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99mTc-labeling of a dithiocarbamate-DWAY fragment using [99mTcN]2+ core for the preparation of potential 5HT1A receptor imaging agents

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Abstract

1-(2-methoxy phenyl) piperazine fragment of WAY100635 or its phenolic analogue, derived from DWAY is used to design the desired structure of 5HT1A receptor imaging agents. In this study a DWAY analogue was labeled with 99mTc-nitrido ([99mTcN]2+) core via dithiocarbamate. 2-(piperazin-1-yl) phenol dithiocarbamate was synthesized by the reaction of 2-(piperazin-1-yl) phenol with an equivalent amount of carbon disulfide in KOH solution then radiolabeled with 99mTc-nitrido core. The final complex was characterized by HPLC and its radiochemical purity was more than 90 %. In vitro stability studies have shown the complex was stable at least 4 h after labeling at room temperature. The n-octanol/water partition coefficient experiment demonstrated log p = 1.34 for 99mTcN–OHPP–DTC. Biodistribution results showed that radio tracer had moderate brain uptake (0.39 ± 0.03 %ID/g at 15 min and 0.29 ± 0.02 %ID/g at 120 min) and good retention, suggesting that this complex may lead to a further development of a radiotracer with specific binding to 5-HT1A receptor.

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Acknowledgments

The authors wish to thank Mr. Mirfallah and Mr. Talebi of the radioisotope department (AEOI) for providing sodium pertechnetate and assistance in quality control tests.

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Authors and Affiliations

  1. Nuclear Science Research School, Nuclear Science and Technology Research Institute (NSTRI), Atomic Energy Organization of Iran (AEOI), End of Karegar Ave., Tehran, Iran

    Mostafa Erfani & Mohammad Shafiei

  2. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

    Leila Hassanzadeh & Seyed Esmaeil Sadat Ebrahimi

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  1. Mostafa Erfani
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  2. Leila Hassanzadeh
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  3. Seyed Esmaeil Sadat Ebrahimi
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  4. Mohammad Shafiei
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Correspondence to Mostafa Erfani.

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Erfani, M., Hassanzadeh, L., Ebrahimi, S.E.S. et al. 99mTc-labeling of a dithiocarbamate-DWAY fragment using [99mTcN]2+ core for the preparation of potential 5HT1A receptor imaging agents. J Radioanal Nucl Chem 295, 1783–1788 (2013). https://doi.org/10.1007/s10967-012-2298-5

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  • DOI: https://doi.org/10.1007/s10967-012-2298-5

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