^99mTc-labeled glimepiride as a tracer for targeting pancreatic β-cells mass. Preparation and preclinical evaluation

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. (author)