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Identification
NameIsradipine
Accession NumberDB00270  (APRD00298)
TypeSmall Molecule
GroupsApproved
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
Dynacirc
Isradipino
Isradipinum
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Isradipinecapsule2.5 mg/1oralActavis Pharma, Inc.2004-01-05Not applicableUs
Isradipinecapsule2.5 mg/1oralGolden State Medical Supply, Inc.2015-05-06Not applicableUs
Isradipinecapsule5 mg/1oralAv Pak2014-01-06Not applicableUs
Isradipinecapsule2.5 mg/1oralAv Pak2014-01-06Not applicableUs
Isradipinecapsule5 mg/1oralEpic Pharma, LLC2014-05-15Not applicableUs
Isradipinecapsule2.5 mg/1oralEpic Pharma, LLC2014-05-15Not applicableUs
Isradipinecapsule5 mg/1oralCarilion Materials Management2006-01-05Not applicableUs
Isradipinecapsule5 mg/1oralActavis Pharma, Inc.2006-01-05Not applicableUs
Isradipinecapsule5 mg/1oralGolden State Medical Supply, Inc.2015-05-06Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ClivotenItalfarmaco (Italy)
DynaCircNovartis (Hong Kong, Malaysia, Mexico, New Zealand, South Africa, Singapore, Thailand, Turkey, United States)
Dynacirc CRReliant, GlaxoSmithKline
EsradinSigma-Tau (Italy)
LomirNovartis (Austria, Brazil, Czech Republic, Denmark, Finland, Germany, Greece, Hungary, Netherlands, Norway, Poland, Russia, Sweden), Sankyo (Belgium, Italy), Daiichi Sankyo (Portugal, Switzerland), Mizar (Spain)
PrescalNovartis (United Kingdom)
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIYO1UK1S598
CAS number75695-93-1
WeightAverage: 371.3871
Monoisotopic: 371.148120797
Chemical FormulaC19H21N3O5
InChI KeyInChIKey=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
Taxonomy
DescriptionThis 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).
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzoxadiazoles
Sub ClassNot Available
Direct ParentBenzoxadiazoles
Alternative Parents
Substituents
  • Dihydropyridinecarboxylic acid derivative
  • Benzoxadiazole
  • Dihydropyridine
  • Benzenoid
  • Hydropyridine
  • Dicarboxylic acid or derivatives
  • Heteroaromatic compound
  • Vinylogous amide
  • Alpha,beta-unsaturated carboxylic ester
  • Enoate ester
  • Methyl ester
  • Oxadiazole
  • Furazan
  • Azole
  • Carboxylic acid ester
  • Oxacycle
  • Azacycle
  • Enamine
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the management of mild to moderate essential hypertension. It may be used alone or concurrently with thiazide-type diuretics.
PharmacodynamicsIsradipine 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 actionIsradipine 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.
Related Articles
AbsorptionIsradipine is 90%-95% absorbed and is subject to extensive first-pass metabolism, resulting in a bioavailability of about 15%-24%.
Volume of distributionNot Available
Protein binding95%
Metabolism

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

Route of eliminationApproximately 60% to 65% of an administered dose is excreted in the urine and 25% to 30% in the feces.
Half life8 hours
ClearanceNot Available
ToxicitySymptoms 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
PathwayCategorySMPDB ID
Isradipine Action PathwayDrug actionSMP00378
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
Manufacturers
  • Smithkline beecham corp dba glaxosmithkline
  • Actavis totowa llc
  • Watson laboratories inc
  • Glaxosmithkline llc
Packagers
Dosage forms
FormRouteStrength
Capsuleoral2.5 mg/1
Capsuleoral5 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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point168-170 °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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
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
ATC CodesC08CA03
AHFS Codes
  • 24:28.08
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (57.4 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe metabolism of Isradipine can be increased when combined with Acetaminophen.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Isradipine.
AlfuzosinAlfuzosin may increase the hypotensive activities of Isradipine.
AmifostineIsradipine may increase the hypotensive activities of Amifostine.
AmobarbitalThe metabolism of Isradipine can be increased when combined with Amobarbital.
AprepitantThe serum concentration of Isradipine can be increased when it is combined with Aprepitant.
AtosibanThe risk or severity of adverse effects can be increased when Isradipine is combined with Atosiban.
Atracurium besylateIsradipine may increase the neuromuscular blocking activities of Atracurium besylate.
BepridilIsradipine may increase the hypotensive activities of Bepridil.
BexaroteneThe serum concentration of Isradipine can be decreased when it is combined with Bexarotene.
BosentanThe serum concentration of Isradipine can be decreased when it is combined with Bosentan.
BrimonidineBrimonidine may increase the antihypertensive activities of Isradipine.
ButabarbitalThe metabolism of Isradipine can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Isradipine can be increased when combined with Butalbital.
ButethalThe metabolism of Isradipine can be increased when combined with Butethal.
CaffeineThe metabolism of Isradipine can be increased when combined with Caffeine.
Calcium AcetateThe therapeutic efficacy of Isradipine can be decreased when used in combination with Calcium Acetate.
Calcium carbonateThe therapeutic efficacy of Isradipine can be decreased when used in combination with Calcium carbonate.
Calcium ChlorideThe therapeutic efficacy of Isradipine can be decreased when used in combination with Calcium Chloride.
Calcium citrateThe therapeutic efficacy of Isradipine can be decreased when used in combination with Calcium citrate.
Calcium gluconateThe therapeutic efficacy of Isradipine can be decreased when used in combination with Calcium gluconate.
CarbamazepineThe metabolism of Isradipine can be increased when combined with Carbamazepine.
CimetidineThe serum concentration of Isradipine can be increased when it is combined with Cimetidine.
Cisatracurium besylateIsradipine may increase the neuromuscular blocking activities of Cisatracurium besylate.
CitalopramIsradipine may increase the QTc-prolonging activities of Citalopram.
ClarithromycinThe metabolism of Isradipine can be decreased when combined with Clarithromycin.
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Isradipine.
ConivaptanThe serum concentration of Isradipine can be increased when it is combined with Conivaptan.
CyclosporineThe metabolism of Isradipine can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Isradipine can be decreased when it is combined with Dabrafenib.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Isradipine.
DasatinibThe serum concentration of Isradipine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Isradipine can be decreased when it is combined with Deferasirox.
DiazoxideDiazoxide may increase the hypotensive activities of Isradipine.
DofetilideIsradipine may increase the QTc-prolonging activities of Dofetilide.
DoxazosinDoxazosin may increase the hypotensive activities of Isradipine.
DuloxetineIsradipine may increase the orthostatic hypotensive activities of Duloxetine.
EfavirenzThe serum concentration of Isradipine can be decreased when it is combined with Efavirenz.
ErythromycinThe metabolism of Isradipine can be decreased when combined with Erythromycin.
FluconazoleThe serum concentration of Isradipine can be increased when it is combined with Fluconazole.
FosaprepitantThe serum concentration of Isradipine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Isradipine.
Fusidic AcidThe serum concentration of Isradipine can be increased when it is combined with Fusidic Acid.
GoserelinIsradipine may increase the QTc-prolonging activities of Goserelin.
HeptabarbitalThe metabolism of Isradipine can be increased when combined with Heptabarbital.
HexobarbitalThe metabolism of Isradipine can be increased when combined with Hexobarbital.
IdelalisibThe serum concentration of Isradipine can be increased when it is combined with Idelalisib.
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Isradipine.
IvacaftorThe serum concentration of Isradipine can be increased when it is combined with Ivacaftor.
KetoconazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Isradipine.
LeuprolideIsradipine may increase the QTc-prolonging activities of Leuprolide.
LevodopaIsradipine may increase the orthostatic hypotensive activities of Levodopa.
LuliconazoleThe serum concentration of Isradipine can be increased when it is combined with Luliconazole.
Magnesium chlorideThe risk or severity of adverse effects can be increased when Isradipine is combined with Magnesium chloride.
Magnesium citrateThe risk or severity of adverse effects can be increased when Isradipine is combined with Magnesium citrate.
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Isradipine is combined with Magnesium hydroxide.
Magnesium oxideThe risk or severity of adverse effects can be increased when Isradipine is combined with Magnesium oxide.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Isradipine is combined with Magnesium salicylate.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Isradipine is combined with Magnesium Sulfate.
MelatoninMelatonin may decrease the antihypertensive activities of Isradipine.
MethohexitalThe metabolism of Isradipine can be increased when combined with Methohexital.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Isradipine.
MifepristoneThe serum concentration of Isradipine can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Isradipine can be decreased when it is combined with Mitotane.
MolsidomineMolsidomine may increase the hypotensive activities of Isradipine.
MoxonidineMoxonidine may increase the hypotensive activities of Isradipine.
NafcillinThe metabolism of Isradipine can be increased when combined with Nafcillin.
NelfinavirThe metabolism of Isradipine can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Isradipine can be increased when it is combined with Netupitant.
NicorandilNicorandil may increase the hypotensive activities of Isradipine.
NitroprussideIsradipine may increase the hypotensive activities of Nitroprusside.
ObinutuzumabIsradipine may increase the hypotensive activities of Obinutuzumab.
PalbociclibThe serum concentration of Isradipine can be increased when it is combined with Palbociclib.
PancuroniumIsradipine may increase the neuromuscular blocking activities of Pancuronium.
PentobarbitalThe metabolism of Isradipine can be increased when combined with Pentobarbital.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Isradipine.
PhenelzinePhenelzine may increase the hypotensive activities of Isradipine.
PhenobarbitalThe metabolism of Isradipine can be increased when combined with Phenobarbital.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Isradipine.
PhentolaminePhentolamine may increase the hypotensive activities of Isradipine.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Isradipine.
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Isradipine.
PrazosinPrazosin may increase the hypotensive activities of Isradipine.
PrimidoneThe metabolism of Isradipine can be increased when combined with Primidone.
QuinineQuinine may increase the hypotensive activities of Isradipine.
RifabutinThe serum concentration of Isradipine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Isradipine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Isradipine can be decreased when it is combined with Rifapentine.
RisperidoneIsradipine may increase the hypotensive activities of Risperidone.
RituximabIsradipine may increase the hypotensive activities of Rituximab.
RocuroniumIsradipine may increase the neuromuscular blocking activities of Rocuronium.
SecobarbitalThe metabolism of Isradipine can be increased when combined with Secobarbital.
SilodosinSilodosin may increase the hypotensive activities of Isradipine.
SiltuximabThe serum concentration of Isradipine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Isradipine can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Isradipine can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe serum concentration of Isradipine can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Isradipine can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Isradipine.
TadalafilTadalafil may increase the antihypertensive activities of Isradipine.
TamsulosinTamsulosin may increase the hypotensive activities of Isradipine.
TelithromycinThe metabolism of Isradipine can be decreased when combined with Telithromycin.
TerazosinTerazosin may increase the hypotensive activities of Isradipine.
TocilizumabThe serum concentration of Isradipine can be decreased when it is combined with Tocilizumab.
TranylcypromineTranylcypromine may increase the hypotensive activities of Isradipine.
TreprostinilTreprostinil may increase the hypotensive activities of Isradipine.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Isradipine.
VardenafilVardenafil may increase the antihypertensive activities of Isradipine.
VecuroniumIsradipine may increase the neuromuscular blocking activities of Vecuronium.
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Isradipine.
YohimbineYohimbine may decrease the antihypertensive activities of Isradipine.
Food InteractionsNot 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, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1C gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1C
Uniprot ID:
Q13936
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-contraction coupling (By similarity).
Gene Name:
CACNA2D1
Uniprot ID:
P54289
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 inactivation, modulating G protein inhibition and controlling the alpha-1 subunit membrane targeting.
Gene Name:
CACNB2
Uniprot ID:
Q08289
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, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1H gives rise to T-type calcium currents. T-type calcium channels belong to the "low-v...
Gene Name:
CACNA1H
Uniprot ID:
O95180
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-type calcium channel (CACNA1A), N-type (CACNA1B), L-type (CACNA1C OR CACNA1D) and possibly T-type (CACNA1G). Overexpression induces apoptosis.
Gene Name:
CACNA2D2
Uniprot ID:
Q9NY47
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, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1D gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1D
Uniprot ID:
Q01668
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, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1S gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1S
Uniprot ID:
Q13698
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
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23