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The Mechanism of 4-AP Action


By Anita Kaiser
Canadian Spinal Research Organization

Spinal cord injury causes damage to the nerves in the spinal cord. Often the myelin, the insulative coating surrounding the nerve axon, is damaged or worn away. The myelin enables speedy transmission of electrical signals across the nerves.

When a healthy nerve cell transmits an electrical signal, it is excited causing potassium ions to flow through it to bring the nerve back to a normal state. A damaged nerve is no longer able to transmit signals. Injury to the myelin allows the potassium ions to leak out preventing the nerve from reaching an excited state to transmit a signal.

A drug 4-AP, (4-aminopyridine) has been discovered that has the ability to counteract the effects of demyelination. It is a nerve conduction enhancing compound. The drug blocks the pore or channel that allows potassium ions to flow through when the nerve cell is excited. This blocking ability makes the cell more excitable. In other words, it amplifies the impulse signal so that it can travel through the nerve past the demyelinated area.

Up until now, 4-AP has provided temporary improvement in chronic, incomplete spinal cord injury, since it has only been administered on a one-time basis. It appears that the drug needs to be given daily in order to obtain sustained improvement. Some effects include increased bowel and bladder control, increased sexual function, increased sensation below the level of injury, decreased stiffness or spasticity, and reduction in pain. Currently, clinical trials are planned to examine the long term usage of 4-AP.

VIDEO  Learn about the effectiveness of 4AP


 


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