FRONT PAGE AMPYRA AUBAGIO AVONEX BETASERON COPAXONE EXTAVIA
Stan's Angels MS News Channel on YouTube GILENYA NOVANTRONE REBIF RITUXAN TECFIDERA TYSABRI
 Daily News for Neuros, Nurses & Savvy MSers: 208,152 Viewers, 8,368 Stories & Studies
Click Here For My Videos, Advice, Tips, Studies and Trials.
Timothy L. Vollmer, MD
Department of Neurology
University of Colorado Health Sciences Center Professor

Co-Director of the RMMSC at Anschutz Medical Center

Medical Director-Rocky Mountain MS Center
Click here to read my columns
Brian R. Apatoff, MD, PhD
Multiple Sclerosis Institute
Center for Neurological Disorders

Associate Professor Neurology and Neuroscience,

Weill Medical College of Cornell University

Clinical Attending in Neurology,
New York-Presbyterian Hospital
CLICK ON THE RED BUTTON BELOW
You'll get FREE Breaking News Alerts on new MS treatments as they are approved
MS NEWS ARCHIVES: by week

HERE'S A FEW OF OUR 6000+ Facebook & MySpace FRIENDS
Timothy L. Vollmer M.D.
Department of Neurology
University of Colorado Health Sciences Center
Co-Director of the RMMSC at Anschutz Medical Center
and
Medical Director-Rocky Mountain MS Center


Click to view 1280 MS Walk photos!

"MS Can Not
Rob You of Joy"
"I'm an M.D....my Mom has MS and we have a message for everyone."
- Jennifer Hartmark-Hill MD
Beverly Dean

"I've had MS for 2 years...this is the most important advice you'll ever hear."
"This is how I give myself a painless injection."
Heather Johnson

"A helpful tip for newly diagnosed MS patients."
"Important advice on choosing MS medication "
Joyce Moore


This page is powered by Blogger. Isn't yours?

Friday

 

Fluorinated 4-aminopyrdines as PET tracers for MS: STUDY




































Image source: GILENYANEWSCHANNEL

Abstract

Objectives:
Multiple sclerosis (MS) is a common neurological disease for which no PET tracers are available. Tracers are in development for inflammation (TSPO ligands) and myelin but no tracers exist for demyelinated axons, the hallmark of MS. Potassium (K+) channels in myelinated axons are normally located beneath the myelin sheath. During MS, myelin becomes damaged leaving these channels exposed. K+ channel blockers, such as 4-aminopyridine (4-AP), are used clinically to enhance axonal conduction and improve neurological function. Here, we explore the possibility that 4-AP analogs can be used to image demyelination. Our goals: - Show that 4-AP has higher uptake in demyelinated areas over myelinated areas in animal models of MS. - Develop fluorinated derivatives of 4-AP and routes to label these molecules with 18F. - Conduct PET imaging studies using [18F] 4-AP in rats and monkeys.

Methods:
[14C] 4-AP was administered to live demyelinated and control mice and the uptake in white matter was measured using autoradiography. - Fluorinated derivatives of 4-AP were synthesized and their binding affinity compared with 4-AP. - A route for 18F labeling of our lead compound was developed. - PET imaging studies in demyelinated rats and monkeys are ongoing.

Results:
4-AP and the fluorinated derivative 3-F-4-AP show significantly higher uptake in demyelinated areas over normally myelinated white matter. These molecules permit distinguishing demyelinated animals from controls using autoradiography. The SUV ratio in brain over blood for 3-F-4-AP 1h post injection is >2. A novel synthetic strategy for 18F labeling of 3-F-4-AP has been developed comprising aromatic nucleophilic substitution followed by reduction. We expect to have microPET results by June 2015.

Conclusions:
We have identified the first compound whose uptake increases upon demyelination, which is also brain permeable and metabolically stable. This compound is based on an approved drug for MS. This compound is a promising PET tracer for demyelinating conditions.

Story Source: The above story is based on materials provided by THEJOURNALOFNUCLEARMEDICINE
Note: Materials may be edited for content and length

Labels:



Go to Newer News Go to Older News