General
Preferred name
DALFAMPRIDINE
Synonyms
fampridine ()
4-Aminopyridine methiodide ()
4-Aminopyridine ()
4-AP ()
4-Pyridinamine ()
4-aminopyridine, Neurorecovery ()
Neurelan ()
EL-970 ()
Ampyra ()
Fampridine (4-aminopyridine) ()
Fampridine ()
Fampyra ()
NSC-15041 ()
Ampyra Extended Release ()
P&D ID
PD001882
CAS
504-24-5
Tags
natural product
drug
available
Approved by
FDA
First approval
2010
Drug Status
approved
Drug indication
Multiple Sclerosis Symptomatic Treatment
Multiple sclerosis
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Fampridine is the INN for this compound, whereas its USAN is dalfampridine. (GtoPdb)
HALF-LIFE Immediate release form = 3.5 hours;; Extended release form = 5.47 hours;
TOXICITY LD50, oral, mouse = 19 mg/kg; LD50, oral, rat = 21 mg/kg
ROE 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%)
MOA 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%
DESCRIPTION Induces depolarization of GABA neurons; weak non-selective ;K+-channel blocker; anticonvulsant (LOPAC library)
DESCRIPTION NMDA antagonist; less active enantiomer of (+)-MK 801 (Tocris Bioactive Compound Library)
DESCRIPTION Non-selective KV channel blocker (Tocriscreen Total)
Compound Sets
26
AdooQ Bioactive Compound Library
A17490
Cayman Chemical Bioactives
18511
ChEMBL Approved Drugs
CHEMBL284348
ChEMBL Drugs
CHEMBL284348
Concise Guide to Pharmacology 2017/18
2416
Concise Guide to Pharmacology 2019/20
2416
Concise Guide to Pharmacology 2021/22
2416
Concise Guide to Pharmacology 2023/24
2416
Drug Repurposing Hub
DrugBank
DB06637
DrugBank Approved Drugs
DB06637
DrugCentral
4163
DrugCentral Approved Drugs
4163
DrugMAP
DMM0PDO
DrugMAP Approved Drugs
DMM0PDO
DrugMatrix
Enamine BioReference Compounds
Guide to Pharmacology
2416
JUMP-Target 1 Compound Set
1727
LOPAC library
NCATS Inxight Approved Drugs
BH3B64OKL9
NPC Screening Collection
ReFrame library
The Spectrum Collection
Tocris Bioactive Compound Library
0940
Tocriscreen Total
External IDs
40
Properties
(calculated by RDKit )
Molecular Weight
94.05
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
1
Rotatable Bonds
0
Ring Count
1
Aromatic Ring Count
1
cLogP
0.66
TPSA
38.91
Fraction CSP3
0.0
Chiral centers
0.0
Largest ring
6.0
QED
0.51
Structural alerts
2
aggregator (Aggregator Advisor)
Aggregators
aggregator (ZINC)
Aggregators
Related compounds
Custom attributes
(extracted from source data)
Selectivity
A-type
Primary Target
Voltage-gated Potassium (KV) Channels
MOA
Blocker
potassium channel blocker
Target
KCNA1, KCNA10, KCNA2, KCNA3, KCNA4, KCNA5, KCNA6, KCNA7, KCNB1, KCNB2, KCNC1, KCNC2, KCNC3, KCNC4, KCND1, KCND2, KCND3, KCNF1, KCNG1, KCNG2, KCNG3, KCNG4, KCNH1, KCNH2, KCNH3, KCNH4, KCNH5, KCNH6, KCNH7, KCNH8, KCNJ13, KCNJ5, KCNQ1, KCNQ2, KCNQ3, KCNQ4, KCNQ5, KCNS1, KCNS2, KCNS3, KCNV1, KCNV2
KCNH7
Indication
multiple sclerosis
Source data