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Medicinal-Pharmaceutical Chemistry

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Radiochemistry

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Full-Text Articles in Chemistry

The Development Of Fluorine-18 Imaging Agents Targeting The Ghsr, Marina D. Childs Apr 2021

The Development Of Fluorine-18 Imaging Agents Targeting The Ghsr, Marina D. Childs

Electronic Thesis and Dissertation Repository

Molecular imaging is an interdisciplinary field of study that allows for real-time visualization of biological processes in both healthy and disease states. Fluorine-18 positron emission tomography (PET) imaging is a highly sensitive technique where molecular probes containing fluorine-18 serve to specifically locate and visualize the expression of relevant disease biomarkers. The growth hormone secretagogue receptor 1a (GHSR) is differentially expressed in cancer and cardiac pathology, making it a biomarker of interest for imaging such diseases. This thesis discusses the development and optimization of GHSR-targeting 18F-PET imaging probes as well as proposes a new imaging agent discovery technique.

Chapter 2 …


Development Of Single And Multimodality Imaging Probes For Pet, Spect And Fluorescence Imaging, Babak Behnam Azad Sep 2011

Development Of Single And Multimodality Imaging Probes For Pet, Spect And Fluorescence Imaging, Babak Behnam Azad

Electronic Thesis and Dissertation Repository

This dissertation is in an integrated format discussing three major projects centered around probe development. In the first project, novel metal-chelated and fluorinated GLP-1 derivatives were prepared all containing D-Ala-8, a modification known to improve resistance towards degradation by dipeptidyl-peptidase IV. The effect of increased distance between DOTA and the peptide chain was investigated using a spacer, in order to reduce steric effects imposed by DOTA. Placement of linker and DOTA moieties were varied within the GLP-1 sequence to test for optimal metal-complex location. Binding affinity of peptide derivatives was determined in vitro with CHO/GLP-1R cell line and shown to …