In-depth Study of a Novel Class of Ditopic Gadolinium(III)-based MRI Probes Sensitive to Zwitterionic Neurotransmitters.

ABSTRACT: The efficacy of Gd-based low-molecular weight ditopic MRI probes on binding zwitterionic neurotransmitters (ZNTs) relies on their structural compatibility. ZNTs are challenging biomarkers for monitoring chemical neurotransmission due to their intrinsic complexity as target molecules. In this work, we focus on tuning the cyclen- and azacrown ether-based binding sites properties to increase the affinity toward ZNTs. Our approach consisted in performing structural modifications on the binding sites in terms of charge and size, followed by the affinity evaluation through T ₁-weighted relaxometric titrations. We prepared and investigated six Gd³⁺ complexes with different structures and thus properties, which were found to be acetylcholine insensitive; moreover, two

SUBMITTER: Toljic Р

PROVIDER: S-EPMC6668053 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature