Christine A. Hiller

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Dopaminergics of types 1 and 2 incorporating a conjugated enyne as an atypical catechol-simulating moiety were synthesized in enantiomerically pure form and investigated for their metabolic stability. Radioligand binding studies indicated high affinity to D2-like receptors. The test compounds were evaluated for their ability to differentially activate(More)
The development of biased (functionally selective) ligands provides a formidable challenge in medicinal chemistry. In an effort to learn to design functionally selective molecular tools for the highly therapeutically relevant dopamine D2 receptor, we synthesized a collection of agonists based on structurally distinct head groups derived from canonical or(More)
G protein-coupled receptors are involved in numerous physiological processes and provide attractive drug targets for diverse diseases. However, the development of selective, efficacious drugs targeting this family of membrane proteins remains challenging due to multidimensional selectivity profiles of GPCR-agonists and antagonists. Selective GPCR ligands(More)
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