Identification

Name
Isradipine
Accession Number
DB00270  (APRD00298)
Type
Small Molecule
Groups
Approved, Investigational
Description

Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. It is structurally related to felodipine, nifedipine, and nimodipine and is the most potent calcium-channel blocking agent of the DHP class. Isradipine binds to calcium channels with high affinity and specificity and inhibits calcium flux into cardiac and arterial smooth muscle cells. It exhibits greater selectivity towards arterial smooth muscle cells owing to alternative splicing of the alpha-1 subunit of the channel and increased prevalence of inactive channels in smooth muscle cells. Isradipine may be used to treat mild to moderate essential hypertension.

Structure
Thumb
Synonyms
  • Isradipino
  • Isradipinum
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DynaCircCapsule5 mg/1OralGlaxosmithkline Inc2007-03-012010-01-01Us
DynaCircTablet, film coated, extended release5 mg/1OralGlaxosmithkline Inc2007-03-012011-10-31Us
DynaCircCapsule5 mg/1OralPhysicians Total Care, Inc.1998-12-012011-05-31Us
DynaCircCapsule2.5 mg/1OralGlaxosmithkline Inc2007-03-012010-01-01Us
DynaCircCapsule2.5 mg/1OralPhysicians Total Care, Inc.1999-03-042011-05-31Us
DynaCircTablet, film coated, extended release10 mg/1OralGlaxosmithkline Inc2007-03-012011-09-30Us
Dynacirc CRTablet, film coated, extended release10 mg/1OralGlaxosmithkline Inc2010-01-042013-10-31Us0173 078520180907 15195 1i271ph
Dynacirc CRTablet, film coated, extended release5 mg/1OralGlaxosmithkline Inc2010-01-042013-09-30Us0173 078420180907 15195 1dr97bi
Dynacirc CRTablet, film coated, extended release5 mg/1OralPhysicians Total Care, Inc.2005-11-222012-07-06Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
IsradipineCapsule2.5 mg/1OralEpic Pharma, LLC2014-05-15Not applicableUs
IsradipineCapsule2.5 mg/1OralActavis Totowa LLC2006-09-012008-08-20Us
IsradipineCapsule5 mg/1OralAv Pak2014-01-06Not applicableUs
IsradipineCapsule2.5 mg/1OralActavis Pharma Company2004-01-05Not applicableUs
IsradipineCapsule5 mg/1OralCarilion Materials Management2006-01-05Not applicableUs
IsradipineCapsule5 mg/1OralGolden State Medical Supply, Inc.2015-05-06Not applicableUs
IsradipineCapsule2.5 mg/1OralAv Pak2014-01-06Not applicableUs
IsradipineCapsule5 mg/1OralEpic Pharma, LLC2014-05-15Not applicableUs
IsradipineCapsule5 mg/1OralActavis Totowa LLC2006-09-012008-08-20Us
IsradipineCapsule2.5 mg/1OralGolden State Medical Supply, Inc.2015-05-06Not applicableUs
International/Other Brands
Clivoten (Italfarmaco (Italy)) / DynaCirc (Novartis (Hong Kong, Malaysia, Mexico, New Zealand, South Africa, Singapore, Thailand, Turkey, United States)) / Dynacirc CR (Reliant, GlaxoSmithKline) / Esradin (Sigma-Tau (Italy)) / Lomir (Novartis (Austria, Brazil, Czech Republic, Denmark, Finland, Germany, Greece, Hungary, Netherlands, Norway, Poland, Russia, Sweden), Sankyo (Belgium, Italy), Daiichi Sankyo (Portugal, Switzerland), Mizar (Spain)) / Prescal (Novartis (United Kingdom))
Categories
UNII
YO1UK1S598
CAS number
75695-93-1
Weight
Average: 371.3871
Monoisotopic: 371.148120797
Chemical Formula
C19H21N3O5
InChI Key
HMJIYCCIJYRONP-UHFFFAOYSA-N
InChI
InChI=1S/C19H21N3O5/c1-9(2)26-19(24)15-11(4)20-10(3)14(18(23)25-5)16(15)12-7-6-8-13-17(12)22-27-21-13/h6-9,16,20H,1-5H3
IUPAC Name
3-methyl 5-propan-2-yl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
SMILES
COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC2=NON=C12)C(=O)OC(C)C

Pharmacology

Indication

For the management of mild to moderate essential hypertension. It may be used alone or concurrently with thiazide-type diuretics.

Associated Conditions
Pharmacodynamics

Isradipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. Calcium ions entering the cell through these channels bind to calmodulin. Calcium-bound calmodulin then binds to and activates myosin light chain kinase (MLCK). Activated MLCK catalyzes the phosphorylation of the regulatory light chain subunit of myosin, a key step in muscle contraction. Signal amplification is achieved by calcium-induced calcium release from the sarcoplasmic reticulum through ryanodine receptors. Inhibition of the initial influx of calcium decreases the contractile activity of arterial smooth muscle cells and results in vasodilation. The vasodilatory effects of isradipine result in an overall decrease in blood pressure.

Mechanism of action

Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. CCBs target L-type calcium channels, the major channel in muscle cells that mediates contraction. Similar to other DHP CCBs, isradipine binds directly to inactive calcium channels stabilizing their inactive conformation. Since arterial smooth muscle depolarizations are longer in duration than cardiac muscle depolarizations, inactive channels are more prevalent in smooth muscle cells. Alternative splicing of the alpha-1 subunit of the channel gives isradipine additional arterial selectivity. At therapeutic sub-toxic concentrations, isradipine has little effect on cardiac myocytes and conduction cells.

TargetActionsOrganism
AVoltage-dependent L-type calcium channel subunit alpha-1C
inhibitor
Human
AVoltage-dependent calcium channel subunit alpha-2/delta-1
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit beta-2
inhibitor
Human
AVoltage-dependent T-type calcium channel subunit alpha-1H
inhibitor
Human
AVoltage-dependent calcium channel subunit alpha-2/delta-2
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1D
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1S
inhibitor
Human
Absorption

Isradipine is 90%-95% absorbed and is subject to extensive first-pass metabolism, resulting in a bioavailability of about 15%-24%.

Volume of distribution
Not Available
Protein binding

95%

Metabolism

Hepatic. Completely metabolized prior to excretion and no unchanged drug is detected in the urine.

Route of elimination

Approximately 60% to 65% of an administered dose is excreted in the urine and 25% to 30% in the feces.

Half life

8 hours

Clearance
Not Available
Toxicity

Symptoms of overdose include lethargy, sinus tachycardia, and transient hypotension. Significant lethality was observed in mice given oral doses of over 200 mg/kg and rabbits given about 50 mg/kg of isradipine. Rats tolerated doses of over 2000 mg/kg without effects on survival.

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

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Isradipine.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Isradipine.
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Isradipine is combined with 2,4-thiazolidinedione.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Isradipine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Isradipine.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Isradipine.
6-Deoxyerythronolide BThe metabolism of Isradipine can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Isradipine.
AbacavirIsradipine may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbafunginThe therapeutic efficacy of Abafungin can be increased when used in combination with Isradipine.
Food Interactions
Not Available

References

General References
  1. Fletcher H, Roberts G, Mullings A, Forrester T: An open trial comparing isradipine with hydralazine and methyl dopa in the treatment of patients with severe pre-eclampsia. J Obstet Gynaecol. 1999 May;19(3):235-8. [PubMed:15512286]
  2. Ganz M, Mokabberi R, Sica DA: Comparison of blood pressure control with amlodipine and controlled-release isradipine: an open-label, drug substitution study. J Clin Hypertens (Greenwich). 2005 Apr;7(4 Suppl 1):27-31. [PubMed:15858400]
  3. Hattori T, Wang PL: Calcium antagonist isradipine-induced calcium influx through nonselective cation channels in human gingival fibroblasts. Eur J Med Res. 2006 Mar 27;11(3):93-6. [PubMed:16751108]
  4. Johnson BA, Roache JD, Ait-Daoud N, Wallace C, Wells L, Dawes M, Wang Y: Effects of isradipine, a dihydropyridine-class calcium-channel antagonist, on d-methamphetamine's subjective and reinforcing effects. Int J Neuropsychopharmacol. 2005 Jun;8(2):203-13. [PubMed:15850499]
External Links
Human Metabolome Database
HMDB0014415
KEGG Drug
D00349
PubChem Compound
3784
PubChem Substance
46505034
ChemSpider
3652
BindingDB
50436176
ChEBI
6073
ChEMBL
CHEMBL1648
Therapeutic Targets Database
DAP000134
PharmGKB
PA450131
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Isradipine
ATC Codes
C08CA03 — Isradipine
MSDS
Download (57.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0SuspendedTreatmentNicotine Dependence1
1CompletedNot AvailableSubstance, Addiction1
1, 2CompletedTreatmentOpioid Dependence1
2CompletedTreatmentParkinson's Disease (PD)2
2TerminatedTreatmentBipolar Disorder (BD)1
2, 3CompletedPreventionHypertension Secondary to Kidney Transplant1
3Active Not RecruitingTreatmentParkinson's Disease (PD)1
Not AvailableCompletedSupportive CareSchizoaffective Disorders / Schizophrenic Disorders1
Not AvailableUnknown StatusBasic ScienceSpinal Cord Injury, Chronic1

Pharmacoeconomics

Manufacturers
  • Smithkline beecham corp dba glaxosmithkline
  • Actavis totowa llc
  • Watson laboratories inc
  • Glaxosmithkline llc
Packagers
  • Actavis Group
  • Alza Corp.
  • Amerisource Health Services Corp.
  • Caremark LLC
  • Cobalt Pharmaceuticals Inc.
  • GlaxoSmithKline Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Novartis AG
  • Patheon Inc.
  • Pharmaceutical Manufacturing Research Services Inc.
  • Physicians Total Care Inc.
  • Watson Pharmaceuticals
Dosage forms
FormRouteStrength
CapsuleOral2.5 mg/1
CapsuleOral5 mg/1
Tablet, film coated, extended releaseOral10 mg/1
Tablet, film coated, extended releaseOral5 mg/1
Prices
Unit descriptionCostUnit
DynaCirc CR 10 mg 24 Hour tablet5.59USD tablet
Dynacirc cr 10 mg tablet4.41USD tablet
DynaCirc CR 5 mg 24 Hour tablet3.0USD tablet
Dynacirc cr 5 mg tablet2.88USD tablet
DynaCirc 5 mg capsule2.31USD capsule
Isradipine 5 mg capsule2.0USD capsule
DynaCirc 2.5 mg capsule1.59USD capsule
Isradipine 2.5 mg capsule1.39USD capsule
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)168-170 °CNot Available
water solubilityPractically insoluble (< 10 mg/L at 37 °C)Not Available
logP4.28SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.228 mg/mLALOGPS
logP3ALOGPS
logP2ChemAxon
logS-3.2ALOGPS
pKa (Strongest Basic)5.33ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area103.55 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity100.08 m3·mol-1ChemAxon
Polarizability37.39 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9965
Blood Brain Barrier-0.8439
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.5855
P-glycoprotein inhibitor IInhibitor0.9322
P-glycoprotein inhibitor IIInhibitor0.8669
Renal organic cation transporterNon-inhibitor0.884
CYP450 2C9 substrateNon-substrate0.8522
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6631
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorInhibitor0.8949
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8557
Ames testNon AMES toxic0.5158
CarcinogenicityNon-carcinogens0.8043
BiodegradationNot ready biodegradable0.9747
Rat acute toxicity2.3960 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8699
hERG inhibition (predictor II)Non-inhibitor0.6895
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/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-0009000000-3c8fe8c9d5e94c018299
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03dl-2589000000-e01ef029445c948c93e7

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzoxadiazoles. These are organic compounds containing a benzene fused to an oxadiazole ring (a five-membered ring with two carbon atoms, one nitrogen atom, and one oxygen atom).
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzoxadiazoles
Sub Class
Not Available
Direct Parent
Benzoxadiazoles
Alternative Parents
Dihydropyridinecarboxylic acids and derivatives / Benzenoids / Dicarboxylic acids and derivatives / Vinylogous amides / Enoate esters / Furazans / Heteroaromatic compounds / Methyl esters / Amino acids and derivatives / Enamines
show 6 more
Substituents
Benzoxadiazole / Dihydropyridinecarboxylic acid derivative / Dihydropyridine / Dicarboxylic acid or derivatives / Benzenoid / Hydropyridine / Azole / Heteroaromatic compound / Furazan / Vinylogous amide
show 21 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

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. Berjukow S, Marksteiner R, Gapp F, Sinnegger MJ, Hering S: Molecular mechanism of calcium channel block by isradipine. Role of a drug-induced inactivated channel conformation. J Biol Chem. 2000 Jul 21;275(29):22114-20. [PubMed:10766758]
  2. Hitzl M, Striessnig J, Neuhuber B, Flucher BE: A mutation in the beta interaction domain of the Ca(2+) channel alpha(1C) subunit reduces the affinity of the (+)-[(3)H]isradipine binding site. FEBS Lett. 2002 Jul 31;524(1-3):188-92. [PubMed:12135765]
  3. Zuhlke RD, Bouron A, Soldatov NM, Reuter H: Ca2+ channel sensitivity towards the blocker isradipine is affected by alternative splicing of the human alpha1C subunit gene. FEBS Lett. 1998 May 8;427(2):220-4. [PubMed:9607315]
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. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  3. 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
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
Scaffold protein binding
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
CACNA1H
Uniprot ID
O95180
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1H
Molecular Weight
259160.2 Da
References
  1. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221]
  2. Perez-Reyes E, Van Deusen AL, Vitko I: Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs. J Pharmacol Exp Ther. 2009 Feb;328(2):621-7. doi: 10.1124/jpet.108.145672. Epub 2008 Oct 30. [PubMed:18974361]
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. Acts as a regulatory subunit for P/Q-t...
Gene Name
CACNA2D2
Uniprot ID
Q9NY47
Uniprot Name
Voltage-dependent calcium channel subunit alpha-2/delta-2
Molecular Weight
129816.095 Da
References
  1. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221]
  2. Perez-Reyes E, Van Deusen AL, Vitko I: Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs. J Pharmacol Exp Ther. 2009 Feb;328(2):621-7. doi: 10.1124/jpet.108.145672. Epub 2008 Oct 30. [PubMed:18974361]
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. Koschak A, Reimer D, Huber I, Grabner M, Glossmann H, Engel J, Striessnig J: alpha 1D (Cav1.3) subunits can form l-type Ca2+ channels activating at negative voltages. J Biol Chem. 2001 Jun 22;276(25):22100-6. Epub 2001 Apr 2. [PubMed:11285265]
  2. Sinnegger-Brauns MJ, Huber IG, Koschak A, Wild C, Obermair GJ, Einzinger U, Hoda JC, Sartori SB, Striessnig J: Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms. Mol Pharmacol. 2009 Feb;75(2):407-14. doi: 10.1124/mol.108.049981. Epub 2008 Nov 24. [PubMed:19029287]
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
CACNA1S
Uniprot ID
Q13698
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1S
Molecular Weight
212348.1 Da
References
  1. Peterson BZ, Catterall WA: Allosteric interactions required for high-affinity binding of dihydropyridine antagonists to Ca(V)1.1 Channels are modulated by calcium in the pore. Mol Pharmacol. 2006 Aug;70(2):667-75. Epub 2006 May 4. [PubMed:16675661]

Enzymes

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. Michalets EL: Update: clinically significant cytochrome P-450 drug interactions. Pharmacotherapy. 1998 Jan-Feb;18(1):84-112. [PubMed:9469685]
  2. Get to Know an Enzyme: CYP3A4 Substrates [Link]

Transporters

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 November 02, 2018 04:40