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99mTc-labeled glimepiride as a tracer for targeting pancreatic β-cells mass: preparation and preclinical evaluation

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Abstract

Complexation of glimepiride with 99mTc, factors affecting yield and suitability of the 99mTc-glimepiride as a tracer for pancreatic β-cells mass were investigated. The radiocomplex showed maximum RCP of 98.2% and remained more than 90% stable up to 8 h in saline and serum. the complex structure and its binding to target sulphonyl urea receptor were assessed in silico. The 99mTc-glimepiride showed saturated in vitro binding with islet cells with a maximum uptake of 73%. Biodistribution and imaging studies suggested the feasibility of the tracer as a good candidate for specifically targeting β-cells mass in humans.

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Authors and Affiliations

  1. Labelled Compounds Department, Atomic Energy Authority, Cairo, 13759, Egypt

    O. A. El-Kawy

  2. Division of Pharmacology and Pharmacotherapy, Faculty of Pharmacy, University of Helsinki, 00014, Helsinki, Finland

    O. A. El-Kawy & J. A. García-Horsman

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  1. O. A. El-Kawy
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  2. J. A. García-Horsman
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Correspondence to O. A. El-Kawy.

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El-Kawy, O.A., García-Horsman, J.A. 99mTc-labeled glimepiride as a tracer for targeting pancreatic β-cells mass: preparation and preclinical evaluation. J Radioanal Nucl Chem 314, 2539–2550 (2017). https://doi.org/10.1007/s10967-017-5615-1

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