Identification
- Summary
Dalfampridine is a potassium channel blocker used for the improvement of motor function in patients with multiple sclerosis (MS).
- Brand Names
- Ampyra, Fampyra
- Generic Name
- Dalfampridine
- DrugBank Accession Number
- DB06637
- Background
Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk. This is the first drug that was specifically approved to help with mobility in these patients. FDA approved on January 22, 2010.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Dalfampridine (DB06637)
- Weight
- Average: 94.1145
Monoisotopic: 94.053098202 - Chemical Formula
- C5H6N2
- Synonyms
- 4-Aminopyridine
- 4-AP
- 4-Pyridinamine
- 4-Pyridylamine
- Dalfampridine
- Fampridina
- Fampridine
- Fampridinum
- p-Aminopyridine
- γ-Aminopyridine
- External IDs
- EL-970
- NSC-15041
Pharmacology
- Indication
Dalfampridine is a neurofunctional modifier that helps improve walking speed in patients with multiple sclerosis (MS).
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 Management of Multiple sclerosis •••••••••••• - 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
Dalfampridine is a board-spectrum lipophillic potassium channel blocker and binds favourably to the open state than closed state of the potassium channel in the CNS. Its pharmacological target are the potassium channels exposed in MS patients. Does not prolong the QTc interval.
- Mechanism of action
In MS, axons are progressively demyelinated which exposes potassium channels. As a result, there is a leak of potassium ions which results in the repolarization of cells and a decrease in neuronal excitability. The overall impact is the impairment of neuromuscular transmission as it is harder to trigger an action potential. Dalfampridine inhibits voltage-gated potassium channels in the CNS to maintain the transmembrane potential and prolong action potential. In other words, dalfampridine works to make sure that the current available is high enough to stimulate conduction in demyelinated axons that are exposed in MS patients. Furthermore, it facilitates neuromuscular and synaptic transmission by relieving conduction blocks in demyelinated axons.
- Absorption
Orally-administered dalfampridine is rapidly and completely absorbed from the gastrointestinal tract. Tmax, immediate release form = 1 hour; Tmax, extended release form = 3.5 hours; Cmax, 10 mg extended release = 17.3 - 21.6 ng/mL; Relative bioavailability of 10 mg extended-release tablets compared to aqueous oral solution = 96%
- Volume of distribution
10 mg extended release = 2.6 L/kg
- Protein binding
10 mg extended release = 1-3% protein bound
- Metabolism
Not extensively metabolized by the liver therefore drugs effecting the cytochrome P450 enzyme system that are concomitantly administered with dalfampridine are not expected to interact with each other. Metabolites include 3-hydroxy-4-aminopyridine and 3-hydroxy-4-aminopyridine sulfate and both are inactive. CYP2E1 is the enzyme responsible for 3-hydroxylation of dalfampridine.
Hover over products below to view reaction partners
- Route of elimination
Almost all of the dose and its metabolites are completely eliminated by the kidneys after 24 hours. Urine (96%; 90% of total dose as unchanged drug); Feces (0.5%)
- Half-life
Immediate release form = 3.5 hours; Extended release form = 5.47 hours;
- Clearance
Not Available
- 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
LD50, oral, mouse = 19 mg/kg LD50, oral, rat = 21 mg/kg
- 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 softwareAbacavir Abacavir may decrease the excretion rate of Dalfampridine which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Dalfampridine which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Dalfampridine which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Dalfampridine which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Dalfampridine which could result in a lower serum level and potentially a reduction in efficacy. - Food Interactions
- Take with or without food. High-fat meals increase drug absorption, but not to a clinically significant extent.
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.- International/Other Brands
- Avitrol / Fampridine-SR
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ampyra Tablet, film coated, extended release 10 mg/1 Oral Elan Pharma International LTD 2010-03-01 2010-05-13 US 
Ampyra Tablet, film coated, extended release 10 mg/1 Oral Acorda Therapeutics, Inc. 2010-03-01 Not applicable US Fampridine Accord Tablet, extended release 10 mg Oral Accord Healthcare S.L.U. 2020-12-16 Not applicable EU 
Fampridine Accord Tablet, extended release 10 mg Oral Accord Healthcare S.L.U. 2020-12-16 Not applicable EU Fampyra Tablet, extended release 10 mg Oral Biogen Netherlands B.V. 2016-09-08 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Dalfampridine Tablet, film coated, extended release 10 mg/1 Oral Mylan Pharmaceuticals Inc. 2022-05-31 Not applicable US Dalfampridine Tablet, extended release 10 mg/1 Oral Sun Pharmaceutical Industries, Inc. 2019-05-22 Not applicable US Dalfampridine Tablet, film coated, extended release 10 mg/1 Oral Ascend Laboratories, LLC 2018-07-31 Not applicable US Dalfampridine Tablet, film coated, extended release 10 mg/1 Oral Mylan Pharmaceuticals Inc. 2018-09-10 2022-05-31 US Dalfampridine Tablet, film coated, extended release 10 mg/1 Oral bryant ranch prepack 2018-07-31 Not applicable US
Categories
- ATC Codes
- N07XX07 — Fampridine
- Drug Categories
- Amines
- Aminopyridines
- Cardiovascular Agents
- Cytochrome P-450 CYP2E1 Substrates
- Cytochrome P-450 CYP2E1 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Membrane Transport Modulators
- Narrow Therapeutic Index Drugs
- Nervous System
- OCT2 Substrates
- OCT2 Substrates with a Narrow Therapeutic Index
- Other Miscellaneous Therapeutic Agents
- Potassium Channel Blockers
- Pyridines
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as aminopyridines and derivatives. These are organic heterocyclic compounds containing an amino group attached to a pyridine ring.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Pyridines and derivatives
- Sub Class
- Aminopyridines and derivatives
- Direct Parent
- Aminopyridines and derivatives
- Alternative Parents
- Heteroaromatic compounds / Azacyclic compounds / Primary amines / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Amine / Aminopyridine / Aromatic heteromonocyclic compound / Azacycle / Heteroaromatic compound / Hydrocarbon derivative / Organic nitrogen compound / Organonitrogen compound / Organopnictogen compound / Primary amine
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- aromatic amine, aminopyridine (CHEBI:34385)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- BH3B64OKL9
- CAS number
- 504-24-5
- InChI Key
- NUKYPUAOHBNCPY-UHFFFAOYSA-N
- InChI
- InChI=1S/C5H6N2/c6-5-1-3-7-4-2-5/h1-4H,(H2,6,7)
- IUPAC Name
- 1,4-dihydropyridin-4-imine
- SMILES
- NC1=CC=NC=C1
References
- Synthesis Reference
Fabio GARAVAGLIA, Alessandro BAROZZA, Jacopo ROLETTO, Paolo PAISSONI, "ONE-POT PROCESS FOR THE SYNTHESIS OF DALFAMPRIDINE." U.S. Patent US20110319628, issued December 29, 2011.
US20110319628- General References
- Panitch H, Applebee A: Treatment of walking impairment in multiple sclerosis: an unmet need for a disease-specific disability. Expert Opin Pharmacother. 2011 Jul;12(10):1511-21. doi: 10.1517/14656566.2011.586338. Epub 2011 Jun 2. [Article]
- Pikoulas TE, Fuller MA: Dalfampridine: a medication to improve walking in patients with multiple sclerosis. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1010-5. doi: 10.1345/aph.1Q714. Epub 2012 Jul 3. [Article]
- Cornblath DR, Bienen EJ, Blight AR: The safety profile of dalfampridine extended release in multiple sclerosis clinical trials. Clin Ther. 2012 May;34(5):1056-69. doi: 10.1016/j.clinthera.2012.03.007. Epub 2012 Apr 11. [Article]
- McDonald S, Clements JN: Dalfampridine: a new agent for symptomatic management of multiple sclerosis. Am J Health Syst Pharm. 2011 Dec 15;68(24):2335-40. doi: 10.2146/ajhp110134. [Article]
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- FDA Approved Drug Products: AMPYRA (dalfampridine) tablets [Link]
- External Links
- KEGG Drug
- D04127
- KEGG Compound
- C13728
- PubChem Compound
- 1727
- PubChem Substance
- 175427081
- ChemSpider
- 1664
- BindingDB
- 10458
- 897018
- ChEBI
- 34385
- ChEMBL
- CHEMBL284348
- ZINC
- ZINC000000599985
- PharmGKB
- PA166123389
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- 4-Aminopyridine
- FDA label
- Download (315 KB)
- MSDS
- Download (95.5 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 Multiple Sclerosis 6 4 Completed Treatment Non Arteritic Ischemic Optic Neuropathy 1 4 Completed Treatment Primary Progressive Multiple Sclerosis (PPMS) / Secondary Progressive Multiple Sclerosis (SPMS) 1 4 Not Yet Recruiting Treatment Multiple Sclerosis 1 4 Terminated Treatment Transverse Myelitis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated, extended release Oral 10 mg/1 Tablet, extended release Oral 10 mg/1 Tablet, extended release Oral 10 mg Tablet, extended release Oral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5540938 No 1996-07-30 2018-07-30 US US8007826 No 2011-08-30 2027-05-26 US US8354437 No 2013-01-15 2026-12-22 US US8440703 No 2013-05-14 2025-04-08 US US8663685 No 2014-03-04 2025-01-18 US US9918973 No 2018-03-20 2024-12-13 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 157-161°C MSDS boiling point (°C) 273°C MSDS water solubility 74 g/L MSDS pKa 11 MSDS - Predicted Properties
Property Value Source Water Solubility 271.0 mg/mL ALOGPS logP 0.08 ALOGPS logP 0.29 Chemaxon logS 0.46 ALOGPS pKa (Strongest Acidic) 16.04 Chemaxon pKa (Strongest Basic) 12.18 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 35.88 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 40.09 m3·mol-1 Chemaxon Polarizability 9.66 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.961 Blood Brain Barrier + 0.9544 Caco-2 permeable + 0.8867 P-glycoprotein substrate Non-substrate 0.8619 P-glycoprotein inhibitor I Non-inhibitor 0.9916 P-glycoprotein inhibitor II Non-inhibitor 0.9885 Renal organic cation transporter Non-inhibitor 0.8423 CYP450 2C9 substrate Non-substrate 0.8832 CYP450 2D6 substrate Non-substrate 0.887 CYP450 3A4 substrate Non-substrate 0.8181 CYP450 1A2 substrate Non-inhibitor 0.8657 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.7984 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8637 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8154 Ames test Non AMES toxic 0.572 Carcinogenicity Non-carcinogens 0.822 Biodegradation Not ready biodegradable 0.9426 Rat acute toxicity 2.5498 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9785 hERG inhibition (predictor II) Non-inhibitor 0.9385
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 109.548388 predictedDarkChem Lite v0.1.0 [M-H]- 120.45022 predictedDeepCCS 1.0 (2019) [M+H]+ 109.689688 predictedDarkChem Lite v0.1.0 [M+H]+ 122.71863 predictedDeepCCS 1.0 (2019) [M+Na]+ 110.003688 predictedDarkChem Lite v0.1.0 [M+Na]+ 131.17389 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
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
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and the central nervous system, but also in the kidney (PubMed:1990381...
- Gene Name
- KCNA1
- Uniprot ID
- Q09470
- Uniprot Name
- Potassium voltage-gated channel subfamily A member 1
- Molecular Weight
- 56465.01 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and the central nervous system, but also in the cardiovascular system....
- Gene Name
- KCNA2
- Uniprot ID
- P16389
- Uniprot Name
- Potassium voltage-gated channel subfamily A member 2
- Molecular Weight
- 56716.21 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated ion channel activity
- Specific Function
- Mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein form...
- Gene Name
- KCNA3
- Uniprot ID
- P22001
- Uniprot Name
- Potassium voltage-gated channel subfamily A member 3
- Molecular Weight
- 63841.09 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes. Forms tetrameric potassium-selective channels through which potassium ions pass in accordance...
- Gene Name
- KCNA4
- Uniprot ID
- P22459
- Uniprot Name
- Potassium voltage-gated channel subfamily A member 4
- Molecular Weight
- 73256.64 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity involved in sa node cell action potential repolarization
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes. Forms tetrameric potassium-selective channels through which potassium ions pass in accordance...
- Gene Name
- KCNA5
- Uniprot ID
- P22460
- Uniprot Name
- Potassium voltage-gated channel subfamily A member 5
- Molecular Weight
- 67227.15 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes. Forms tetrameric potassium-selective channels through which potassium ions pass in accordance...
- Gene Name
- KCNA6
- Uniprot ID
- P17658
- Uniprot Name
- Potassium voltage-gated channel subfamily A member 6
- Molecular Weight
- 58728.21 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Delayed rectifier potassium channel activity
- Specific Function
- Mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein form...
- Gene Name
- KCNA7
- Uniprot ID
- Q96RP8
- Uniprot Name
- Potassium voltage-gated channel subfamily A member 7
- Molecular Weight
- 50558.415 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Intracellular cyclic nucleotide activated cation channel activity
- Specific Function
- Mediates voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a ...
- Gene Name
- KCNA10
- Uniprot ID
- Q16322
- Uniprot Name
- Potassium voltage-gated channel subfamily A member 10
- Molecular Weight
- 57784.47 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Ubiquitin-like protein binding
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain, but also in the pancreas and cardiovascular system. Contributes to th...
- Gene Name
- KCNB1
- Uniprot ID
- Q14721
- Uniprot Name
- Potassium voltage-gated channel subfamily B member 1
- Molecular Weight
- 95876.615 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and smooth muscle cells. Channels open or close in response to the vol...
- Gene Name
- KCNB2
- Uniprot ID
- Q92953
- Uniprot Name
- Potassium voltage-gated channel subfamily B member 2
- Molecular Weight
- 102561.99 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein form...
- Gene Name
- KCNC1
- Uniprot ID
- P48547
- Uniprot Name
- Potassium voltage-gated channel subfamily C member 1
- Molecular Weight
- 57941.87 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain. Contributes to the regulation of the fast action potential repolariza...
- Gene Name
- KCNC2
- Uniprot ID
- Q96PR1
- Uniprot Name
- Potassium voltage-gated channel subfamily C member 2
- Molecular Weight
- 70224.915 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- This protein mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the...
- Gene Name
- KCNC3
- Uniprot ID
- Q14003
- Uniprot Name
- Potassium voltage-gated channel subfamily C member 3
- Molecular Weight
- 80577.23 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Metal ion binding
- Specific Function
- Pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels. May contribute to I(To) current in heart and I(Sa) current in neurons. Channel properties are modulated...
- Gene Name
- KCND1
- Uniprot ID
- Q9NSA2
- Uniprot Name
- Potassium voltage-gated channel subfamily D member 1
- Molecular Weight
- 71329.6 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain. Mediates the major part of the dendritic A-type current I(SA) in brai...
- Gene Name
- KCND2
- Uniprot ID
- Q9NZV8
- Uniprot Name
- Potassium voltage-gated channel subfamily D member 2
- Molecular Weight
- 70535.825 Da
References
- Goodman AD, Stone RT: Enhancing neural transmission in multiple sclerosis (4-aminopyridine therapy). Neurotherapeutics. 2013 Jan;10(1):106-10. doi: 10.1007/s13311-012-0156-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Metal ion binding
- Specific Function
- Pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels. May contribute to I(To) current in heart and I(Sa) current in neurons. Channel properties are modulated...
- Gene Name
- KCND3
- Uniprot ID
- Q9UK17
- Uniprot Name
- Potassium voltage-gated channel subfamily D member 3
- Molecular Weight
- 73450.53 Da
References
- Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- Pikoulas TE, Fuller MA: Dalfampridine: a medication to improve walking in patients with multiple sclerosis. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1010-5. doi: 10.1345/aph.1Q714. Epub 2012 Jul 3. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Quaternary ammonium group transmembrane transporter activity
- Specific Function
- Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
Drug created at March 19, 2008 16:42 / Updated at February 20, 2024 23:55