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Media type:
E-Article
Title:
Translating a Low‐Molecular‐Weight MRI Probe Sensitive to Amino Acid Neurotransmitters into a PAMAM Dendrimer Conjugate: The Impact of Conjugation
Contributor:
Toljić, Đorđe;
Angelovski, Goran
Published:
Wiley, 2019
Published in:
ChemNanoMat, 5 (2019) 12, Seite 1456-1460
Description:
<jats:title>Abstract</jats:title><jats:p>A novel nano‐sized MRI probe sensitive to zwitterionic amino acid neurotransmitters (ZNTs) was prepared by the conjugation of bismacrocyclic ZNT‐responsive units to a generation 4 (G4) polyamidoamine (PAMAM) dendrimer. <jats:italic>In vitro</jats:italic> evaluation through <jats:sup>1</jats:sup>H NMR relaxometric titrations provided binding profiles revealing a surface morphology‐dependent interaction with the ZNTs. The positively charged dendrimeric periphery gave higher initial relaxivities and a milder decrease upon interaction with the target molecules. To improve solubility under physiologically relevant conditions, polyethylene glycol (PEG) units were additionally conjugated to the dendrimeric surface. The PEGylated conjugate displayed discrimination towards acetylcholine and a slightly increased binding affinity towards glutamate over the massively abundant competitive metabolite hydrogencarbonate.</jats:p>