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New Hope for Neuropathic Pain: Drug Keeps Nerve-Calming Potassium Channels Open

  [ 37 votes ]   [ Discuss This Article ] • May 23, 2012

New medication, already licensed & headed for clinical trials, "could bring relief to hundreds of millions."

Neuropathic pain (aka nerve pain or neuropathy) involves impulses from damaged, sensitive nerve fibers which are felt, for example, as tingling, burning, or stabbing sensations. Nerve pain often becomes chronic and can be disabling, and commonly develops in diabetes, lupus, shingles, complex regional pain syndromes, sciatica, phantom limb pain, MS, Parkinson's, post-stroke pain, and more.

Nerve pain is hard to alleviate with commonly used over-the-counter analgesics such as paracetamol or ibuprofen, or even morphine.

But a drug developed at Tel Aviv University – dubbed BL 7050 – offers new hope for people suffering with neuropathic pain.

According to the developers, Drs. Bernard Attali and Asher Peretz, working in the Sackler School of Medicine's Attali lab:

• BL 7050, delivered in pill form, has been demonstrated in pre-clinical animal trials to efficiently inhibit transmission of pain signals and epileptic seizures as well. It does this by avoiding nerve fiber hyperexcitement. While on the medication, rats experiencing both epilepsy and neuropathic pain were no longer affected by stimuli that had previously caused pain. Measures in the electrical activities of neurons also revealed that the medication was able to induce "calm" in the neurons, inhibiting pain pathways.

• BL 7050 has already been licensed for development & commercialization via Tel Aviv University’s technology transfer arm.

• And will move to clinical trials in humans “in the near future.”

The Quest to Stabilize Cellular Potassium Channels

As the researchers have reported in the journal PNAS as their work progressed, the medication works by targeting a group of proteins which act as channels or ‘pores’ in membranes of cells – allowing potassium to flow readily across the membrane. Understanding the  the mechanism that controls these potassium channels was crucial to development of the drug.

• Potassium has a crucial role in the excitability of cells, specifically those in the nervous system and the heart.

• When potassium channels don't function properly, cells are prone to hyper-excitability, leading to neurological and cardiovascular disorders such as epilepsy and arrhythmias.

• These are also the channels that convey pain signals caused by nerve or tissue damage, known as neuropathic pain.

• The researchers set out to develop a medication that could bind to and stabilize the body's potassium channels, controlling their hyper-excitability and preventing the occurrence of pain by keeping the channels open for the outflow of potassium.

• And, subject to upcoming phase one clinical trials, BL 7050 so far appears to fit the bill.

Source: Adapted from Friends of Tel Aviv University Press Release, Apr 30, 2012

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