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Photochromic Fentanyl Derivatives for Controlled μ-Opioid Receptor Activation.


ABSTRACT: Photoswitchable ligands as biological tools provide an opportunity to explore the kinetics and dynamics of the clinically relevant μ-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 μ-opioid receptor.

SUBMITTER: Lahmy R 

PROVIDER: S-EPMC9826449 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature

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Photochromic Fentanyl Derivatives for Controlled μ-Opioid Receptor Activation.

Lahmy Ranit R   Hübner Harald H   Schmidt Maximilian F MF   Lachmann Daniel D   Gmeiner Peter P   König Burkhard B  

Chemistry (Weinheim an der Bergstrasse, Germany) 20220912 63


Photoswitchable ligands as biological tools provide an opportunity to explore the kinetics and dynamics of the clinically relevant μ-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 cur  ...[more]

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