Name: 4-Aminopyridine
Brand: Alomone Labs
SKU: A-115

Cat #: A-115

Alternative Name 4-AP

Lyophilized Powder yes

Bioassay Tested

Source Synthetic

MW: 94.1

Purity: >99% (HPLC)

Effective concentration IC₅₀ ~ 0.1-18 mM.

Structure

Chemical name 4-Aminopyridine.

Molecular formula C₅H₆N₂.

CAS No.: 504-24-5

Activity 4-Aminopyridine is a non-selective K_V channel blocker¹, which blocks nearly all K_V currents although its potency varies over a wide range². It blocks K_V2.1 and K_V3.1 channels with IC₅₀ of 18 and 0.1 mM, respectively, in oocytes². K_V1.1 and K_V1.2 channels are blocked by 4-AP with IC₅₀ of 147 μM and 230 μM, respectively, in CHO cells¹. It has also been used in the clinic to manage some of the symptoms of Multiple Sclerosis³.

References-Activity

Perreault, P. et al. (1991) J. Neurophysiol. 65, 771.
Stephens, G.J. et al. (1994) J. Physiol. 477, 187.
Kirsch, G.E. et al. (1993) Neuron 11, 503.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility Water. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to one week at 4°C or six months at -20°C.

Our bioassay

Alomone Labs 4-Aminopyridine blocks K_V1.2 channel currents heterologously expressed in Xenopus oocytes.
A. Time course of current reversible inhibition by 1 mM 4-Aminopyridine (#A-115) (as extracted from the ramp response at 60 mV). B. Example traces of K_V1.2 currents in response to 200 sec ramp depolarization (from -80 mV to 60 mV during 100 msec) before and during 1 mM 4-Aminopyridine application.

References - Scientific background

Roeper, J. et al. (1996) Curr. Opin Neurobiol. 6, 338.
Mathie, A. et al. (1998) Gen. Pharmacol. 30, 13.
Stephens, G.J. et al. (1994) J. Physiol. 477, 187.
Tseng, G.N. et al. (1996) J. Pharmacol. Exp. Ther. 279, 865.
Kirsch, G.E. et al. (1993) Neuron 11, 503.
Martin, R. et al. (1992) Annu. Rev. Immunol. 10, 153.
Rasband, M.N. et al. (1998) J. Neurosci. 18, 36.

Scientific background

Voltage-gated K⁺ channels (K_V) play an important role in a number of different aspects of electrical responses of the nervous system. Their activity determines the frequency of action potentials 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^1,2.

4-Aminopyridine (4-AP) is a non-selective K_V channel blocker³, which can block a wide variety of K_V channels with different state dependencies⁴. Therefore, in search for clues for the structural determinants of K_V channels that are important for the state dependencies of drug-channel interactions, 4-AP serves as a useful tool. For example, it blocks K_V2.1 and K_V3.1 channels with IC₅₀s of 18 and 0.1 mM, respectively, in oocytes⁵. K_V1.1 and K_V1.2 channels are blocked by 4-AP with IC₅₀s of 147 µM and 230 µM, respectively, in CHO cells³.

Multiple sclerosis (MS) is an inflammatory demyelinating disease of the central nervous system, characterized by axonal conduction block⁶. 4-AP has been tested as a symptomatic treatment in patients with MS based on the clinical rationale that neurological 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 system⁷. In addition, 4-AP increased presynaptic action potential duration and amplitude leading to enhanced transmitter release⁸.

Target K_V K⁺ channels

Lyophilized Powder

Last update: 02/01/2022

4-Aminopyridine (#A-115) is a highly pure, synthetic, and biologically active compound.

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4-Aminopyridine

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