PMID: 7581293Sep 1, 1995Paper

Synthesis of 5-HT3 receptor antagonists, [11C]Y-25130 and [11C]YM060

Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine
K IshiwataM Senda

Abstract

Two high-affinity 5-HT3 receptor ligands, Y-25130 and YM 060, have been labeled with 11C for use in PET studies to measure 5-HT3 receptors. The [11C]Y-25130 was prepared by N-methylation of nor-Y-25130-BH3 complex with [11C]CH3I in the presence of K2CO3 followed by HCl hydrolysis. Likewise, N-methylation of nor-YM060 gave [11C]YM060. After HPLC separation, the decay-corrected radiochemical yield of the two 11C-labeled ligands was 34-40% based on [11C]CH3I, the specific activity was 10-12 GBq/mumol at 35-40 min from EOB, and the radiochemical and chemical purities were > 99%. In mice, the brain uptake of the two compounds was the lowest among the tissues investigated, but the level of the brain radioactivity increased with time.

References

Apr 1, 1992·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·L BarréJ C Baron
Aug 1, 1992·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·M SakamoriM Setoguchi
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Apr 1, 1994·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·K IshiwataM Senda

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Citations

Apr 1, 1996·Nuclear Medicine and Biology·K IshiwataM Senda
Jun 16, 2011·Medicinal Research Reviews·Louise M PatersonGitte M Knudsen
Jul 29, 1998·Bioorganic & Medicinal Chemistry·T KatouninaL Barré

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