Applications of 4-Aminopyridine

4-Aminopyridine (INN fampridine, USAN dalfampridine) is an organic compound with the chemical formula C5H4N–NH2. The molecule is one of the three isomeric amines of pyridine. It is used primarily as a research tool, in characterizing subtypes of potassium channel, and has also been used 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 drug has orphan drug status in the United States under the trade name Neurelan. It was undergoing Phase III clinical trials as of 2008, and the U.S. Food and Drug Administration (FDA) approved the compound on January 22, 2010. Fampridine is also marketed as Ampyra (pronounced "am-PEER-ah," according to the maker's website) in the United States by Acorda Therapeutics and as Fampyra in Europe.
Applications
The largest scale industrial application of 4-Aminopyridine is as a precursor to the drug pinacidil, which affects potassium ion channels.
In the laboratory, 4-AP is a useful pharmacological tool in studying various potassium conductances in physiology and biophysics. It is a relatively selective blocker of members of Kv1 (Shaker, KCNA) family of voltage-activated K+ channels. At concentration of 1 mM it selectively and reversibly inhibits Shaker channels without significant effect on other sodium, calcium, and potassium conductances.
4-Aminopyridine is also used as a bird control agent, under the trade name Avitrol; it causes convulsions and typically death, depending on dosage. The use of 4-aminopyridine in bird control has been criticized by the Humane Society of the United States.
Medical use
Fampridine has been used clinically in Lambert-Eaton myasthenic syndrome and multiple sclerosis. It acts by blocking potassium channels, prolonging action potentials and thereby increasing neurotransmitter release at the neuromuscular junction. The drug has been shown to reverse tetrodotoxin toxicity in animal experiments.
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