Identification

Name
Nicardipine
Accession Number
DB00622  (APRD00088)
Type
Small Molecule
Groups
Approved, Investigational
Description

A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. [PubChem]

Structure
Thumb
Synonyms
  • Nicardipino
  • Nicardipinum
Product Ingredients
IngredientUNIICASInChI Key
Nicardipine HydrochlorideK5BC5011K354527-84-3AIKVCUNQWYTVTO-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cardene 20mg CapsulesCapsule20 mgOralHoffmann La Roche1996-12-312001-07-19Canada
Cardene 30mg CapsulesCapsule30 mgOralHoffmann La Roche1998-01-212001-07-19Canada
Cardene Cap 30mgCapsule30 mgOralSyntex Inc.1990-12-311998-09-03Canada
Cardene I.V.Injection, solution0.2 mg/1mLIntravenousEkr Therapeutics1992-01-302017-10-01Us
Cardene I.V.Injection2.5 mg/1mLIntravenousEkr Therapeutics1992-01-30Not applicableUs
Cardene I.V.Injection, solution0.1 mg/1mLIntravenousEkr Therapeutics1992-01-302017-10-01Us
Cardene I.V.Injection, solution0.2 mg/1mLIntravenousEkr Therapeutics1992-01-302017-10-01Us
Cardene I.V.Injection, solution0.1 mg/1mLIntravenousEkr Therapeutics1992-01-302017-10-01Us
Cardene IVInjection, solution0.1 mg/1mLIntravenousChiesi Pharmaceuticals Inc.1992-01-30Not applicableUs
Cardene IVInjection, solution0.2 mg/1mLIntravenousChiesi Pharmaceuticals Inc.1992-01-30Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nicardipine HydrochlorideInjection2.5 mg/1mLIntravenousSandoz2009-11-17Not applicableUs
Nicardipine HydrochlorideCapsule20 mg/1OralEpic Pharma, LLC2010-05-05Not applicableUs
Nicardipine HydrochlorideCapsule20 mg/1OralMylan Pharmaceuticals1996-07-19Not applicableUs
Nicardipine HydrochlorideInjection2.5 mg/1mLIntravenousEmcure Pharmaceuticals Ltd.2009-11-17Not applicableUs
Nicardipine HydrochlorideInjection, solution2.5 mg/1mLIntravenousAmerican Regent2009-11-17Not applicableUs
Nicardipine HydrochlorideCapsule20 mg/1OralPuraCap Laboratories LLC dba Blu Pharmaceuticals2016-12-15Not applicableUs
Nicardipine HydrochlorideCapsule30 mg/1OralAv Kare, Inc.2010-05-052017-11-01Us
Nicardipine HydrochlorideCapsule20 mg/1OralGenpharm Ulc2015-11-012015-11-30Us
Nicardipine HydrochlorideCapsule30 mg/1OralTeva2011-02-282011-02-28Us
Nicardipine HydrochlorideInjection2.5 mg/1mLIntravenousWockhardt2009-11-17Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
CardeneNicardipine Hydrochloride (60 mg/1)Capsule, extended releaseOralRoche Pharmaceuticals2006-04-12Not applicableUs
CardeneNicardipine Hydrochloride (2.5 mg/1mL)InjectionIntravenousESP Pharma, Inc.2006-10-08Not applicableUs
CardeneNicardipine Hydrochloride (30 mg/1)Capsule, gelatin coatedOralRoche Pharmaceuticals2007-03-31Not applicableUs
CardeneNicardipine Hydrochloride (45 mg/1)Capsule, extended releaseOralRoche Pharmaceuticals2006-04-12Not applicableUs
CardeneNicardipine Hydrochloride (20 mg/1)Capsule, gelatin coatedOralRoche Pharmaceuticals2007-03-31Not applicableUs
CardeneNicardipine Hydrochloride (30 mg/1)Capsule, extended releaseOralRoche Pharmaceuticals2006-04-12Not applicableUs
CardeneNicardipine Hydrochloride (2.5 mg/1mL)InjectionIntravenousESP Pharma, Inc.2007-03-30Not applicableUs
Cardene SRNicardipine Hydrochloride (45 mg/1)Capsule, gelatin coatedOralPDL BioPharma, Inc.2008-04-21Not applicableUs
Cardene SRNicardipine Hydrochloride (30 mg/1)Capsule, gelatin coatedOralPDL BioPharma, Inc.2008-04-21Not applicableUs
Cardene SRNicardipine Hydrochloride (60 mg/1)Capsule, gelatin coatedOralPDL BioPharma, Inc.2008-04-21Not applicableUs
International/Other Brands
Cardene (Roche)
Categories
UNII
CZ5312222S
CAS number
55985-32-5
Weight
Average: 479.525
Monoisotopic: 479.205635675
Chemical Formula
C26H29N3O6
InChI Key
ZBBHBTPTTSWHBA-UHFFFAOYSA-N
InChI
InChI=1S/C26H29N3O6/c1-17-22(25(30)34-4)24(20-11-8-12-21(15-20)29(32)33)23(18(2)27-17)26(31)35-14-13-28(3)16-19-9-6-5-7-10-19/h5-12,15,24,27H,13-14,16H2,1-4H3
IUPAC Name
3-{2-[benzyl(methyl)amino]ethyl} 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
SMILES
COC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OCCN(C)CC1=CC=CC=C1

Pharmacology

Indication

Used for the management of patients with chronic stable angina and for the treatment of hypertension.

Associated Conditions
Pharmacodynamics

Nicardipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nicardipine is similar to other peripheral vasodilators. Nicardipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Mechanism of action

By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

TargetActionsOrganism
AVoltage-dependent L-type calcium channel subunit alpha-1C
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit beta-2
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1D
inhibitor
Human
AVoltage-dependent calcium channel subunit alpha-2/delta-1
inhibitor
Human
UCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A
inhibitor
Human
UCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B
inhibitor
Human
UAlpha-1A adrenergic receptor
antagonist
Human
UAlpha-1B adrenergic receptor
antagonist
Human
UAlpha-1D adrenergic receptor
antagonist
Human
UMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M3
antagonist
Human
UMuscarinic acetylcholine receptor M4
antagonist
Human
UMuscarinic acetylcholine receptor M5
antagonist
Human
UCalmodulin
other/unknown
Human
Absorption

While nicardipine is completely absorbed, it is subject to saturable first pass metabolism and the systemic bioavailability is about 35% following a 30 mg oral dose at steady state.

Volume of distribution
  • 8.3 L/kg
Protein binding

>95%

Metabolism

Nicardipine HCl is metabolized extensively by the liver.

Route of elimination

Nicardipine has been shown to be rapidly and extensively metabolized by the liver.

Half life

8.6 hours

Clearance
  • 0.4 L/hr∙kg [Following infusion]
Toxicity

Oral LD50 Rat = 184 mg/kg, Oral LD50 Mouse = 322 mg/kg

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

Interactions

Drug Interactions
DrugInteraction
(2-benzhydryloxyethyl)diethyl-methylammonium iodideThe risk or severity of adverse effects can be increased when Nicardipine is combined with (2-benzhydryloxyethyl)diethyl-methylammonium iodide.
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Nicardipine.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Nicardipine.
1,10-PhenanthrolineThe therapeutic efficacy of Nicardipine can be decreased when used in combination with 1,10-Phenanthroline.
16-BromoepiandrosteroneThe metabolism of 16-Bromoepiandrosterone can be decreased when combined with Nicardipine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Nicardipine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Nicardipine.
4-MethoxyamphetamineThe therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Nicardipine.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Nicardipine.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Nicardipine.
Food Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment. Grapefruit can increase serum levels of this product.
  • Take without regard to meals.

References

Synthesis Reference

Takashi Sonobe, Hiroitsu Kawata, Masayoshi Aruga, Tadayoshi Ohmura, Satoru Yoneya, Chiharu Yamada, Yukio Kubota, "Composition for long acting nicardipine preparation and process of producing the composition." U.S. Patent US4758437, issued March, 1979.

US4758437
General References
Not Available
External Links
Human Metabolome Database
HMDB0014760
KEGG Compound
C07264
PubChem Compound
4474
PubChem Substance
46504482
ChemSpider
4319
BindingDB
50017085
ChEBI
7550
ChEMBL
CHEMBL1484
Therapeutic Targets Database
DAP000486
PharmGKB
PA450620
IUPHAR
2559
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Nicardipine
ATC Codes
C08CA04 — Nicardipine
FDA label
Download (1.26 MB)
MSDS
Download (106 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentCoronary Artery Disease1
1CompletedTreatmentHigh Blood Pressure (Hypertension) / Intracerebral Hemorrhage / Strokes1
1CompletedTreatmentNeoplasms, Brain1
1RecruitingBasic ScienceCardiovascular System Disease / Drug-Related Side Effects and Adverse Reactions1
2TerminatedTreatmentAortic Aneurysm, Thoracic1
2TerminatedTreatmentCerebral Vasospasm1
2WithdrawnTreatmentHigh Blood Pressure (Hypertension)1
3CompletedTreatmentHeart Failure, Unspecified / High Blood Pressure (Hypertension)1
3CompletedTreatmentHigh Blood Pressure (Hypertension)1
3RecruitingPreventionOcclusion of Artery / Radial Artery Injury at Wrist and Hand Level / Vasodilation1
3RecruitingTreatmentHigh Blood Pressure (Hypertension) / Preeclampsia1
3TerminatedTreatmentIntracerebral Hemorrhage1
3Unknown StatusTreatmentHypertension During Pre-Eclampsia1
4CompletedPreventionSpinal Stenosis1
4CompletedTreatmentEnd-organ Damage / Hypertension Emergency1
4CompletedTreatmentHypertensive Urgency1
4RecruitingHealth Services ResearchCerebral Vasospasm1
4Unknown StatusTreatmentAcute Coronary Syndromes (ACS) / Coronary Artery Disease1
4Unknown StatusTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableCompletedNot AvailableIntracerebral Hemorrhage / Subarachnoid Hemorrhage1
Not AvailableCompletedPreventionHealthy Volunteers1
Not AvailableCompletedTreatmentCVA (Cerebrovascular Accident) / Intracerebral Hemorrhage / Intracranial Hemorrhages1
Not AvailableRecruitingNot AvailableAcute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cyanide Poisoning / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / Gynaecological infection / Headaches / Herpes Simplex Virus / High Blood Cholesterol Level / High Blood Pressure (Hypertension) / Hospital-acquired bacterial pneumonia / Hyperlipidemias / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombosis / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal1
Not AvailableRecruitingDiagnosticGeneral Surgery1
Not AvailableRecruitingTreatmentScheduled Laparoscopic Surgery1
Not AvailableUnknown StatusPreventionIntubation, Endotracheal / Patients Who Are Intubated for General Anesthesia1

Pharmacoeconomics

Manufacturers
  • Ekr therapeutics inc
  • Amneal pharmaceutical
  • Barr laboratories inc
  • Mylan pharmaceuticals inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Bedford laboratories div ben venue laboratories inc
  • Bioniche pharma usa llc
  • Exela pharma sciences
  • Navinta llc
  • Pharmaforce inc
  • Sun pharma global inc
  • Wockhardt ltd
Packagers
  • Amneal Pharmaceuticals
  • Barr Pharmaceuticals
  • Baxter International Inc.
  • Berk Pharmaceuticals
  • Chelsea Laboratories Inc.
  • EKR Therapeutics Inc.
  • Emcure Pharmaceuticals Ltd.
  • Genpharm LP
  • Ivax Pharmaceuticals
  • Kaiser Foundation Hospital
  • Legacy Pharmaceuticals Packaging LLC
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • PDL BioPharma Inc.
  • Pharmaforce Inc.
  • Physicians Total Care Inc.
  • Sandoz
  • Sun Pharmaceutical Industries Ltd.
  • Teva Pharmaceutical Industries Ltd.
  • Wockhardt Ltd.
Dosage forms
FormRouteStrength
Capsule, extended releaseOral30 mg/1
Capsule, extended releaseOral45 mg/1
Capsule, extended releaseOral60 mg/1
Capsule, gelatin coatedOral20 mg/1
Capsule, gelatin coatedOral30 mg/1
InjectionIntravenous2.5 mg/1mL
CapsuleOral20 mg
CapsuleOral30 mg
Injection, solutionIntravenous0.1 mg/1mL
Capsule, gelatin coatedOral45 mg/1
Capsule, gelatin coatedOral60 mg/1
Injection, solutionIntravenous0.2 mg/1mL
CapsuleOral20 mg/1
CapsuleOral30 mg/1
InjectionIntravenous25 mg/10mL
Injection, solutionIntravenous2.5 mg/1mL
Prices
Unit descriptionCostUnit
Cardene SR 60 60 mg 12 Hour Capsule Bottle142.91USD bottle
Nicardipine 25 mg/10 ml ampule25.01USD ml
Nicardipine 25 mg/10 ml vial10.42USD ml
Cardene SR 45 mg 12 Hour Capsule3.22USD capsule
Cardene sr 45 mg capsule2.9USD capsule
Cardene sr 60 mg capsule sa2.29USD capsule
Cardene SR 30 mg 12 Hour Capsule2.02USD capsule
Cardene sr 45 mg capsule sa1.91USD capsule
Cardene-dex 40 mg/200 ml iv1.35USD ml
Cardene-nacl 40 mg/200 ml iv1.35USD ml
Cardene 30 mg capsule1.28USD capsule
Cardene sr 30 mg capsule sa1.21USD capsule
Cardene sr 30 mg capsule0.87USD capsule
Cardene 20 mg capsule0.8USD capsule
NiCARdipine HCl 30 mg capsule0.68USD capsule
Cardene-dex 20 mg/200 ml soln0.67USD ml
Cardene-nacl 20 mg/200 ml soln0.67USD ml
Nicardipine 30 mg capsule0.66USD capsule
NiCARdipine HCl 20 mg capsule0.48USD capsule
Nicardipine 20 mg capsule0.46USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5164405No1992-11-172009-11-17Us
US7659291No2007-04-182027-04-18Us
US8455524No2007-04-182027-04-18Us
US7612102No2007-12-262027-12-26Us
US9364564No2007-12-262027-12-26Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)136-138 °CPhysProp
water solubility2.2 mg/LNot Available
logP3.82SANGSTER (1993)
Predicted Properties
PropertyValueSource
Water Solubility0.00247 mg/mLALOGPS
logP4.34ALOGPS
logP3.56ChemAxon
logS-5.3ALOGPS
pKa (Strongest Basic)8.18ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area113.69 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity134.8 m3·mol-1ChemAxon
Polarizability49.95 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.932
Blood Brain Barrier-0.9549
Caco-2 permeable-0.83
P-glycoprotein substrateSubstrate0.8581
P-glycoprotein inhibitor IInhibitor0.9036
P-glycoprotein inhibitor IIInhibitor0.8253
Renal organic cation transporterNon-inhibitor0.7502
CYP450 2C9 substrateNon-substrate0.8296
CYP450 2D6 substrateNon-substrate0.5554
CYP450 3A4 substrateSubstrate0.7228
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorInhibitor0.8948
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorInhibitor0.7959
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8558
Ames testNon AMES toxic0.562
CarcinogenicityNon-carcinogens0.7262
BiodegradationNot ready biodegradable0.9604
Rat acute toxicity2.9030 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.7332
hERG inhibition (predictor II)Non-inhibitor0.7316
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 dihydropyridinecarboxylic acids and derivatives. These are compounds containing a dihydropyridine moiety bearing a carboxylic acid group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyridines and derivatives
Sub Class
Hydropyridines
Direct Parent
Dihydropyridinecarboxylic acids and derivatives
Alternative Parents
Nitrobenzenes / Phenylmethylamines / Benzylamines / Nitroaromatic compounds / Aralkylamines / Dicarboxylic acids and derivatives / Vinylogous amides / Enoate esters / Methyl esters / Trialkylamines
show 11 more
Substituents
Dihydropyridinecarboxylic acid derivative / Nitrobenzene / Nitroaromatic compound / Benzylamine / Phenylmethylamine / Aralkylamine / Monocyclic benzene moiety / Dicarboxylic acid or derivatives / Benzenoid / Methyl ester
show 29 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
dihydropyridine (CHEBI:7550)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1C
Uniprot ID
Q13936
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1C
Molecular Weight
248974.1 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
Gene Name
CACNB2
Uniprot ID
Q08289
Uniprot Name
Voltage-dependent L-type calcium channel subunit beta-2
Molecular Weight
73579.925 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity involved sa node cell action potential
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1D
Uniprot ID
Q01668
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1D
Molecular Weight
245138.75 Da
References
  1. Bell DC, Butcher AJ, Berrow NS, Page KM, Brust PF, Nesterova A, Stauderman KA, Seabrook GR, Nurnberg B, Dolphin AC: Biophysical properties, pharmacology, and modulation of human, neuronal L-type (alpha(1D), Ca(V)1.3) voltage-dependent calcium currents. J Neurophysiol. 2001 Feb;85(2):816-27. [PubMed:11160515]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The alpha-2/delta subunit of voltage-dependent calcium channels regulates calcium current density and activation/inactivation kinetics of the calcium channel. Plays an important role in excitation-...
Gene Name
CACNA2D1
Uniprot ID
P54289
Uniprot Name
Voltage-dependent calcium channel subunit alpha-2/delta-1
Molecular Weight
124566.93 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes. Has a higher affinity for cG...
Gene Name
PDE1A
Uniprot ID
P54750
Uniprot Name
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A
Molecular Weight
61251.38 Da
References
  1. Sharma RK, Wang JH, Wu Z: Mechanisms of inhibition of calmodulin-stimulated cyclic nucleotide phosphodiesterase by dihydropyridine calcium antagonists. J Neurochem. 1997 Aug;69(2):845-50. [PubMed:9231746]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes. Has a preference for cGMP as...
Gene Name
PDE1B
Uniprot ID
Q01064
Uniprot Name
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B
Molecular Weight
61379.235 Da
References
  1. Sharma RK, Wang JH, Wu Z: Mechanisms of inhibition of calmodulin-stimulated cyclic nucleotide phosphodiesterase by dihydropyridine calcium antagonists. J Neurochem. 1997 Aug;69(2):845-50. [PubMed:9231746]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Alpha1-adrenergic receptor activity
Specific Function
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name
ADRA1D
Uniprot ID
P25100
Uniprot Name
Alpha-1D adrenergic receptor
Molecular Weight
60462.205 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Titin binding
Specific Function
Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number...
Gene Name
CALM1
Uniprot ID
P0DP23
Uniprot Name
Calmodulin
Molecular Weight
16837.47 Da
References
  1. Thayer SA, Fairhurst AS: The interaction of dihydropyridine calcium channel blockers with calmodulin and calmodulin inhibitors. Mol Pharmacol. 1983 Jul;24(1):6-9. [PubMed:6865927]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. Nakamura K, Ariyoshi N, Iwatsubo T, Fukunaga Y, Higuchi S, Itoh K, Shimada N, Nagashima K, Yokoi T, Yamamoto K, Horiuchi R, Kamataki T: Inhibitory effects of nicardipine to cytochrome P450 (CYP) in human liver microsomes. Biol Pharm Bull. 2005 May;28(5):882-5. [PubMed:15863898]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 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]
Details
3. Cytochrome P450 2C9
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Drocourt L, Pascussi JM, Assenat E, Fabre JM, Maurel P, Vilarem MJ: Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes. Drug Metab Dispos. 2001 Oct;29(10):1325-31. [PubMed:11560876]
  2. Katoh M, Nakajima M, Shimada N, Yamazaki H, Yokoi T: Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):843-52. [PubMed:10805063]
  3. Ma B, Prueksaritanont T, Lin JH: Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30. [PubMed:10640508]
  4. Hanatani T, Fukuda T, Onishi S, Funae Y, Azuma J: No major difference in inhibitory susceptibility between CYP2C9.1 and CYP2C9.3. Eur J Clin Pharmacol. 2003 Jul;59(3):233-5. doi: 10.1007/s00228-003-0603-5. Epub 2003 May 17. [PubMed:12756514]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 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]
  2. Katoh M, Nakajima M, Shimada N, Yamazaki H, Yokoi T: Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):843-52. [PubMed:10805063]
  3. Nakamura K, Ariyoshi N, Iwatsubo T, Fukunaga Y, Higuchi S, Itoh K, Shimada N, Nagashima K, Yokoi T, Yamamoto K, Horiuchi R, Kamataki T: Inhibitory effects of nicardipine to cytochrome P450 (CYP) in human liver microsomes. Biol Pharm Bull. 2005 May;28(5):882-5. [PubMed:15863898]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
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]
  2. Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [PubMed:26721703]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inducer
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 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
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 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
Inhibitor
General Function
Oxygen binding
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 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]
  2. McConn DJ 2nd, Lin YS, Allen K, Kunze KL, Thummel KE: Differences in the inhibition of cytochromes P450 3A4 and 3A5 by metabolite-inhibitor complex-forming drugs. Drug Metab Dispos. 2004 Oct;32(10):1083-91. doi: 10.1124/dmd.32.10.. [PubMed:15377640]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Katoh M, Nakajima M, Yamazaki H, Yokoi T: Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4. Pharm Res. 2000 Oct;17(10):1189-97. [PubMed:11145223]
  2. Lentz KA, Polli JW, Wring SA, Humphreys JE, Polli JE: Influence of passive permeability on apparent P-glycoprotein kinetics. Pharm Res. 2000 Dec;17(12):1456-60. [PubMed:11303953]
  3. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514]
  4. Takara K, Sakaeda T, Tanigawara Y, Nishiguchi K, Ohmoto N, Horinouchi M, Komada F, Ohnishi N, Yokoyama T, Okumura K: Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression. Eur J Pharm Sci. 2002 Aug;16(3):159-65. [PubMed:12128170]
  5. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389]
  6. Ibrahim S, Peggins J, Knapton A, Licht T, Aszalos A: Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation. J Pharmacol Exp Ther. 2000 Dec;295(3):1276-83. [PubMed:11082465]
  7. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Karlgren M, Ahlin G, Bergstrom CA, Svensson R, Palm J, Artursson P: In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions. Pharm Res. 2012 Feb;29(2):411-26. doi: 10.1007/s11095-011-0564-9. Epub 2011 Aug 23. [PubMed:21861202]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]

Drug created on June 13, 2005 07:24 / Updated on September 17, 2018 20:43