Wirth, Ulrike and Raabe, Konstantin and Kalaba, Predrag and Keimpema, Erik and Muttenthaler, Markus and Koenig, Burkhard (2023) Photoswitchable Probes of Oxytocin and Vasopressin. JOURNAL OF MEDICINAL CHEMISTRY, 66 (21). pp. 14853-14865. ISSN 0022-2623, 1520-4804
Full text not available from this repository. (Request a copy)Abstract
Oxytocin (OT) and vasopressin (VP) are related neuropeptides that regulate many biological processes. In humans, OT and VP act via four G protein-coupled receptors, OTR, V1aR, V1bR, and V2R (VPRs), which are associated with several disorders. To investigate the therapeutic potential of these receptors, particularly in the receptor-dense areas of the brain, molecular probes with a high temporal and spatial resolution are required. Such a spatiotemporal resolution can be achieved by incorporating photochromic moieties into OT and VP. Here, we report the design, synthesis, and (photo)pharmacological characterization of 12 OT- and VP-derived photoprobes using different modification strategies. Despite OT's and VP's sensitivity toward structural changes, we identified two photoprobes with good potency and photoswitch window for investigating the OTR and V1bR. These photoprobes should be of high value for producing cutting-edge photocontrollable peptide probes for the study of dynamic and kinetic receptor activation processes in specific regions of the brain.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | SOCIAL NEUROPEPTIDES; LINEAR ANTAGONISTS; OPTICAL CONTROL; BLOOD-PRESSURE; RESEARCH TOOLS; RECEPTOR; AGONISTS; BINDING; HOMEOSTASIS; RESPONSES; |
| 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: | 13 Mar 2024 13:15 |
| Last Modified: | 13 Mar 2024 13:15 |
| URI: | https://pred.uni-regensburg.de/id/eprint/59940 |
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