Deans' stroke musings: Researchers Report Progress On Compound To Treat Neurological Diseases

Changing stroke rehab and research worldwide now.Time is Brain! trillions and trillions of neurons that DIE each day because there are NO effective hyperacute therapies besides tPA(only 12% effective). I have 523 posts on hyperacute therapy, enough for researchers to spend decades proving them out. These are my personal ideas and blog on stroke rehabilitation and stroke research. Do not attempt any of these without checking with your medical provider. Unless you join me in agitating, when you need these therapies they won't be there.

What this blog is for:

My blog is not to help survivors recover, it is to have the 10 million yearly stroke survivors light fires underneath their doctors, stroke hospitals and stroke researchers to get stroke solved. 100% recovery. The stroke medical world is completely failing at that goal, they don't even have it as a goal. Shortly after getting out of the hospital and getting NO information on the process or protocols of stroke rehabilitation and recovery I started searching on the internet and found that no other survivor received useful information. This is an attempt to cover all stroke rehabilitation information that should be readily available to survivors so they can talk with informed knowledge to their medical staff. It lays out what needs to be done to get stroke survivors closer to 100% recovery. It's quite disgusting that this information is not available from every stroke association and doctors group.

Monday, November 7, 2011

Researchers Report Progress On Compound To Treat Neurological Diseases

http://www.medicalnewstoday.com/releases/235716.php
Results of a study by a group of University of Notre Dame researchers represent a promising step on the road to developing new drugs for a variety of neurological diseases.

The group from the University's Departments of Chemistry and Biochemistry and Biological Sciences and the Friemann Life Sciences Center focused on the design, synthesis and evaluation of water-soluble "gelatinase inhibitor" compounds.

Gelatinases, a class of enzymes, have been implicated in a host of human diseases from cancer to cardiovascular conditions and in particular neurological conditions such as stroke, aneurysm and traumatic brain injury. Researchers have increasingly focused on developing potent gelatinase inhibitor drugs to treat acute gelatinase-dependent diseases.

The Notre Dame group has been investigating variants of a compound called "SB-3CT," which shows promise as a selective and potent gelatinase inhibitor. SB-3CT has exhibited potent efficacy in animal models for a variety of neurological and cancer diseases.

The preferred method of treatment for acute gelatinase-dependent diseases is intravenous infusion. Intravenous administration requires that the compound be water soluble. Unfortunately SB-3CT has poor water solubility and poor drug-like properties..

In a new approach, the Notre Dame researchers used a prodrug strategy to address this issue. A prodrug is an inactive precursor of a drug that is converted into its active form in the body by normal metabolic processes.

The prodrug strategy produced a greater than 5,000-fold increase in water solubility compared to SB-3CT. In addition to its high water solubility, the prodrug (referred to as ND-478) was chemically stable, non-toxic and was quickly converted to the active drug in the blood.. These favorable properties of ND-478 make it suitable for intravenous administration in the treatment of acute gelatinase-dependent diseases. Such a compound offers the possibility of translation into the clinic for treatment of strokes, aneurysms and traumatic brain injury.