Identification

Name
Nisoldipine
Accession Number
DB00401  (APRD00635)
Type
Small Molecule
Groups
Approved
Description

Nisoldipine is a 1,4-dihydropyridine calcium channel blocker. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, nisoldipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction. Nisoldipine may be used in alone or in combination with other agents in the management of hypertension.

Structure
Thumb
Synonyms
  • isobutyl methyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
  • Nisoldipin
  • Nisoldipina
  • Nisoldipine
  • Nisoldipino
  • Nisoldipinum
External IDs
Bay K 5552
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SularTablet, film coated, extended release34 mg/1OralShionogi1995-02-02Not applicableUs59630 0503 10 nlmimage10 4f1627b1
SularTablet, film coated, extended release25.5 mg/1OralPhysicians Total Care, Inc.2009-02-24Not applicableUs
SularTablet, film coated, extended release17 mg/1OralCovis Pharma2017-02-03Not applicableUs
SularTablet, film coated, extended release17 mg/1OralShionogi1995-02-02Not applicableUs
SularTablet, film coated, extended release25.5 mg/1OralShionogi Pharma, Inc.1995-02-022010-06-01Us
SularTablet, film coated, extended release8.5 mg/1OralCovis Pharma2017-02-03Not applicableUs
SularTablet, film coated, extended release8.5 mg/1OralShionogi1995-02-02Not applicableUs
SularTablet, film coated, extended release34 mg/1OralCovis Pharma2017-02-03Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NisoldipineTablet, film coated, extended release34 mg/1OralUnited Research Laboratories, Inc.2009-09-01Not applicableUs
NisoldipineTablet, film coated, extended release25.5 mg/1OralMylan Pharmaceuticals2011-01-28Not applicableUs
NisoldipineTablet, film coated, extended release8.5 mg/1OralUnited Research Laboratories, Inc.2009-09-01Not applicableUs
NisoldipineTablet, film coated, extended release8.5 mg/1OralMylan Pharmaceuticals2011-01-28Not applicableUs
NisoldipineTablet, film coated, extended release8.5 mg/1OralPrasco, Laboratories2012-02-27Not applicableUs
NisoldipineTablet, film coated, extended release20 mg/1OralMylan Pharmaceuticals2008-07-25Not applicableUs
NisoldipineTablet, film coated, extended release25.5 mg/1OralUnited Research Laboratories, Inc.2009-09-01Not applicableUs
NisoldipineTablet, film coated, extended release34 mg/1OralPrasco, Laboratories2012-02-27Not applicableUs66993 0475 02 nlmimage10 814540ba
NisoldipineTablet, film coated, extended release40 mg/1OralMylan Pharmaceuticals2008-07-25Not applicableUs
NisoldipineTablet, film coated, extended release40 mg/1OralPhysicians Total Care, Inc.2008-08-29Not applicableUs
International/Other Brands
Baymycard (Bayer) / Baymycard RR (Bayer) / Bo Ping (Rui Yang Pharm) / Di Yi Xin (Tasly) / Ji Ni Le Er (Jiankang Pharmaceutical) / Ninobarucin (Choseido Pharmaceutical) / Nisomynard (Yoshindo) / Riohard (Taiyo Pharmaceutical) / Ruidi (Nanjing Sanrui Pharmaceutical Co.) / Sular / Syscor (Bayer)
Categories
UNII
4I8HAB65SZ
CAS number
63675-72-9
Weight
Average: 388.4144
Monoisotopic: 388.16343651
Chemical Formula
C20H24N2O6
InChI Key
VKQFCGNPDRICFG-UHFFFAOYSA-N
InChI
InChI=1S/C20H24N2O6/c1-11(2)10-28-20(24)17-13(4)21-12(3)16(19(23)27-5)18(17)14-8-6-7-9-15(14)22(25)26/h6-9,11,18,21H,10H2,1-5H3
IUPAC Name
3-methyl 5-(2-methylpropyl) 2,6-dimethyl-4-(2-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)OCC(C)C

Pharmacology

Indication

For the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.

Associated Conditions
Pharmacodynamics

Nisoldipine, 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. Nisoldipine is similar to other peripheral vasodilators. Nisoldipine 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, Nisoldipine 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 calcium channel subunit alpha-2/delta-1
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 L-type calcium channel subunit alpha-1S
inhibitor
Human
Absorption

Relatively well absorbed into the systemic circulation with 87% of the radiolabeled drug recovered in urine and feces. The absolute bioavailability of nisoldipine is about 5%.

Volume of distribution
Not Available
Protein binding

99%

Metabolism

Pre-systemic metabolism in the gut wall, and this metabolism decreases from the proximal to the distal parts of the intestine. Nisoldipine is highly metabolized; 5 major urinary metabolites have been identified. The major biotransformation pathway appears to be the hydroxylation of the isobutyl ester. A hydroxylated derivative of the side chain, present in plasma at concentrations approximately equal to the parent compound, appears to be the only active metabolite and has about 10% of the activity of the parent compound. Cytochrome P450 enzymes are believed to play a major role in the metabolism of nisoldipine. The particular isoenzyme system responsible for its metabolism has not been identified, but other dihydropyridines are metabolized by cytochrome P450 IIIA4.

Route of elimination

Although 60-80% of an oral dose undergoes urinary excretion, only traces of unchanged nisoldipine are found in urine.

Half life

7-12 hours

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

Interactions

Drug Interactions
DrugInteraction
AbafunginThe therapeutic efficacy of Abafungin can be increased when used in combination with Nisoldipine.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Nisoldipine.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Nisoldipine.
AceclofenacThe therapeutic efficacy of Nisoldipine can be decreased when used in combination with Aceclofenac.
AcemetacinThe therapeutic efficacy of Nisoldipine can be decreased when used in combination with Acemetacin.
AcepromazineThe risk or severity of hypotension can be increased when Acepromazine is combined with Nisoldipine.
AcetaminophenAcetaminophen may decrease the excretion rate of Nisoldipine which could result in a higher serum level.
Acetylsalicylic acidThe therapeutic efficacy of Nisoldipine can be decreased when used in combination with Acetylsalicylic acid.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Nisoldipine.
AlbaconazoleThe therapeutic efficacy of Albaconazole can be increased when used in combination with Nisoldipine.
Food Interactions
  • Do not take with grapefruit juice as this has been shown to interfere with nisoldipine metabolism, resulting in a mean increase in Cmax of about 3-fold (up to about 7-fold) and AUC of almost 2-fold (up to 5-fold).

References

Synthesis Reference

Massimo Ferrari, Marcello Ghezzi, Manuel Alberelli, Alberto Ambrosini, "Industrial process for the synthesis of isobutyl methyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridine dicarboxylate (nisoldipine)." U.S. Patent US20050240022, issued October 27, 2005.

US20050240022
General References
  1. Mielcarek J, Grobelny P, Szamburska O: The effect of beta-carotene on the photostability of nisoldipine. Methods Find Exp Clin Pharmacol. 2005 Apr;27(3):167-71. [PubMed:15834448]
  2. Missan S, Zhabyeyev P, Dyachok O, Jones SE, McDonald TF: Block of cardiac delayed-rectifier and inward-rectifier K+ currents by nisoldipine. Br J Pharmacol. 2003 Nov;140(5):863-70. Epub 2003 Oct 6. [PubMed:14530219]
  3. Hamilton SF, Houle LM, Thadani U: Rapid-release and coat-core formulations of nisoldipine in treatment of hypertension, angina, and heart failure. Heart Dis. 1999 Nov-Dec;1(5):279-88. [PubMed:11720635]
External Links
Human Metabolome Database
HMDB0014545
KEGG Drug
D00618
KEGG Compound
C07699
PubChem Compound
4499
PubChem Substance
46504546
ChemSpider
4343
BindingDB
50011689
ChEBI
76917
ChEMBL
CHEMBL1726
Therapeutic Targets Database
DAP000595
PharmGKB
PA450634
IUPHAR
2524
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Nisoldipine
ATC Codes
C08CA07 — Nisoldipine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers2
4CompletedTreatmentDiabetic Nephropathies1

Pharmacoeconomics

Manufacturers
  • Mylan pharmaceuticals inc
  • Shionogi pharma inc
Packagers
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Bayer Healthcare
  • Bryant Ranch Prepack
  • Heartland Repack Services LLC
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Physicians Total Care Inc.
  • Quality Care
  • Remedy Repack
  • Sciele Pharma Inc.
  • Shionogi Pharma Inc.
  • Skyepharma Production Sas
  • United Research Laboratories Inc.
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseOral17 mg/1
Tablet, film coated, extended releaseOral20 mg/1
Tablet, film coated, extended releaseOral25.5 mg/1
Tablet, film coated, extended releaseOral30 mg/1
Tablet, film coated, extended releaseOral34 mg/1
Tablet, film coated, extended releaseOral40 mg/1
Tablet, film coated, extended releaseOral8.5 mg/1
Prices
Unit descriptionCostUnit
Sular 25.5 mg 24 Hour tablet6.84USD tablet
Sular 34 mg 24 Hour tablet6.84USD tablet
Sular 17 mg 24 Hour tablet6.48USD tablet
Sular 34 mg tablet5.64USD tablet
Sular 17 mg tablet5.17USD tablet
Nisoldipine er 30 mg tablet5.07USD tablet
Nisoldipine er 40 mg tablet5.07USD tablet
Sular 10 mg tablet5.04USD tablet
Sular 8.5 mg 24 Hour tablet5.04USD tablet
Nisoldipine er 20 mg tablet4.65USD tablet
Sular 25.5 mg tablet4.35USD tablet
Sular 8.5 mg tablet4.13USD tablet
Sular 20 mg tablet3.37USD tablet
Sular 30 mg 24 Hour tablet3.23USD tablet
Sular 40 mg 24 Hour tablet3.23USD tablet
Sular 30 mg tablet3.1USD tablet
Sular 40 mg tablet2.61USD tablet
Sular 10 mg 24 Hour tablet2.36USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5626874No1994-11-302014-11-30Us
US5422123No1995-06-062012-06-06Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP3.26MASUMOTO,K ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.00577 mg/mLALOGPS
logP3.63ALOGPS
logP3.06ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)5.32ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area110.45 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity105.91 m3·mol-1ChemAxon
Polarizability39.72 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9357
Blood Brain Barrier-0.947
Caco-2 permeable+0.6928
P-glycoprotein substrateSubstrate0.5548
P-glycoprotein inhibitor IInhibitor0.8824
P-glycoprotein inhibitor IIInhibitor0.9239
Renal organic cation transporterNon-inhibitor0.8925
CYP450 2C9 substrateNon-substrate0.7874
CYP450 2D6 substrateNon-substrate0.8929
CYP450 3A4 substrateSubstrate0.7366
CYP450 1A2 substrateInhibitor0.8782
CYP450 2C9 inhibitorInhibitor0.7826
CYP450 2D6 inhibitorNon-inhibitor0.9141
CYP450 2C19 inhibitorInhibitor0.7804
CYP450 3A4 inhibitorInhibitor0.8414
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8982
Ames testNon AMES toxic0.778
CarcinogenicityNon-carcinogens0.5782
BiodegradationNot ready biodegradable0.9335
Rat acute toxicity2.6277 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8882
hERG inhibition (predictor II)Non-inhibitor0.9175
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 / Nitroaromatic compounds / Dicarboxylic acids and derivatives / Vinylogous amides / Enoate esters / Methyl esters / Amino acids and derivatives / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Enamines
show 6 more
Substituents
Dihydropyridinecarboxylic acid derivative / Nitrobenzene / Nitroaromatic compound / Monocyclic benzene moiety / Dicarboxylic acid or derivatives / Benzenoid / Methyl ester / Enoate ester / Alpha,beta-unsaturated carboxylic ester / Vinylogous amide
show 23 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
C-nitro compound, diester, methyl ester, dihydropyridine (CHEBI:76917)

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. Hu H, Marban E: Isoform-specific inhibition of L-type calcium channels by dihydropyridines is independent of isoform-specific gating properties. Mol Pharmacol. 1998 May;53(5):902-7. [PubMed:9584217]
  3. Morel N, Buryi V, Feron O, Gomez JP, Christen MO, Godfraind T: The action of calcium channel blockers on recombinant L-type calcium channel alpha1-subunits. Br J Pharmacol. 1998 Nov;125(5):1005-12. [PubMed:9846638]
  4. Wei X, Pan S, Lang W, Kim H, Schneider T, Perez-Reyes E, Birnbaumer L: Molecular determinants of cardiac Ca2+ channel pharmacology. Subunit requirement for the high affinity and allosteric regulation of dihydropyridine binding. J Biol Chem. 1995 Nov 10;270(45):27106-11. [PubMed:7592963]
  5. 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 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
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. 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
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 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]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
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. 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]

Drug created on June 13, 2005 07:24 / Updated on September 13, 2018 15:37