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Details

Stereochemistry ACHIRAL
Molecular Formula C5H6N2.ClH
Molecular Weight 130.575
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of 4-Aminopyridine hydrochloride

SMILES

Cl.NC1=CC=NC=C1

InChI

InChIKey=CBFZWGRQXZYRRR-UHFFFAOYSA-N
InChI=1S/C5H6N2.ClH/c6-5-1-3-7-4-2-5;/h1-4H,(H2,6,7);1H

HIDE SMILES / InChI

Description

Dalfampridine is a potassium channel blocker, used as a research tool in characterizing subtypes of the potassium channel. Dalfampridine has also been used as a drug, to manage some of the symptoms of multiple sclerosis, and is indicated for symptomatic improvement of walking in adults with several variations of the disease. The mechanism by which dalfampridine exerts its therapeutic effect has not been fully elucidated. Dalfampridine is a broad spectrum potassium channel blocker. In animal studies, dalfampridine has been shown to increase conduction of action potentials in demyelinated axons through inhibition of potassium channels.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
195.0 µM [Kd]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
AMPYRA

Cmax

ValueDoseCo-administeredAnalytePopulation
23.77 ng/mL
10 mg single, oral
DALFAMPRIDINE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
246.48 ng × h/mL
10 mg single, oral
DALFAMPRIDINE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
0.16 h
10 mg single, oral
DALFAMPRIDINE plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
97%
10 mg single, oral
DALFAMPRIDINE plasma
Homo sapiens

Doses

AEs

Drug as perpetrator​

Drug as victim

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
The maximum recommended dose of AMPYRA is one 10 mg tablet twice daily, taken with or without food, and should not be exceeded.
Route of Administration: Oral
In Vitro Use Guide
At DIV25, the differentiating cells were re-seeded to Matrigel coated 12-mm glass coverslips in densities of 400,000 cells per well. Media was replaced completely the next day by fresh maturation media. Media containing either 100 mM 4-Aminopyridine diluted in DMSO or the equivalent amount DMSO only was given to the cells 72 hours before the start of week 7 (DIV42) and lasted until the cells were analyzed during week 7. Half the media was replaced every third day. Final electrophysiological recordings of the treated vs. non-treated cells rigorously were taken in pairs of one treated and one nontreated coverslip within a time frame of 48 hours.