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

• Record Type: Journal Article
• Authors: Dolles, Dominik; Strasser, Andrea; Wittmann, Hans‐Joachim; Marinelli, Oliviero; Nabissi, Massimo; Pertwee, Roger G.; Decker, Michael
• Is Part Of: Advanced therapeutics. Volume 1:Issue 1(2018)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2018-05
• Subjects: Therapeutics -- Periodicals; Pharmaceutical technology -- Periodicals; Pharmacogenetics -- Periodicals; 615.5
• DOI: 10.1002/adtp.201870003
• Languages: English
• ISSNs: 2366-3987

Abstract

Abstract : 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.