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IUBMB Life ; 71(12): 2003-2009, 2019 12.
Article in English | MEDLINE | ID: mdl-31633875

ABSTRACT

The 99m Tc-DTPA (Technetium99m diethylenetriaminepentaacetic acid), is a radiopharmaceutical used in renal scintigraphy. The human serum albumin (HSA) binding site(s) for the 99m Tc-DTPA have never been characterized. This study will cover in vitro the binding rates of 99m Tc-DTPA on HSA and the 99m Tc-DTPA competition interactions with two drugs having known human serum albumin binding sites. Furosemide (FUR) and metformin (MET) were added to 99m Tc-DTPA solution (weight ratios 1/1 vol:vol) followed by the quantification of 99m Tc-DTPA binding rates to HSA (40 g/L) using equilibrium dialysis and the qualification of this binding using Molecular Modeling methods. The 99m Tc-DTPA binding rates to human serum albumin increased with the highest concentration. Both drugs FUR and MET displaced 99m Tc-DTPA binding. 99m Tc-DTPA could bind to human serum albumin in many locations in site I and I-II, but strongly bound to site I through hydrogen bonds.


Subject(s)
Furosemide/pharmacokinetics , Metformin/pharmacokinetics , Serum Albumin, Human/chemistry , Serum Albumin, Human/metabolism , Technetium Tc 99m Pentetate/metabolism , Binding, Competitive , Dialysis , Furosemide/chemistry , Humans , Hydrogen Bonding , Metformin/chemistry , Molecular Docking Simulation , Technetium Tc 99m Pentetate/chemistry
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