The First Photochromic Affinity Switch for the Human Cannabinoid Receptor 2 (Adv. Therap. 1/2018)

Photopharmacology The human cannabinoid receptor type 2 plays a central role in the immune system. In article no. 1700032 Michael Decker and co‐workers report the development of photochromic affinity switches based on a drugable benzimidazole core through azologization and computational studies. Str...

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Bibliographic Details
Published in:Advanced therapeutics 2018-05, Vol.1 (1), p.n/a
Main Authors: Dolles, Dominik, Strasser, Andrea, Wittmann, Hans‐Joachim, Marinelli, Oliviero, Nabissi, Massimo, Pertwee, Roger G., Decker, Michael
Format: Article
Language:English
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Summary:Photopharmacology The human cannabinoid receptor type 2 plays a central role in the immune system. In article no. 1700032 Michael Decker and co‐workers report the development of photochromic affinity switches based on a drugable benzimidazole core through azologization and computational studies. Structureactivity relationships (SARs) lead to compounds with high selectivity over hCB1R that can be reversibly switched to a higher affinity cis‐form, proved on the receptor level by radioligand binding studies and translating into an affinity change in a functional GTPγS assay. cAMP ELISA and the change in expression level of two genes regulated by CREB proves that the compounds act as partial agonists.
ISSN:2366-3987
2366-3987
DOI:10.1002/adtp.201870003