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Study Shows Leconotide, an Investigative Calcium Channel Blocker, Has Potential as a Selective, Efficacious, Non-Opioid Pain Treatment
Date:1/28/2009

ute of Medical Research studied 322 rodents in a model of induced diabetic neuropathy and hyperalgesia, or extreme sensitivity to pain. Roughly one-third of the rodents were given injections of two calcium channel blockers (leconotide or ziconotide) alone and in combination with flupirtine (a potassium channel opener). Roughly another third were given a range of doses up to the maximum that would not induce sedation. About half of the rodent's pain was reduced in the group with leconotide compared to less than 1 percent when ziconotide was given alone.

Leconotide in combination with flupirtine increased the reduction of pain, demonstrating selectivity -- it did not act on the channels that cause the side effects seen with ziconotide treatment.

Leconotide is derived from marine hunting cone snail Conus Catus.

About Calcium Channel Blockers

Every cell in the body is enclosed by a membrane which acts as a barrier controlling the flow of chemicals into and out of the cell. Channels through the membrane control the passage of substances into and out of the cell. Some are specialized for the flow of chemical ions such as sodium, potassium and calcium. The amount of ions of each species passing through those channels controls many functions of the cell such as force of contraction of a muscle cell in the heart or blood vessels or rate of electrical firing or production of chemical messengers in nerve cells. Calcium antagonists block calcium channels. There are many types of calcium channels. Medicines can be selective to bind just with one type (e.g. heart and blood vessels to lower blood pressure). Calcium channels in nerve cells are involved with many functions (e.g., pain, memory and control of consciousness). The goal is to find a calcium antagonist that only affects the channels involved with pain to cause pain relief without side effects like feeling sleepy.

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SOURCE American Academy of Pain Medicine
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