Design, synthesis and pharmacological evaluation of novel fluorescent ligands for the mu-opioid receptor

There are increasing reports in the literature suggesting that the Mu-opioid receptor (MOR) is overexpressed in several human malignancies. This has led to the hypothesis that there is an association between peripheral MOR expression and tumour progression. Of particular concern is that MOR agonists are routinely used in cancer patients to control pain, through activation of central MORs, but also activate peripheral MORs (leading to undesirable effects). It is therefore important to investigate how different ligands influence tumour progression through interaction with peripheral and central opioid receptors. This project focuses on the design, synthesis and pharmacological characterisation of novel fluorescent opioid receptor ligands, as tools to investigate this phenomenon further.