Identification

Name
Dalfampridine
Accession Number
DB06637
Type
Small Molecule
Groups
Approved
Description

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.

Structure
Thumb
Synonyms
  • 4-Aminopyridine
  • 4-AP
  • 4-Pyridinamine
  • 4-Pyridylamine
  • Avitrol
  • Dalfampridine
  • Fampridina
  • Fampridine
  • Fampridine-SR
  • Fampridinum
  • gamma-Aminopyridine
  • N07XX07
  • P-Aminopyridine
External IDs
EL-970 / NSC-15041
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AmpyraTablet, film coated, extended release10 mg/1OralAcorda Therapeutics2010-03-01Not applicableUs
FampyraTablet, extended release10 mgOralBiogen2012-02-24Not applicableCanada
FampyraTablet, extended release10 mgOralBiogen Idec Limited2011-07-20Not applicableEu
FampyraTablet, extended release10 mgOralBiogen Idec Limited2011-07-20Not applicableEu
FampyraTablet, extended release10 mgOralBiogen Idec Limited2011-07-20Not applicableEu
FampyraTablet, extended release10 mgOralBiogen Idec Limited2011-07-20Not applicableEu
International/Other Brands
Ampyra
Categories
UNII
BH3B64OKL9
CAS number
504-24-5
Weight
Average: 94.1145
Monoisotopic: 94.053098202
Chemical Formula
C5H6N2
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

Pharmacology

Indication

Dalfampridine is a neurofunctional modifier that helps improve walking speed in patients with multiple sclerosis (MS).

Structured Indications
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.

TargetActionsOrganism
APotassium voltage-gated channel subfamily A member 1
antagonist
Human
APotassium voltage-gated channel subfamily A member 2
antagonist
Human
APotassium voltage-gated channel subfamily A member 3
antagonist
Human
APotassium voltage-gated channel subfamily A member 4
antagonist
Human
APotassium voltage-gated channel subfamily A member 5
antagonist
Human
APotassium voltage-gated channel subfamily A member 6
antagonist
Human
APotassium voltage-gated channel subfamily A member 7
antagonist
Human
APotassium voltage-gated channel subfamily A member 10
antagonist
Human
APotassium voltage-gated channel subfamily B member 1
antagonist
Human
APotassium voltage-gated channel subfamily B member 2
antagonist
Human
APotassium voltage-gated channel subfamily C member 1
antagonist
Human
APotassium voltage-gated channel subfamily C member 2
antagonist
Human
APotassium voltage-gated channel subfamily C member 3
antagonist
Human
APotassium voltage-gated channel subfamily D member 1
antagonist
Human
APotassium voltage-gated channel subfamily D member 2
antagonist
Human
APotassium voltage-gated channel subfamily D member 3
antagonist
Human
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.

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
Toxicity

LD50, oral, mouse = 19 mg/kg LD50, oral, rat = 21 mg/kg

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
CimetidineThe serum concentration of Dalfampridine can be increased when it is combined with Cimetidine.Approved
ClotrimazoleThe metabolism of Dalfampridine can be decreased when combined with Clotrimazole.Approved, Vet Approved
Cyproterone acetateThe serum concentration of Dalfampridine can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
IsoniazidThe metabolism of Dalfampridine can be decreased when combined with Isoniazid.Approved
MetforminThe serum concentration of Dalfampridine can be increased when it is combined with Metformin.Approved
NicotineThe metabolism of Dalfampridine can be decreased when combined with Nicotine.Approved
QuinidineThe serum concentration of Dalfampridine can be increased when it is combined with Quinidine.Approved
TiclopidineThe metabolism of Dalfampridine can be decreased when combined with Ticlopidine.Approved
Food Interactions
  • A high fat meal significantly increases Cmax but this effect is not clinically relevant. May take dalfampridine without regard to meals

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
  1. 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. [PubMed:21635193]
  2. 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. [PubMed:22764324]
  3. 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. [PubMed:22497693]
  4. 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. [PubMed:22135060]
  5. 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. [PubMed:16472864]
External Links
KEGG Drug
D04127
KEGG Compound
C13728
PubChem Compound
1727
PubChem Substance
175427081
ChemSpider
1664
BindingDB
10458
ChEBI
34385
ChEMBL
CHEMBL284348
PharmGKB
PA166123389
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
4-Aminopyridine
ATC Codes
N07XX07 — Fampridine
AHFS Codes
  • 92:92.00 — Other Miscellaneous Therapeutic Agents
FDA label
Download (315 KB)
MSDS
Download (95.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers1
1RecruitingTreatmentMotor Neuron Disease, Upper1
1, 2CompletedTreatmentGait disturbances / Parkinson's Disease (PD)1
2Active Not RecruitingTreatmentDisseminated Sclerosis2
2Active Not RecruitingTreatmentIdiopathic Transverse Myelitis / Myelitis NOS / Neuromyelitis Optica / Transverse Myelitis1
2CompletedNot AvailableMiller Fisher Syndrome1
2CompletedTreatmentDisseminated Sclerosis2
2CompletedTreatmentDisseminated Sclerosis / Tiredness1
2CompletedTreatmentSleep Apnea, Obstructive1
2RecruitingBasic ScienceDisseminated Sclerosis / Internuclear Ophthalmoplegia / Tiredness1
2RecruitingTreatmentSpinal Cord Injuries (SCI)1
2Unknown StatusTreatmentEpisodic Ataxia Type 21
2, 3CompletedTreatmentDisseminated Sclerosis1
2, 3CompletedTreatmentDisseminated Sclerosis / Optic Neuritis1
2, 3CompletedTreatmentSpinal Muscular Atrophy (SMA)1
3CompletedTreatmentDisseminated Sclerosis8
3CompletedTreatmentDisseminated Sclerosis / Multiple Sclerosis, Primary Progressive / Multiple Sclerosis, Remittent Progressive / Relapsing Remitting Multiple Sclerosis (RRMS) / Secondary Progressive Multiple Sclerosis (SPMS)1
3CompletedTreatmentMuscle Spasticity / Spinal Cord Injuries (SCI)2
3CompletedTreatmentPost-Ischemic Stroke1
3TerminatedTreatmentPost-Ischemic Stroke1
4Active Not RecruitingTreatmentMultiple Sclerosis, Primary Progressive / Secondary Progressive Multiple Sclerosis (SPMS)1
4CompletedTreatmentDisseminated Sclerosis4
4CompletedTreatmentNon Arteritic Ischemic Optic Neuropathy1
4RecruitingTreatmentDisseminated Sclerosis1
4TerminatedTreatmentTransverse Myelitis1
4Unknown StatusTreatmentDisseminated Sclerosis2
Not AvailableCompletedTreatmentSpinocerebellar Ataxias Type 1 / Spinocerebellar Ataxias Type 2 / Spinocerebellar Ataxias Type 3 / Spinocerebellar Ataxias Type 61
Not AvailableRecruitingNot AvailableDisseminated Sclerosis2
Not AvailableRecruitingNot AvailableDisseminated Sclerosis / EDSS 4-71
Not AvailableTerminatedNot AvailableDisseminated Sclerosis / Pregnancy1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseOral10 mg/1
Tablet, extended releaseOral10 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5540938No1998-07-302018-07-30Us
US8007826No2007-05-262027-05-26Us
US8354437No2006-12-222026-12-22Us
US8440703No2005-04-082025-04-08Us
US8663685No2005-01-182025-01-18Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)157-161°CMSDS
boiling point (°C)273°CMSDS
water solubility74 g/LMSDS
pKa11MSDS
Predicted Properties
PropertyValueSource
Water Solubility6.73 mg/mLALOGPS
logP-0.65ALOGPS
logP0.29ChemAxon
logS-1.2ALOGPS
pKa (Strongest Acidic)16.04ChemAxon
pKa (Strongest Basic)12.18ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area35.88 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity40.09 m3·mol-1ChemAxon
Polarizability9.66 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.961
Blood Brain Barrier+0.9544
Caco-2 permeable+0.8867
P-glycoprotein substrateNon-substrate0.8619
P-glycoprotein inhibitor INon-inhibitor0.9916
P-glycoprotein inhibitor IINon-inhibitor0.9885
Renal organic cation transporterNon-inhibitor0.8423
CYP450 2C9 substrateNon-substrate0.8832
CYP450 2D6 substrateNon-substrate0.887
CYP450 3A4 substrateNon-substrate0.8181
CYP450 1A2 substrateNon-inhibitor0.8657
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.7984
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8637
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8154
Ames testNon AMES toxic0.572
CarcinogenicityNon-carcinogens0.822
BiodegradationNot ready biodegradable0.9426
Rat acute toxicity2.5498 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9785
hERG inhibition (predictor II)Non-inhibitor0.9385
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
GC-MS Spectrum - EI-BGC-MSsplash10-0006-9000000000-d76cf775a4e0c55c9a50
Mass Spectrum (Electron Ionization)MSsplash10-0006-9000000000-8298bac1cfd86955d1ee
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
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable

Taxonomy

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
Aminopyridine / Heteroaromatic compound / Azacycle / Organic nitrogen compound / Organopnictogen compound / Hydrocarbon derivative / Primary amine / Organonitrogen compound / Amine / Aromatic heteromonocyclic compound
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
aromatic amine, aminopyridine (CHEBI:34385)

Targets

Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:23184313]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:16472864]

Enzymes

Kind
Protein
Organism
Human
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
  1. 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. [PubMed:22764324]

Drug created on March 19, 2008 10:42 / Updated on November 19, 2017 20:34