolene can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Dantrolene can be decreased when combined with Delavirdine.Approved
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Dantrolene.Approved, Investigational
DihydroergotamineThe metabolism of Dantrolene can be decreased when combined with Dihydroergotamine.Approved
DiltiazemDantrolene may increase the hyperkalemic activities of Diltiazem.Approved
DiltiazemThe metabolism of Dantrolene can be decreased when combined with Diltiazem.Approved
DoxycyclineThe metabolism of Dantrolene can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Dantrolene can be decreased when combined with Dronedarone.Approved
EnzalutamideThe serum concentration of Dantrolene can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Dantrolene can be decreased when combined with Erythromycin.Approved, Vet Approved
FluconazoleThe metabolism of Dantrolene can be decreased when combined with Fluconazole.Approved
FluvoxamineThe metabolism of Dantrolene can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Dantrolene can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Dantrolene can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Dantrolene can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Dantrolene can be increased when it is combined with Fusidic Acid.Approved
IdelalisibThe metabolism of Dantrolene can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Dantrolene can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Dantrolene can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Dantrolene can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Dantrolene can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Dantrolene can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Dantrolene can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Dantrolene can be decreased when combined with Ketoconazole.Approved, Investigational
LacidipineThe risk or severity of adverse effects can be increased when Lacidipine is combined with Dantrolene.Approved, Investigational
LopinavirThe metabolism of Dantrolene can be decreased when combined with Lopinavir.Approved
LovastatinThe metabolism of Dantrolene can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Dantrolene can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Dantrolene can be increased when combined with Lumacaftor.Approved
MifepristoneThe serum concentration of Dantrolene can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Dantrolene can be decreased when it is combined with Mitotane.Approved
NefazodoneThe metabolism of Dantrolene can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Dantrolene can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Dantrolene can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Dantrolene can be increased when combined with Nevirapine.Approved
NilotinibThe metabolism of Dantrolene can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Dantrolene can be decreased when combined with Olaparib.Approved
OsimertinibThe serum concentration of Dantrolene can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Dantrolene can be increased when it is combined with Palbociclib.Approved
PentobarbitalThe metabolism of Dantrolene can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Dantrolene can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Dantrolene can be increased when combined with Phenytoin.Approved, Vet Approved
PosaconazoleThe metabolism of Dantrolene can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Dantrolene can be increased when combined with Primidone.Approved, Vet Approved
RanolazineThe metabolism of Dantrolene can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Dantrolene can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Dantrolene can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Dantrolene can be increased when combined with Rifapentine.Approved
RucaparibThe metabolism of Dantrolene can be decreased when combined with Rucaparib.Approved, Investigational
SaquinavirThe metabolism of Dantrolene can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Dantrolene can be decreased when used in combination with Sarilumab.Approved
SildenafilThe metabolism of Dantrolene can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Dantrolene can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Dantrolene can be increased when it is combined with Simeprevir.Approved
St. John's WortThe serum concentration of Dantrolene can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Dantrolene can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Dantrolene can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TelaprevirThe metabolism of Dantrolene can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Dantrolene can be decreased when combined with Telithromycin.Approved
TiclopidineThe metabolism of Dantrolene can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Dantrolene can be decreased when it is combined with Tocilizumab.Approved
VecuroniumDantrolene may increase the neuromuscular blocking activities of Vecuronium.Approved
VemurafenibThe serum concentration of Dantrolene can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Dantrolene can be decreased when combined with Venlafaxine.Approved
VerapamilDantrolene may increase the hyperkalemic activities of Verapamil.Approved
VerapamilThe metabolism of Dantrolene can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Dantrolene can be decreased when combined with Voriconazole.Approved, Investigational
ZiprasidoneThe metabolism of Dantrolene can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Take without regard to meals.

References

Synthesis Reference

Davis, C.S. and Snyder, H.R. Jr.; US. Patent 3,415,821; December 10, 1968; assigned to The Norwich Pharmacal Company.

General References
  1. Krause T, Gerbershagen MU, Fiege M, Weisshorn R, Wappler F: Dantrolene--a review of its pharmacology, therapeutic use and new developments. Anaesthesia. 2004 Apr;59(4):364-73. [PubMed:15023108]
External Links
KEGG Drug
D02347
KEGG Compound
C06939
PubChem Compound
6914273
PubChem Substance
46504976
ChemSpider
5290202
ChEBI
4317
ChEMBL
CHEMBL1201288
Therapeutic Targets Database
DNC001623
PharmGKB
PA449208
IUPHAR
4172
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Dantrolene
ATC Codes
M03CA01 — Dantrolene
AHFS Codes
  • 12:20.08 — Direct-acting Skeletal Muscle Relaxants
MSDS
Download (43 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1, 2CompletedTreatmentCerebral Vasospasm After Subarachnoid Hemorrhage1
1, 2CompletedTreatmentCerebral Vasospasm / Subarachnoid Hemorrhage1
1, 2RecruitingTreatmentAtaxia / Diabetes Mellitus (DM) / Optic Nerve Atrophy / Wolfram Syndrome1
2, 3TerminatedTreatmentHyperthermia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
CapsuleOral100 mg/1
CapsuleOral50 mg/1
InjectionIntravenous20 mg/60mL
CapsuleOral100 mg
CapsuleOral25 mg
Powder, for solutionIntravenous20 mg
Injection, powder, for solutionIntravenous20 mg/1
CapsuleOral25 mg/1
Injection, powder, lyophilized, for solutionIntravenous20 mg/60mL
Injection, suspensionIntravenous250 mg/5mL
Prices
Unit descriptionCostUnit
Dantrium 20 mg vial106.37USD vial
Dantrolene sodium 20 mg vial97.2USD vial
Dantrolene sodium powder17.6USD g
Dantrium 100 mg capsule2.4USD capsule
Dantrolene sodium 100 mg capsule2.03USD capsule
Dantrium 50 mg capsule1.93USD capsule
Dantrolene sodium 50 mg capsule1.63USD capsule
Dantrium 25 mg capsule1.29USD capsule
Dantrolene sodium 25 mg capsule1.09USD capsule
Dantrium 100 mg Capsule0.8USD capsule
Dantrium 25 mg Capsule0.4USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8685460No2003-02-152023-02-15Us
US7758890No2005-07-012025-07-01Us
US8110225No2002-12-242022-12-24Us
US8604072No2002-12-242022-12-24Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)279-280 °CDavis, C.S. and Snyder, H.R. Jr.; US. Patent 3,415,821; December 10, 1968; assigned to The Norwich Pharmacal Company.
water solubilityLow (146 mg/L)Not Available
logP1.70JANSEN,ACA ET AL. (1991)
Predicted Properties
PropertyValueSource
Water Solubility0.0805 mg/mLALOGPS
logP1.65ALOGPS
logP1.26ChemAxon
logS-3.6ALOGPS
pKa (Strongest Acidic)9.23ChemAxon
pKa (Strongest Basic)-1.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area120.73 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity78.87 m3·mol-1ChemAxon
Polarizability29.98 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9974
Blood Brain Barrier+0.9581
Caco-2 permeable-0.5587
P-glycoprotein substrateNon-substrate0.6562
P-glycoprotein inhibitor INon-inhibitor0.8977
P-glycoprotein inhibitor IINon-inhibitor0.978
Renal organic cation transporterNon-inhibitor0.8656
CYP450 2C9 substrateNon-substrate0.81
CYP450 2D6 substrateNon-substrate0.8935
CYP450 3A4 substrateSubstrate0.5848
CYP450 1A2 substrateInhibitor0.8916
CYP450 2C9 inhibitorNon-inhibitor0.8808
CYP450 2D6 inhibitorNon-inhibitor0.9203
CYP450 2C19 inhibitorNon-inhibitor0.8752
CYP450 3A4 inhibitorNon-inhibitor0.8985
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7676
Ames testAMES toxic0.8925
CarcinogenicityNon-carcinogens0.8732
BiodegradationReady biodegradable0.5901
Rat acute toxicity2.5390 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7215
hERG inhibition (predictor II)Non-inhibitor0.9223
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

Taxonomy

Description
This compound belongs to the class of organic compounds known as hydantoins. These are heterocyclic compounds containing an imidazolidine substituted by ketone group at positions 2 and 4.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Azolidines
Sub Class
Imidazolidines
Direct Parent
Hydantoins
Alternative Parents
Alpha amino acids and derivatives / Nitrobenzenes / Nitroaromatic compounds / Semicarbazones / Dicarboximides / Furans / Heteroaromatic compounds / Organic carbonic acids and derivatives / Oxacyclic compounds / Azacyclic compounds
show 7 more
Substituents
Hydantoin / Alpha-amino acid or derivatives / Nitrobenzene / Nitroaromatic compound / Monocyclic benzene moiety / Semicarbazone / Benzenoid / Heteroaromatic compound / Dicarboximide / Furan
show 21 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
hydrazone, imidazolidine-2,4-dione (CHEBI:4317)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Voltage-gated calcium channel activity
Specific Function
Calcium channel that mediates the release of Ca(2+) from the sarcoplasmic reticulum into the cytoplasm and thereby plays a key role in triggering muscle contraction following depolarization of T-tu...
Gene Name
RYR1
Uniprot ID
P21817
Uniprot Name
Ryanodine receptor 1
Molecular Weight
565170.715 Da
References
  1. Britt BA, Scott E, Frodis W, Clements MJ, Endrenyi L: Dantrolene--in vitro studies in malignant hyperthermia susceptible (MHS) and normal skeletal muscle. Can Anaesth Soc J. 1984 Mar;31(2):130-54. [PubMed:6704779]
  2. Harrison GG: Control of the malignant hyperpyrexic syndrome in MHS swine by dantrolene sodium. 1975. Br J Anaesth. 1998 Oct;81(4):626-9; discussion 625. [PubMed:9924249]
  3. Flewellen EH, Nelson TE: Dantrolene dose response in malignant hyperthermia-susceptible (MHS) swine: method to obtain prophylaxis and therapeusis. Anesthesiology. 1980 Apr;52(4):303-8. [PubMed:7362049]
  4. Tonner PH, Scholz J, Richter A, Loscher W, Steinfath M, Wappler F, Wlaz P, Hadji B, Roewer N, Schulte am Esch J: Alterations of inositol polyphosphates in skeletal muscle during porcine malignant hyperthermia. Br J Anaesth. 1995 Oct;75(4):467-71. [PubMed:7488490]
  5. Zhao X, Weisleder N, Han X, Pan Z, Parness J, Brotto M, Ma J: Azumolene inhibits a component of store-operated calcium entry coupled to the skeletal muscle ryanodine receptor. J Biol Chem. 2006 Nov 3;281(44):33477-86. Epub 2006 Aug 31. [PubMed:16945924]
  6. Krause T, Gerbershagen MU, Fiege M, Weisshorn R, Wappler F: Dantrolene--a review of its pharmacology, therapeutic use and new developments. Anaesthesia. 2004 Apr;59(4):364-73. [PubMed:15023108]
  7. Gerbershagen MU, Fiege M, Krause T, Agarwal K, Wappler F: [Dantrolene. Pharmacological and therapeutic aspects]. Anaesthesist. 2003 Mar;52(3):238-45. [PubMed:12666006]
  8. Paul-Pletzer K, Yamamoto T, Bhat MB, Ma J, Ikemoto N, Jimenez LS, Morimoto H, Williams PG, Parness J: Identification of a dantrolene-binding sequence on the skeletal muscle ryanodine receptor. J Biol Chem. 2002 Sep 20;277(38):34918-23. Epub 2002 Jul 11. [PubMed:12167662]
  9. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
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 January 15, 2018 08:52