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Identification
NameBepridil
Accession NumberDB01244  (APRD00727)
TypeSmall Molecule
GroupsApproved, Withdrawn
Description

A long-acting, non selective, calcium channel blocker with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. [PubChem] It is no longer marketed in the United States, as it has been implicated in causing ventricular arrhythmias (ie. Torsade de pointes).

Structure
Thumb
Synonyms
Bepadin
Bepridil
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AngoprilNot Available
CordiumNot Available
VascorNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Bepridil hydrochloride
ThumbNot applicableDBSALT001436
Categories
UNII755BO701MA
CAS number64706-54-3
WeightAverage: 366.5396
Monoisotopic: 366.26711372
Chemical FormulaC24H34N2O
InChI KeyInChIKey=UIEATEWHFDRYRU-UHFFFAOYSA-N
InChI
InChI=1S/C24H34N2O/c1-21(2)19-27-20-24(25-15-9-10-16-25)18-26(23-13-7-4-8-14-23)17-22-11-5-3-6-12-22/h3-8,11-14,21,24H,9-10,15-20H2,1-2H3
IUPAC Name
N-benzyl-N-[3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl]aniline
SMILES
CC(C)COCC(CN(CC1=CC=CC=C1)C1=CC=CC=C1)N1CCCC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylmethylamines. These are compounds containing a phenylmethtylamine moiety, which consists of a phenyl group substituted by an methanamine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylmethylamines
Direct ParentPhenylmethylamines
Alternative Parents
Substituents
  • Dialkylarylamine
  • Phenylmethylamine
  • Benzylamine
  • Aralkylamine
  • Aniline
  • N-alkylpyrrolidine
  • Pyrrolidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Dialkyl ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of hypertension, and chronic stable angina (classic effort-associated angina).
PharmacodynamicsBepridil is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It is not related chemically to other calcium channel blockers such as diltiazem hydrochloride, nifedipine and verapamil hydrochloride.
Mechanism of actionBepridil has inhibitory effects on both the slow calcium (L-type) and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. Bepridil inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. This has been demonstrated in isolated myocardial and vascular smooth muscle preparations in which both the slope of the calcium dose response curve and the maximum calcium-induced inotropic response were significantly reduced by bepridil. In cardiac myocytes in vitro, bepridil was shown to be tightly bound to actin. Bepridil regularly reduces heart rate and arterial pressure at rest and at a given level of exercise by dilating peripheral arterioles and reducing total peripheral resistance (afterload) against which the heart works.
Related Articles
AbsorptionRapidly and completely absorbed after oral administration.
Volume of distributionNot Available
Protein binding99%
Metabolism

Hepatic.

Route of eliminationNot Available
Half life24-50 hours
ClearanceNot Available
ToxicityThere has been one experience with overdosage in which a patient inadvertently took a single dose of 1600 mg of bepridil. The patient was observed for 72 hours in intensive care, but no significant adverse experiences were noted.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9859
Blood Brain Barrier+0.9003
Caco-2 permeable+0.5593
P-glycoprotein substrateSubstrate0.7013
P-glycoprotein inhibitor IInhibitor0.7951
P-glycoprotein inhibitor IIInhibitor0.8387
Renal organic cation transporterInhibitor0.6774
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.5495
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorNon-inhibitor0.8462
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5636
Ames testNon AMES toxic0.67
CarcinogenicityNon-carcinogens0.8688
BiodegradationNot ready biodegradable0.9938
Rat acute toxicity2.4903 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.536
hERG inhibition (predictor II)Inhibitor0.796
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point128Mauvernay, R.Y., Busch, N., Moleyre, J., Monteil, A. and Simond, J.; U.S. Patent 3,962,238; June 8,1976; assigned to Centre Europeen de Recherches Mauvernay "CERM".
water solubilitySlightly solubleNot Available
logP5.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00655 mg/mLALOGPS
logP5.33ALOGPS
logP5.49ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)9.16ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area15.71 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity115.12 m3·mol-1ChemAxon
Polarizability43.5 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Mauvernay, R.Y., Busch, N., Moleyre, J., Monteil, A. and Simond, J.; U.S. Patent 3,962,238;
June 8,1976; assigned to Centre Europeen de Recherches Mauvernay “CERM”.

General ReferencesNot Available
External Links
ATC CodesC08EA02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcetaminophenThe metabolism of Bepridil can be increased when combined with Acetaminophen.
AlfentanilAlfentanil may increase the bradycardic activities of Bepridil.
AmiodaroneBepridil may increase the bradycardic activities of Amiodarone.
AmlodipineAmlodipine may increase the hypotensive activities of Bepridil.
AmobarbitalThe metabolism of Bepridil can be increased when combined with Amobarbital.
AtazanavirThe metabolism of Bepridil can be decreased when combined with Atazanavir.
Atracurium besylateBepridil may increase the neuromuscular blocking activities of Atracurium besylate.
BoceprevirThe serum concentration of Bepridil can be increased when it is combined with Boceprevir.
ButabarbitalThe metabolism of Bepridil can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Bepridil can be increased when combined with Butalbital.
CaffeineThe metabolism of Bepridil can be increased when combined with Caffeine.
Calcium AcetateThe therapeutic efficacy of Bepridil can be decreased when used in combination with Calcium Acetate.
Calcium carbonateThe therapeutic efficacy of Bepridil can be decreased when used in combination with Calcium carbonate.
Calcium ChlorideThe therapeutic efficacy of Bepridil can be decreased when used in combination with Calcium Chloride.
Calcium citrateThe therapeutic efficacy of Bepridil can be decreased when used in combination with Calcium citrate.
Calcium gluconateThe therapeutic efficacy of Bepridil can be decreased when used in combination with Calcium gluconate.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Bepridil.
CimetidineThe serum concentration of Bepridil can be increased when it is combined with Cimetidine.
CisaprideCisapride may increase the QTc-prolonging activities of Bepridil.
Cisatracurium besylateBepridil may increase the neuromuscular blocking activities of Cisatracurium besylate.
ClarithromycinThe metabolism of Bepridil can be decreased when combined with Clarithromycin.
ClevidipineClevidipine may increase the hypotensive activities of Bepridil.
ClonidineClonidine may increase the atrioventricular blocking (AV block) activities of Bepridil.
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Bepridil.
CyclosporineThe metabolism of Cyclosporine can be decreased when combined with Bepridil.
DantroleneDantrolene may increase the hyperkalemic activities of Bepridil.
DarunavirThe metabolism of Bepridil can be decreased when combined with Darunavir.
DigoxinBepridil may increase the atrioventricular blocking (AV block) activities of Digoxin.
DoxazosinDoxazosin may increase the hypotensive activities of Bepridil.
EfavirenzThe serum concentration of Bepridil can be decreased when it is combined with Efavirenz.
ErythromycinThe metabolism of Bepridil can be decreased when combined with Erythromycin.
EtravirineThe serum concentration of Bepridil can be decreased when it is combined with Etravirine.
FelodipineFelodipine may increase the hypotensive activities of Bepridil.
FentanylFentanyl may increase the bradycardic activities of Bepridil.
FluconazoleThe serum concentration of Bepridil can be increased when it is combined with Fluconazole.
FosamprenavirThe metabolism of Bepridil can be decreased when combined with Fosamprenavir.
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Bepridil.
IndinavirThe metabolism of Bepridil can be decreased when combined with Indinavir.
IsradipineIsradipine may increase the hypotensive activities of Bepridil.
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Bepridil.
IvabradineBepridil may increase the bradycardic activities of Ivabradine.
KetoconazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Bepridil.
LopinavirThe metabolism of Bepridil can be decreased when combined with Lopinavir.
Magnesium chlorideThe risk or severity of adverse effects can be increased when Bepridil is combined with Magnesium chloride.
Magnesium citrateThe risk or severity of adverse effects can be increased when Bepridil is combined with Magnesium citrate.
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Bepridil is combined with Magnesium hydroxide.
Magnesium oxideThe risk or severity of adverse effects can be increased when Bepridil is combined with Magnesium oxide.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Bepridil is combined with Magnesium salicylate.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Bepridil is combined with Magnesium Sulfate.
MethohexitalThe metabolism of Bepridil can be increased when combined with Methohexital.
MidodrineBepridil may increase the bradycardic activities of Midodrine.
NafcillinThe metabolism of Bepridil can be increased when combined with Nafcillin.
NelfinavirThe metabolism of Bepridil can be decreased when combined with Nelfinavir.
NicardipineNicardipine may increase the hypotensive activities of Bepridil.
NifedipineNifedipine may increase the hypotensive activities of Bepridil.
NimodipineNimodipine may increase the hypotensive activities of Bepridil.
NisoldipineNisoldipine may increase the hypotensive activities of Bepridil.
NitroprussideBepridil may increase the hypotensive activities of Nitroprusside.
PancuroniumBepridil may increase the neuromuscular blocking activities of Pancuronium.
PentobarbitalThe metabolism of Bepridil can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Bepridil can be increased when combined with Phenobarbital.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Bepridil.
PhentolaminePhentolamine may increase the hypotensive activities of Bepridil.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Bepridil.
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Bepridil.
PrazosinPrazosin may increase the hypotensive activities of Bepridil.
RegorafenibRegorafenib may increase the bradycardic activities of Bepridil.
RemifentanilRemifentanil may increase the bradycardic activities of Bepridil.
RifabutinThe serum concentration of Bepridil can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Bepridil can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Bepridil can be decreased when it is combined with Rifapentine.
RitonavirThe metabolism of Bepridil can be decreased when combined with Ritonavir.
RocuroniumBepridil may increase the neuromuscular blocking activities of Rocuronium.
SaquinavirBepridil may increase the arrhythmogenic activities of Saquinavir.
SecobarbitalThe metabolism of Bepridil can be increased when combined with Secobarbital.
SilodosinSilodosin may increase the hypotensive activities of Bepridil.
SufentanilSufentanil may increase the bradycardic activities of Bepridil.
SulfisoxazoleThe metabolism of Bepridil can be decreased when combined with Sulfisoxazole.
TamsulosinTamsulosin may increase the hypotensive activities of Bepridil.
TelaprevirThe risk or severity of adverse effects can be increased when Telaprevir is combined with Bepridil.
TelithromycinThe metabolism of Bepridil can be decreased when combined with Telithromycin.
TerazosinTerazosin may increase the hypotensive activities of Bepridil.
TipranavirThe serum concentration of Bepridil can be increased when it is combined with Tipranavir.
VecuroniumBepridil may increase the neuromuscular blocking activities of Vecuronium.
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Bepridil.
Food Interactions
  • Alcohol may further decrease blood pressure and increase dizziness and drowsiness
  • Take with food to reduce nausea.

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-1A gives rise to P and/or Q-type calcium currents. P/Q-type calcium channels belong to...
Gene Name:
CACNA1A
Uniprot ID:
O00555
Molecular Weight:
282362.39 Da
References
  1. 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 ]
  2. 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 ]
  3. Bezprozvanny I, Tsien RW: Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967). Mol Pharmacol. 1995 Sep;48(3):540-9. [PubMed:7565636 ]
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. Bezprozvanny I, Tsien RW: Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967). Mol Pharmacol. 1995 Sep;48(3):540-9. [PubMed:7565636 ]
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. Bezprozvanny I, Tsien RW: Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967). Mol Pharmacol. 1995 Sep;48(3):540-9. [PubMed:7565636 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hormone binding
Specific Function:
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions, providing the energy for active transport of various nutrients.
Gene Name:
ATP1A1
Uniprot ID:
P05023
Molecular Weight:
112895.01 Da
References
  1. Kovacic H, Gallice P, Crevat A: Inhibition of sodium pump by bepridil. An in vitro and microcalorimetric study. Biochem Pharmacol. 1992 Oct 20;44(8):1529-34. [PubMed:1329768 ]
  2. Raess BU, Record DM: Inhibition of erythrocyte Ca2(+)-pump by Ca2+ antagonists. Biochem Pharmacol. 1990 Dec 1;40(11):2549-55. [PubMed:2148481 ]
  3. Smith SJ, England PJ: The effects of reported Ca2+ sensitisers on the rates of Ca2+ release from cardiac troponin C and the troponin-tropomyosin complex. Br J Pharmacol. 1990 Aug;100(4):779-85. [PubMed:2207500 ]
  4. Lamers JM, Cysouw KJ, Verdouw PD: Slow calcium channel blockers and calmodulin. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. Biochem Pharmacol. 1985 Nov 1;34(21):3837-43. [PubMed:2933041 ]
  5. Fuchs J, Mainka L, Reifart N, Zimmer G: Effects of bepridil on heart mitochondrial membrane and the isolated rat heart preparation. Arzneimittelforschung. 1986 Feb;36(2):209-12. [PubMed:2938592 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function:
Potassium channel that plays an important role in a number of tissues, including heart, inner ear, stomach and colon (By similarity) (PubMed:10646604). Associates with KCNE beta subunits that modulates current kinetics (By similarity) (PubMed:9312006, PubMed:9108097, PubMed:8900283, PubMed:10646604, PubMed:11101505, PubMed:19687231). Induces a voltage-dependent by rapidly activating and slowly ...
Gene Name:
KCNQ1
Uniprot ID:
P51787
Molecular Weight:
74697.925 Da
References
  1. Chouabe C, Drici MD, Romey G, Barhanin J: Effects of calcium channel blockers on cloned cardiac K+ channels IKr and IKs. Therapie. 2000 Jan-Feb;55(1):195-202. [PubMed:10860024 ]
  2. Yumoto Y, Horie M, Kubota T, Ninomiya T, Kobori A, Takenaka K, Takano M, Niwano S, Izumi T: Bepridil block of recombinant human cardiac IKs current shows a time-dependent unblock. J Cardiovasc Pharmacol. 2004 Feb;43(2):178-82. [PubMed:14716203 ]
  3. Chouabe C, Drici MD, Romey G, Barhanin J, Lazdunski M: HERG and KvLQT1/IsK, the cardiac K+ channels involved in long QT syndromes, are targets for calcium channel blockers. Mol Pharmacol. 1998 Oct;54(4):695-703. [PubMed:9765513 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other
General Function:
Troponin t binding
Specific Function:
Troponin is the central regulatory protein of striated muscle contraction. Tn consists of three components: Tn-I which is the inhibitor of actomyosin ATPase, Tn-T which contains the binding site for tropomyosin and Tn-C. The binding of calcium to Tn-C abolishes the inhibitory action of Tn on actin filaments.
Gene Name:
TNNC1
Uniprot ID:
P63316
Molecular Weight:
18402.36 Da
References
  1. Abusamhadneh E, Abbott MB, Dvoretsky A, Finley N, Sasi S, Rosevear PR: Interaction of bepridil with the cardiac troponin C/troponin I complex. FEBS Lett. 2001 Sep 28;506(1):51-4. [PubMed:11591369 ]
  2. Wang X, Li MX, Sykes BD: Structure of the regulatory N-domain of human cardiac troponin C in complex with human cardiac troponin I147-163 and bepridil. J Biol Chem. 2002 Aug 23;277(34):31124-33. Epub 2002 Jun 11. [PubMed:12060657 ]
  3. MacLachlan LK, Reid DG, Mitchell RC, Salter CJ, Smith SJ: Binding of a calcium sensitizer, bepridil, to cardiac troponin C. A fluorescence stopped-flow kinetic, circular dichroism, and proton nuclear magnetic resonance study. J Biol Chem. 1990 Jun 15;265(17):9764-70. [PubMed:2351672 ]
  4. Kleerekoper Q, Liu W, Choi D, Putkey JA: Identification of binding sites for bepridil and trifluoperazine on cardiac troponin C. J Biol Chem. 1998 Apr 3;273(14):8153-60. [PubMed:9525919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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 of protein kinases and phosphatases. Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis.
Gene Name:
CALM1
Uniprot ID:
P62158
Molecular Weight:
16837.47 Da
References
  1. Lamers JM, Cysouw KJ, Verdouw PD: Slow calcium channel blockers and calmodulin. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. Biochem Pharmacol. 1985 Nov 1;34(21):3837-43. [PubMed:2933041 ]
  2. Lamers JM, Verdouw PD, Mas-Oliva J: The effects of felodipine and bepridil on calcium-stimulated calmodulin binding and calcium pumping ATPase of cardiac sarcolemma before and after removal of endogenous calmodulin. Mol Cell Biochem. 1987 Dec;78(2):169-76. [PubMed:2964559 ]
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 a substrate.
Gene Name:
PDE1B
Uniprot ID:
Q01064
Molecular Weight:
61379.235 Da
References
  1. Lamers JM, Cysouw KJ, Verdouw PD: Slow calcium channel blockers and calmodulin. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. Biochem Pharmacol. 1985 Nov 1;34(21):3837-43. [PubMed:2933041 ]
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 cGMP than for cAMP.
Gene Name:
PDE1A
Uniprot ID:
P54750
Molecular Weight:
61251.38 Da
References
  1. Lamers JM, Cysouw KJ, Verdouw PD: Slow calcium channel blockers and calmodulin. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. Biochem Pharmacol. 1985 Nov 1;34(21):3837-43. [PubMed:2933041 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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 ]

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
Molecular Weight:
141477.255 Da
References
  1. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on November 30, 2015 12:10