Photochromic Fentanyl Derivatives for Controlled mu-Opioid Receptor Activation

Lahmy, Ranit and Hübner, Harald and Schmidt, Maximilian F. and Lachmann, Daniel and Gmeiner, Peter and König, Burkhard (2022) Photochromic Fentanyl Derivatives for Controlled mu-Opioid Receptor Activation. CHEMISTRY-A EUROPEAN JOURNAL, 28 (63): e202201515. ISSN 0947-6539, 1521-3765

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Abstract

Photoswitchable ligands as biological tools provide an opportunity to explore the kinetics and dynamics of the clinically relevant mu-opioid receptor. These ligands can potentially activate or deactivate the receptor when desired by using light. Spatial and temporal control of biological activity allows for application in a diverse range of biological investigations. Photoswitchable ligands have been developed in this work, modelled on the known agonist fentanyl, with the aim of expanding the current "toolbox" of fentanyl photoswitchable ligands. In doing so, ligands have been developed that change geometry (isomerize) upon exposure to light, with varying photophysical and biochemical properties. This variation in properties could be valuable in further studying the functional significance of the mu-opioid receptor.

Item Type: Article
Uncontrolled Keywords: PROTEIN-COUPLED RECEPTORS; PHOTOSWITCHES; AGONIST; PHOTOPHARMACOLOGY; ARYLAZOPYRAZOLES; ISOMERIZATION; MECHANISMS; CHEMISTRY; DISCOVERY; TARGETS; arylazopyrazoles; fentanyl; mu-opioid receptor; G protein-coupled receptor; photopharmacology
Subjects: 500 Science > 540 Chemistry & allied sciences
Divisions: Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
Depositing User: Dr. Gernot Deinzer
Date Deposited: 08 Feb 2024 06:44
Last Modified: 08 Feb 2024 06:44
URI: https://pred.uni-regensburg.de/id/eprint/57369

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