13 June 2018

4-aminopyridine-3-methanol

Purdue University researchers, working under the guidance of Professor Riyi Shi, have developed a drug – 4-aminopyridine-3-methanol – to treat the effects of spinal cord injuries. The mechanism of action of this drug is similar to that of the drug 4-aminopyridine (4-AP), previously developed by the same group and approved by the U.S. Food and Drug Administration (FDA) as a treatment for multiple sclerosis.

In spinal injuries, even in cases of preservation of the integrity of the spinal cord itself, i.e. long processes of nerve cells known as axons, damage to the myelin sheath covering nerve fibers can lead to the loss of various body functions, primarily motor functions. The reason is that damage to the myelin sheath leads to the opening of potassium channels located under it, which disrupts the passage of an electrical signal. Both drugs developed by the authors close these channels, restoring the conductivity of axons.

Manifestations characteristic of multiple sclerosis, such as impaired mobility and sensitivity, also develop due to the destruction of the myelin sheath, in this case resulting from the destructive action of their own immune cells. Approved 10 years ago as a treatment for multiple sclerosis, 4-AP has not been used in the treatment of spinal cord injuries due to the narrow spectrum of therapeutic dosage and potential toxicity.

Experiments on cell cultures and rats have shown that the new drug 4-aminopyridine-3-methanol copes with this task much better than 4-AP. It is safer and at least 50% more effective in closing potassium channels, and its action lasts for a longer period.

In addition to partial recovery of motor functions in spinal cord injuries, 4-aminopyridine-3-methanol has demonstrated the ability to significantly reduce the severity of chronic pain, which is a serious problem for such patients. Professor Shi notes that this indicates the expediency of its use for the relief of pain, regardless of the restoration of motor functions.

Also, the advantage of 4-aminopyridine-3-methanol is a wide range of its therapeutic dosage. The minimum effective dose of the drug may be 10 times less than the minimum effective dose of 4-AP, but at the same time, its maximum permissible dose may be 5 times higher.

Article by Jessica C. Page et al. Parallel Evaluation of Two Potassium Channel Blockers in Restoring Conduction in Mechanical Spinal Cord Injury in Rat is published in the Journal of Neurotrauma.

Evgenia Ryabtseva, portal "Eternal Youth" http://vechnayamolodost.ru based on materials from Purdue University: Possible new treatment for spinal cord injuries identified in animal studies.


Found a typo? Select it and press ctrl + enter Print version