Identification
- Summary
Levamlodipine is a calcium channel blocker used to treat hypertension.
- Brand Names
- Conjupri
- Generic Name
- Levamlodipine
- DrugBank Accession Number
- DB09237
- Background
Levamlodipine, also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive medication.8 Levamlodipine belongs to the dihydropyridine group of calcium channel blockers.8 This medication was first marketed in Russia and India before being granted FDA approval.9 The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however.8 As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.7
Levamlodipine was granted FDA approval on 19 December 2019.8
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Levamlodipine (DB09237)
- Weight
- Average: 408.88
Monoisotopic: 408.1451996 - Chemical Formula
- C20H25ClN2O5
- Synonyms
- Levamlodipine
- Levoamlodipine
- S-amlodipine
Pharmacology
- Indication
Levamlodipine is indicated alone or in combination to treat hypertension in adults and children.8
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat High blood pressure (hypertension) •••••••••••• •••••• ••••••••• •••••• Treatment of High blood pressure (hypertension) •••••••••••• •••••• ••••••••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Levamlodipine inhibits L-type calcium channels in vascular smooth muscle, reducing peripheral vascular resistance and blood pressure.8 It is given once daily in doses of 1.25-2.5mg in children and 2.5-5mg in adults.8 Patients should be counselled regarding the risk of symptomatic hypotension, worsening angina, and myocardial infarction.8
- Mechanism of action
Levamlodipine blocks the transmembrane influx of calcium through L-type calcium channels into the vascular and cardiac smooth muscles resulting in vasodilation and a subsequent decrease in blood pressure.4,8 Levamlodipine inhibits calcium influx in vascular smooth muscle to a greater degree than in cardiac muscle, leading to decreased peripheral vascular resistance and lowered blood pressure.8 In vitro studies have shown a negative inotropic effect but this is unlikely to be clinically relevant.8
Target Actions Organism UVoltage-dependent L-type calcium channel subunit alpha-1C antagonistHumans UVoltage-dependent L-type calcium channel subunit alpha-1D antagonistHumans UNitric oxide synthase, endothelial agonistHumans UNitric oxide synthase, inducible agonistHumans - Absorption
Oral levamlodipine has a Tmax of 6-12h and a bioavailability of 64-90%.8 Absorption of levamlodipine is not significantly affected by food.8
20mg or oral s-amlodipine besylate reaches a Cmax of 6.13±1.29ng/mL with a Tmax of 8.4±3.6h and an AUC of 351±72h*ng/mL.3 20mg or oral s-amlodipine maleate reaches a Cmax of 5.07±1.09ng/mL with a Tmax of 10.7±3.4h and an AUC of 330±88h*ng/mL.3
- Volume of distribution
The volume of distribution of levamlodipine is similar to amlodipine.3 The volume of distribution of amlodipine is 21L/kg.5,6
- Protein binding
Levamlodipine is 93% protein bound in plasma,8 largely to human serum albumin.2
- Metabolism
Levamlodipine is 90% metabolized to inactive metabolites.8 Incubation with liver microsomes has shown that this metabolism is primarily mediated by CYP3A4.1 Levamlodipine's dehydrogenation to a pyridine metabolite (M9) is the most important metabolic pathway in human liver microsomes.1 This derivative can be further oxidatively deaminated or O-dealkylated, but does not appear to undergo O-demethylation like racemic amlodipine.1
Hover over products below to view reaction partners
- Route of elimination
Levamlodipine is 60% eliminated in urine with 10% eliminated as the unmetabolized drug.8
- Half-life
Levamlodipine has a half life of 30-50h.8
- Clearance
The oral clearance of S-amlodipine besylate is 6.9±1.6mL/min/kg and the oral clearance of S-amlodipine maleate is 7.3±2.1mL/min/kg.3
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Patients experiencing an overdose may present with hypotension and reflex tachycardia.8 Treat overdose with cardiac and respiratory monitoring, frequent blood pressure measurement, elevation of extremities to treat hypotension, and possible administration of vasopressors.8 Hemodialysis is not expected to be useful as levamlodipine is highly protein bound.8
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbaloparatide Abaloparatide may increase the hypotensive activities of Levamlodipine. Abametapir The serum concentration of Levamlodipine can be increased when it is combined with Abametapir. Abatacept The metabolism of Levamlodipine can be increased when combined with Abatacept. Acalabrutinib The serum concentration of Levamlodipine can be increased when it is combined with Acalabrutinib. Acarbose The risk or severity of hypoglycemia can be increased when Levamlodipine is combined with Acarbose. - Food Interactions
- Take with or without food. Co-administration with food does not affect bioavailability.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Levamlodipine maleate 12WW9T2ITA 135969-53-8 TZNOWAJJWCGILX-HNUXRKMMSA-N - International/Other Brands
- Asomex (Emcure Pharmaceutical Ltd) / Conjupri / EsCordi Cor (Actavis Pharma) / Eslo (Zuventus Healthcare Ltd.) / Espin (Intas Pharmaceuticals Ltd)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Conjupri Tablet 5 mg/1 Oral Burke Therapeutics, LLC 2020-09-01 2022-08-11 US 
Conjupri Tablet 5 mg/5mg Oral CSPC Ouyi Pharmaceutical Co. Ltd 2020-12-19 Not applicable US Conjupri Tablet 2.5 mg/1 Oral Wraser Llc 2021-08-15 Not applicable US Conjupri Tablet 2.5 mg/1 Oral Burke Therapeutics, LLC 2020-09-01 2022-08-11 US Conjupri Tablet 2.5 mg/2.5mg Oral CSPC Ouyi Pharmaceutical Co. Ltd 2021-10-08 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Levamlodipine Tablet 5 mg/1 Oral Xspire Pharma, Llc 2021-08-15 Not applicable US Levamlodipine Tablet 2.5 mg/1 Oral Xspire Pharma, Llc 2021-08-15 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ALENCAL IRBE® 2.5/150 MG TABLETAS RECUBIERTAS Levamlodipine (2.5 mg) + Irbesartan (150 mg) Tablet, coated Oral CLARIPACK S.A 2014-02-25 Not applicable Colombia 
ALENCAL VALS 2.5/160MG TABLETAS RECUBIERTAS Levamlodipine (2.5 mg) + Valsartan (160 mg) Tablet, coated Oral CLARIPACK S.A. 2015-01-23 2020-08-05 Colombia ALENCAL VALS 2.5/320 MG TABLETAS RECUBIERTAS Levamlodipine (2.5 mg) + Valsartan (320 mg) Tablet, coated Oral COLOMPACK S.A. 2017-03-16 Not applicable Colombia VOLTRAMOS 2.5 MG/160 MG FILM KAPLI TABLET, 28 ADET Levamlodipine (2.5 mg) + Valsartan (160 mg) Tablet, coated Oral POLPHARMA SAĞLIK ÜRÜNLERİ SAN. VE TİC. A.Ş. 2020-08-14 2017-11-14 Turkey 
VOLTRAMOS 5 MG/160 MG FILM KAPLI TABLET, 28 ADET Levamlodipine (5 mg) + Valsartan (160 mg) Tablet, coated Oral POLPHARMA SAĞLIK ÜRÜNLERİ SAN. VE TİC. A.Ş. 2020-08-14 2017-11-14 Turkey
Categories
- ATC Codes
- C08CA17 — Levamlodipine
- Drug Categories
- Antiarrhythmic agents
- Antihypertensive Agents
- Antihypertensive Agents Indicated for Hypertension
- Calcium Channel Blockers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Substrates
- Dihydropyridine Derivatives
- Nicotinic Acids
- P-glycoprotein substrates
- Pyridines
- Selective Calcium Channel Blockers With Mainly Vascular Effects
- Chemical TaxonomyProvided by Classyfire
- 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
- Chlorobenzenes / Aryl chlorides / Dicarboxylic acids and derivatives / Vinylogous amides / Methyl esters / Enoate esters / Amino acids and derivatives / Azacyclic compounds / Dialkyl ethers / Dialkylamines show 7 more
- Substituents
- Alpha,beta-unsaturated carboxylic ester / Amine / Amino acid or derivatives / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Carbonyl group / Carboxylic acid derivative show 25 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- amlodipine (CHEBI:53796)
- Affected organisms
- Humans
Chemical Identifiers
- UNII
- 0P6NLP6806
- CAS number
- 103129-82-4
- InChI Key
- HTIQEAQVCYTUBX-KRWDZBQOSA-N
- InChI
- InChI=1S/C20H25ClN2O5/c1-4-28-20(25)18-15(11-27-10-9-22)23-12(2)16(19(24)26-3)17(18)13-7-5-6-8-14(13)21/h5-8,17,23H,4,9-11,22H2,1-3H3/t17-/m0/s1
- IUPAC Name
- 3-ethyl 5-methyl (4S)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
- SMILES
- CCOC(=O)C1=C(COCCN)NC(C)=C([C@@H]1C1=CC=CC=C1Cl)C(=O)OC
References
- General References
- Zhu Y, Wang F, Li Q, Zhu M, Du A, Tang W, Chen W: Amlodipine metabolism in human liver microsomes and roles of CYP3A4/5 in the dihydropyridine dehydrogenation. Drug Metab Dispos. 2014 Feb;42(2):245-9. doi: 10.1124/dmd.113.055400. Epub 2013 Dec 3. [Article]
- Liu Z, Zheng X, Yang X, Wang E, Wang J: Affinity and specificity of levamlodipine-human serum albumin interactions: insights into its carrier function. Biophys J. 2009 May 20;96(10):3917-25. doi: 10.1016/j.bpj.2008.12.3965. [Article]
- Laufen H, Leitold M: Enantioselective disposition of oral amlodipine in healthy volunteers. Chirality. 1994;6(7):531-6. doi: 10.1002/chir.530060704. [Article]
- Striessnig J, Ortner NJ, Pinggera A: Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets? Curr Mol Pharmacol. 2015;8(2):110-22. [Article]
- Meredith PA, Elliott HL: Clinical pharmacokinetics of amlodipine. Clin Pharmacokinet. 1992 Jan;22(1):22-31. doi: 10.2165/00003088-199222010-00003. [Article]
- Faulkner JK, McGibney D, Chasseaud LF, Perry JL, Taylor IW: The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily. Br J Clin Pharmacol. 1986 Jul;22(1):21-5. [Article]
- Liu F, Qiu M, Zhai SD: Tolerability and effectiveness of (S)-amlodipine compared with racemic amlodipine in hypertension: a systematic review and meta-analysis. Curr Ther Res Clin Exp. 2010 Feb;71(1):1-29. doi: 10.1016/j.curtheres.2010.02.005. [Article]
- FDA Approved Drug Products: Conjupri Levamlodipine Oral Tablets [Link]
- S-Amlodipine [Link]
- External Links
- PubChem Compound
- 9822750
- PubChem Substance
- 310265141
- ChemSpider
- 7998499
- 2376944
- ChEBI
- 53796
- ChEMBL
- CHEMBL2111097
- ZINC
- ZINC000100001964
- PDBe Ligand
- 6UB
- Wikipedia
- Levamlodipine
- PDB Entries
- 5kmd / 6ke5 / 7jpx / 8we8
- FDA label
- Download (350 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Hypertension 2 4 Unknown Status Treatment Hypertension 1 4 Unknown Status Treatment Hypertension, Essential Hypertension 1 3 Completed Treatment Hypertension 3 3 Unknown Status Treatment Hypertension 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 2.5 mg Tablet Oral 250000 mg Tablet, coated Oral 5 mg Tablet Oral 1.25 mg/1 Tablet Oral 1.25 mg/1.25mg Tablet Oral 2.5 mg/2.5mg Tablet Oral 2.5 mg/1 Tablet Oral 5 mg/5mg Tablet Oral 5 mg/1 Tablet, coated Oral - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 138 https://comptox.epa.gov/dashboard/dsstoxdb/results?formula=1&isotopes=1&search=C24H31ClN2O10 boiling point (°C) 413 https://comptox.epa.gov/dashboard/dsstoxdb/results?formula=1&isotopes=1&search=C24H31ClN2O10 water solubility 81 mg/mL http://www.selleckchem.com/products/levamlodipine.html logP 3.30 https://comptox.epa.gov/dashboard/dsstoxdb/results?formula=1&isotopes=1&search=C24H31ClN2O10 pKa 8.6 FDA Label - Predicted Properties
Property Value Source Water Solubility 0.0074 mg/mL ALOGPS logP 2.22 ALOGPS logP 1.64 Chemaxon logS -4.7 ALOGPS pKa (Strongest Acidic) 19.12 Chemaxon pKa (Strongest Basic) 9.45 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 99.88 Å2 Chemaxon Rotatable Bond Count 10 Chemaxon Refractivity 108.64 m3·mol-1 Chemaxon Polarizability 42.11 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-07fs-0009100000-9b57943551fbdd06a2b2 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-066r-0009200000-01d7ac102a78a1193f78 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0pxs-0019200000-afac5bbded5eaac7522a Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0009000000-f69bd27017aa8c548520 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-00ei-2093000000-ed19c8ab0979143df9b2 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0ug0-3159000000-c0dfd6c3948e96bf6eb3 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 201.61644 predictedDeepCCS 1.0 (2019) [M+H]+ 203.97444 predictedDeepCCS 1.0 (2019) [M+Na]+ 210.40398 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- 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
- Striessnig J, Ortner NJ, Pinggera A: Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets? Curr Mol Pharmacol. 2015;8(2):110-22. [Article]
- Johnson R, Dludla P, Mabhida S, Benjeddou M, Louw J, February F: Pharmacogenomics of amlodipine and hydrochlorothiazide therapy and the quest for improved control of hypertension: a mini review. Heart Fail Rev. 2019 May;24(3):343-357. doi: 10.1007/s10741-018-09765-y. [Article]
- FDA Approved Drug Products: Conjupri Levamlodipine Oral Tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- 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
- Johnson R, Dludla P, Mabhida S, Benjeddou M, Louw J, February F: Pharmacogenomics of amlodipine and hydrochlorothiazide therapy and the quest for improved control of hypertension: a mini review. Heart Fail Rev. 2019 May;24(3):343-357. doi: 10.1007/s10741-018-09765-y. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Tetrahydrobiopterin binding
- Specific Function
- Produces nitric oxide (NO) which is implicated in vascular smooth muscle relaxation through a cGMP-mediated signal transduction pathway. NO mediates vascular endothelial growth factor (VEGF)-induce...
- Gene Name
- NOS3
- Uniprot ID
- P29474
- Uniprot Name
- Nitric oxide synthase, endothelial
- Molecular Weight
- 133287.62 Da
References
- He Y, Si D, Yang C, Ni L, Li B, Ding M, Yang P: The effects of amlodipine and S(-)-amlodipine on vascular endothelial function in patients with hypertension. Am J Hypertens. 2014 Jan;27(1):27-31. doi: 10.1093/ajh/hpt138. Epub 2013 Aug 19. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Tetrahydrobiopterin binding
- Specific Function
- Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In macrophages, NO mediates tumoricidal and bactericidal actions. Also has nitrosylase activity ...
- Gene Name
- NOS2
- Uniprot ID
- P35228
- Uniprot Name
- Nitric oxide synthase, inducible
- Molecular Weight
- 131116.3 Da
References
- He Y, Si D, Yang C, Ni L, Li B, Ding M, Yang P: The effects of amlodipine and S(-)-amlodipine on vascular endothelial function in patients with hypertension. Am J Hypertens. 2014 Jan;27(1):27-31. doi: 10.1093/ajh/hpt138. Epub 2013 Aug 19. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- 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
- Zhu Y, Wang F, Li Q, Zhu M, Du A, Tang W, Chen W: Amlodipine metabolism in human liver microsomes and roles of CYP3A4/5 in the dihydropyridine dehydrogenation. Drug Metab Dispos. 2014 Feb;42(2):245-9. doi: 10.1124/dmd.113.055400. Epub 2013 Dec 3. [Article]
- Amlodipine Metabolism in Human Liver Microsomes and Roles of CYP3A4/5 in the Dihydropyridine Dehydrogenation [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Tetrahydrobiopterin binding
- Specific Function
- Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In macrophages, NO mediates tumoricidal and bactericidal actions. Also has nitrosylase activity ...
- Gene Name
- NOS2
- Uniprot ID
- P35228
- Uniprot Name
- Nitric oxide synthase, inducible
- Molecular Weight
- 131116.3 Da
References
- He Y, Si D, Yang C, Ni L, Li B, Ding M, Yang P: The effects of amlodipine and S(-)-amlodipine on vascular endothelial function in patients with hypertension. Am J Hypertens. 2014 Jan;27(1):27-31. doi: 10.1093/ajh/hpt138. Epub 2013 Aug 19. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Tetrahydrobiopterin binding
- Specific Function
- Produces nitric oxide (NO) which is implicated in vascular smooth muscle relaxation through a cGMP-mediated signal transduction pathway. NO mediates vascular endothelial growth factor (VEGF)-induce...
- Gene Name
- NOS3
- Uniprot ID
- P29474
- Uniprot Name
- Nitric oxide synthase, endothelial
- Molecular Weight
- 133287.62 Da
References
- He Y, Si D, Yang C, Ni L, Li B, Ding M, Yang P: The effects of amlodipine and S(-)-amlodipine on vascular endothelial function in patients with hypertension. Am J Hypertens. 2014 Jan;27(1):27-31. doi: 10.1093/ajh/hpt138. Epub 2013 Aug 19. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Liu Z, Zheng X, Yang X, Wang E, Wang J: Affinity and specificity of levamlodipine-human serum albumin interactions: insights into its carrier function. Biophys J. 2009 May 20;96(10):3917-25. doi: 10.1016/j.bpj.2008.12.3965. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Johnson R, Dludla P, Mabhida S, Benjeddou M, Louw J, February F: Pharmacogenomics of amlodipine and hydrochlorothiazide therapy and the quest for improved control of hypertension: a mini review. Heart Fail Rev. 2019 May;24(3):343-357. doi: 10.1007/s10741-018-09765-y. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Bile acid:sodium symporter activity
- Specific Function
- Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine. Plays a key role in cholesterol metabolism.
- Gene Name
- SLC10A2
- Uniprot ID
- Q12908
- Uniprot Name
- Ileal sodium/bile acid cotransporter
- Molecular Weight
- 37713.405 Da
References
- Zheng X, Diao L, Ekins S, Polli JE: Why we should be vigilant: drug cytotoxicity observed with in vitro transporter inhibition studies. Biochem Pharmacol. 2010 Oct 1;80(7):1087-92. doi: 10.1016/j.bcp.2010.06.012. Epub 2010 Jun 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Symporter activity
- Specific Function
- Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
- Gene Name
- SLC22A5
- Uniprot ID
- O76082
- Uniprot Name
- Solute carrier family 22 member 5
- Molecular Weight
- 62751.08 Da
References
- Zheng X, Diao L, Ekins S, Polli JE: Why we should be vigilant: drug cytotoxicity observed with in vitro transporter inhibition studies. Biochem Pharmacol. 2010 Oct 1;80(7):1087-92. doi: 10.1016/j.bcp.2010.06.012. Epub 2010 Jun 23. [Article]
Drug created at October 23, 2015 16:47 / Updated at August 13, 2021 04:44