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Investigators from Chiba University Have Reported New Data on Medicinal Chemistry (Synthesis and evaluation of F-18-labeled mitiglinide derivatives...

July 14, 2014



Investigators from Chiba University Have Reported New Data on Medicinal Chemistry (Synthesis and evaluation of F-18-labeled mitiglinide derivatives as positron emission tomography tracers for beta-cell imaging)

By a News Reporter-Staff News Editor at Gastroenterology Week -- A new study on Health and Medicine is now available. According to news reporting from Chiba, Japan, by NewsRx journalists, research stated, "Measuring changes in beta-cell mass in vivo during progression of diabetes mellitus is important for understanding the pathogenesis, facilitating early diagnosis, and developing novel therapeutics for this disease. However, a non-invasive method has not been developed."

The news correspondents obtained a quote from the research from Chiba University, "A novel series of mitiglinide derivatives (o-FMIT, m-FMIT and p-FMIT; FMITs) were synthesized and their binding affinity for the sulfonylurea receptor 1 (SUR1) of pancreatic islets were evaluated by inhibition studies. (+)-(S)-o-FMIT had the highest affinity of our synthesized FMITs (IC50 = 1.8 mu M). (+)-(S)-o-[F-18]FMIT was obtained with radiochemical yield of 18% by radiofluorination of racemic precursor 7, hydrolysis, and optical resolution with chiral HPLC; its radiochemical purity was >99%. In biodistribution experiments using normal mice, (+)-(S)-o-[F-18]FMIT showed 1.94 +/- 0.42% ID/g of pancreatic uptake at 5 min p.i., and decreases in radioactivity in the liver (located close to the pancreas) was relatively rapid. Ex vivo autoradiography experiments using pancreatic sections confirmed accumulation of (+)-(S)-o-[F-18]FMIT in pancreatic beta-cells."

According to the news reporters, the research concluded: "These results suggest that (+)-(S)-o-[F-18]FMIT meets the basic requirements for an radiotracer, and could be a candidate positron emission tomography tracer for in vivo imaging of pancreatic beta-cells."

For more information on this research see: Synthesis and evaluation of F-18-labeled mitiglinide derivatives as positron emission tomography tracers for beta-cell imaging. Bioorganic & Medicinal Chemistry, 2014;22(13):3270-3278. Bioorganic & Medicinal Chemistry can be contacted at: Pergamon-Elsevier Science Ltd, The Boulevard, Langford Lane, Kidlington, Oxford OX5 1GB, England. (Elsevier - www.elsevier.com; Bioorganic & Medicinal Chemistry - www.elsevier.com/wps/product/cws_home/129)

Our news journalists report that additional information may be obtained by contacting H. Kimura, Chiba University, Grad Sch Med, Dept. of Med Physiol, Chuo Ku, Chiba 2608677, Japan. Additional authors for this research include H. Matsuda, H. Fujimoto, K. Arimitsu, K. Toyoda, E. Mukai, H. Nakamura, Y. Ogawa, M. Takagi, M. Ono, N. Inagaki and H. Saji (see also Health and Medicine).

Keywords for this news article include: Asia, Chiba, Japan, Pancreas, Gastroenterology, Health and Medicine

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2014, NewsRx LLC


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Source: Gastroenterology Week


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