Drug intelligence / Profile preview

2,4-diaminopyridine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

2,4-diaminopyridine is a small molecule potassium channel blocker that acts primarily by antagonizing presynaptic voltage-gated potassium channels, thereby enhancing neuromuscular transmission[2]. It increases the duration of the action potential at the nerve terminal, leading to increased calcium influx and augmented release of acetylcholine at the neuromuscular junction. In preclinical and clinical studies, 2,4-diaminopyridine has shown efficacy in reversing the effects of various muscle relaxants (such as curare derivatives) used in anesthesia, and in potentiating neuromuscular transmission in diseases that reduce neurotransmission, such as myasthenia gravis and botulism[2]. It is reported to be about as potent as 3,4-diaminopyridine and markedly less toxic than 3,4-diaminopyridine and 4-aminopyridine, with fewer central nervous system stimulant side effects[2]. Its use has primarily been described in research and patent literature; it is not widely marketed or approved as a pharmaceutical product.

Other names
2,4-diaminopyridine2,4-DAP
02

Targets

Kir (Inward-rectifier potassium channels)

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