4-Aminopyridine

4-Aminopyridine. A Non Specific K⁺ Channel Blocker.

Voltage-gated K⁺ channels (K_v ) play an important role in number of different aspects of the electrical responses of the nervous system. Their activity determines the frequency of action potential and the shape of the action potential waveform.
Furthermore, K_v channels may regulate the excitability of individual neurons, and may control the strength of synaptic contacts between neurons.
4-Aminopyridine (4-AP) is a non-selective K_v channel blocker, which can block a wide variety of K_v channels with different state dependences. Therefore, in search for clues for the structural determinants of K_v channels that are important for the state dependences of drug-channel interactions, 4-AP serves as a useful tool. For example, it blocks K_v 2.1 and K_v 3.1 channels with IC₅₀ of 18 and 0.1 mM, respectively, in oocytes. K_v 1.1 and K_v 1.2 channels are blocked by 4-AP with IC₅₀ of 147 μM and 230 μM, respectively, in CHO cells.
Multiple sclerosis (MS) is an inflammatory demyelinating disease of the central nervous system, characterized by axonal conduction block. 4-AP has been tested as a symptomatic treatment in patients with MS based on the clinical rationale that neurologic function could be improved by overcoming conduction block in demyelinated axons present in MS lesions. Indeed, 4-AP restored conduction in experimentally demyelinated nerves in the peripheral nervous system. In addition, 4-AP increased presynaptic action potential duration and amplitude leading to enhanced transmitter release.

Ion Channel Modulators; K⁺ Channel Blockers.

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