Imaging against multiple sclerosis: Iodinated radiotracer candidate for PET and SPECT imaging

Feb 04, 2011

(PhysOrg.com) -- A first-line treatment for relapsing forms of multiple sclerosis (MS) was approved in September 2010 by the US Food and Drug Administration: FTY720 (fingolimod, Gilenya), which acts as a sphingosine 1-phosphate (S1P) receptor modulator.

There is preclinical evidence that in addition to decreasing infiltration of lymphocytes into the (CNS), FTY720 may provide additional neuroprotection through modulation of cerebral S1P receptors.

To further study the action of FTY720 in the CNS, Emmanuelle Briard, Yves Auberson, and colleagues at the Institutes for BioMedical Research in Basel (Switzerland) evaluated a series of iodinated FTY720 derivatives that could be used to study the drug's brain distribution in patients using nuclear imaging techniques, and their results are reported in ChemMedChem.

After extensive profiling, they identified 2-iodo-FTY720 (BZM055) as a close mimic of FTY720, having similar physicochemical properties and organ distribution, despite the addition of an iodine atom. They also showed that BZM055 is phosphorylated into its biologically active form at a similar rate to FTY720, retaining an affinity and selectivity for S1P receptors comparable to FTY720-phosphate, as well as similar brain penetration kinetics.

[123I]BZM055 is currently being developed as a SPECT tracer for studying the pharmacokinetics and distribution of FTY720 in the human . In addition, and since FTY720 has been shown to accumulate in myelin sheaths, this tracer might also prove useful to image myelin in MS patients.

Explore further: Conjecture on the lateral growth of Type I collagen fibrils

More information: Emmanuelle Briard, BZM055, an Iodinated Radiotracer Candidate for PET and SPECT Imaging of Myelin and FTY720 Brain Distribution, ChemMedChem, Permalink to the article: dx.doi.org/10.1002/cmdc.201000477

add to favorites email to friend print save as pdf

Related Stories

A biotherapy strategy for esophageal cancer in the future

Apr 19, 2010

A research team from China focused on esophageal squamous cell carcinoma (ESCC) and characterized sphingosine 1-phosphate (S1P) receptor expression pattern and investigated the role of S1P receptors on ESCC cells proliferation ...

Caffeine prevents multiple sclerosis-like disease in mice

Apr 07, 2008

Mice given caffeine equivalent to a human drinking six to eight cups of coffee a day were protected from developing experimental autoimmune encephalomyelitis (EAE), the animal model for the human disease Multiple Sclerosis ...

Recommended for you

Chemical biologists find new halogenation enzyme

6 hours ago

Molecules containing carbon-halogen bonds are produced naturally across all kingdoms of life and constitute a large family of natural products with a broad range of biological activities. The presence of halogen substituents ...

Protein secrets of Ebola virus

11 hours ago

The current Ebola virus outbreak in West Africa, which has claimed more than 2000 lives, has highlighted the need for a deeper understanding of the molecular biology of the virus that could be critical in ...

Protein courtship revealed through chemist's lens

12 hours ago

Staying clear of diseases requires that the proteins in our cells cooperate with one another. But, it has been a well-guarded secret how tens of thousands of different proteins find the correct dancing partners ...

Decoding 'sweet codes' that determine protein fates

14 hours ago

We often experience difficulties in identifying the accurate shape of dynamic and fluctuating objects. This is especially the case in the nanoscale world of biomolecules. The research group lead by Professor Koichi Kato of ...

Conjecture on the lateral growth of Type I collagen fibrils

Sep 12, 2014

Whatever the origin and condition of extraction of type I collagen ļ¬brils, in vitro as well as in vivo, the radii of their circular circular cross sections stay distributed in a range going from 50 to 100 nm for the most ...

User comments : 0