This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Identification
- Generic Name
- Cariporide
- DrugBank Accession Number
- DB06468
- Background
Not Available
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for Cariporide (DB06468)
- Weight
- Average: 283.35
Monoisotopic: 283.099062593 - Chemical Formula
- C12H17N3O3S
- Synonyms
- Cariporide
Pharmacology
- Indication
Investigated for use/treatment in cardiac surgery.
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Not Available
- Mechanism of action
Cariporide is a selective sodium-hydrogen antiporter inhibitor. The sodium-hydrogen exchanger is an importatn player in the pathophysiology of myocardial ischemia-referfusion injury. The accumulation of hydrogen ions in the myocyte cytoso; during ischemia creates a proton gradiant that promote the efflux of hydrogen ions in exchange for the influx of sodium ions. This sodium buildup can secondary activates the sodium-calcium exchanger to operate in the reverse mode, resulting in a net calcium accumulation in myocyte cytosol, which leads to dysfunction and cell death. By inhibiting sodium-hydrogen exchange, Cariporide can prevent the accumulation of calcium in cytosol, therefore reduce the infarct size.
Target Actions Organism USodium/hydrogen exchanger 1 Not Available Humans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 softwareAcebutolol Acebutolol may increase the arrhythmogenic activities of Cariporide. Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Cariporide. Acrivastine The risk or severity of QTc prolongation can be increased when Cariporide is combined with Acrivastine. Adenosine Adenosine may increase the arrhythmogenic activities of Cariporide. Ajmaline Ajmaline may increase the arrhythmogenic activities of Cariporide. Alfuzosin The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Cariporide. Alimemazine The risk or severity of QTc prolongation can be increased when Alimemazine is combined with Cariporide. Amantadine The risk or severity of QTc prolongation can be increased when Amantadine is combined with Cariporide. Amifampridine The risk or severity of QTc prolongation can be increased when Cariporide is combined with Amifampridine. Amiodarone The risk or severity of adverse effects can be increased when Amiodarone is combined with Cariporide. 
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- Not Available
Products
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Ingredient UNII CAS InChI Key Cariporide Mesylate 0543W2JFRZ 159138-81-5 FNDLQABGYJQJPH-UHFFFAOYSA-N
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as aromatic monoterpenoids. These are monoterpenoids containing at least one aromatic ring.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Prenol lipids
- Sub Class
- Monoterpenoids
- Direct Parent
- Aromatic monoterpenoids
- Alternative Parents
- Monocyclic monoterpenoids / Phenylpropanes / Cumenes / Benzoic acids and derivatives / Benzenesulfonyl compounds / Benzoyl derivatives / Acylguanidines / Sulfones / Propargyl-type 1,3-dipolar organic compounds / Carboxylic acids and derivatives show 5 more
- Substituents
- Acylguanidine / Aromatic homomonocyclic compound / Aromatic monoterpenoid / Benzenesulfonyl group / Benzenoid / Benzoic acid or derivatives / Benzoyl / Carboximidamide / Carboxylic acid derivative / Cumene show 17 more
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 7E3392891K
- CAS number
- 159138-80-4
- InChI Key
- IWXNYAIICFKCTM-UHFFFAOYSA-N
- InChI
- InChI=1S/C12H17N3O3S/c1-7(2)9-5-4-8(11(16)15-12(13)14)6-10(9)19(3,17)18/h4-7H,1-3H3,(H4,13,14,15,16)
- IUPAC Name
- N-carbamimidoyl-3-methanesulfonyl-4-(propan-2-yl)benzamide
- SMILES
- CC(C)C1=CC=C(C=C1S(C)(=O)=O)C(=O)NC(N)=N
References
- General References
- Not Available
- External Links
- ChemSpider
- 133240
- BindingDB
- 50058759
- ChEMBL
- CHEMBL436559
- ZINC
- ZINC000013474734
- PDBe Ligand
- HG0
- Wikipedia
- Cariporide
- PDB Entries
- 7dsx
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.15 mg/mL ALOGPS logP 0.86 ALOGPS logP 0.63 Chemaxon logS -3.3 ALOGPS pKa (Strongest Acidic) 10.27 Chemaxon pKa (Strongest Basic) 7.62 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 113.11 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 84.17 m3·mol-1 Chemaxon Polarizability 29 Å3 Chemaxon Number of Rings 1 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 GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Solute:proton antiporter activity
- Specific Function
- Involved in pH regulation to eliminate acids generated by active metabolism or to counter adverse environmental conditions. Major proton extruding system driven by the inward sodium ion chemical gr...
- Gene Name
- SLC9A1
- Uniprot ID
- P19634
- Uniprot Name
- Sodium/hydrogen exchanger 1
- Molecular Weight
- 90762.13 Da
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Peroxidase activity
- Specific Function
- Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production o...
- Gene Name
- MPO
- Uniprot ID
- P05164
- Uniprot Name
- Myeloperoxidase
- Molecular Weight
- 83867.71 Da
References
- McAllister SE, Moses MA, Jindal K, Ashrafpour H, Cahoon NJ, Huang N, Neligan PC, Forrest CR, Lipa JE, Pang CY: Na+/H+ exchange inhibitor cariporide attenuates skeletal muscle infarction when administered before ischemia or reperfusion. J Appl Physiol (1985). 2009 Jan;106(1):20-8. doi: 10.1152/japplphysiol.91069.2008. Epub 2008 Nov 20. [Article]
Drug created at March 19, 2008 16:34 / Updated at February 21, 2021 18:52