The First Photochromic Affinity Switch for the Human Cannabinoid Receptor 2
Dominik Dolles
1
,
Andrea Strasser
2
,
Hans-Joachim Wittmann
2
,
Oliviero Marinelli
3
,
Massimo Nabissi
3
,
Roger G. Pertwee
4
,
Publication type: Journal Article
Publication date: 2018-02-05
scimago Q1
wos Q3
SJR: 0.865
CiteScore: 6.6
Impact factor: 2.6
ISSN: 23663987
Medicine (miscellaneous)
Pharmacology
Pharmaceutical Science
Pharmacology (medical)
Genetics (clinical)
Biochemistry (medical)
Abstract
The hCB2R plays an important in the immune system and is centrally expressed in microglia. The hCB2R activated by agonists hold great therapeutic potential, e.g., in neuroinflammation. It is currently not yet elucidated how pathophysiological processes are mediated by the hCB2R. Here, photochromic affinity switches based on a drugable benzimidazole core through azologization and computational studies are developed. Structure‐activity 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.
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Metrics
25
Total citations:
25
Citations from 2024:
5
(20%)
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MLA
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GOST
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Dolles D. et al. The First Photochromic Affinity Switch for the Human Cannabinoid Receptor 2 // Advanced Therapeutics. 2018. Vol. 1. No. 1. p. 1700032.
GOST all authors (up to 50)
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Dolles D., Strasser A., Wittmann H., Marinelli O., Nabissi M., Pertwee R. G., Decker M. The First Photochromic Affinity Switch for the Human Cannabinoid Receptor 2 // Advanced Therapeutics. 2018. Vol. 1. No. 1. p. 1700032.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1002/adtp.201700032
UR - https://onlinelibrary.wiley.com/doi/10.1002/adtp.201700032
TI - The First Photochromic Affinity Switch for the Human Cannabinoid Receptor 2
T2 - Advanced Therapeutics
AU - Dolles, Dominik
AU - Strasser, Andrea
AU - Wittmann, Hans-Joachim
AU - Marinelli, Oliviero
AU - Nabissi, Massimo
AU - Pertwee, Roger G.
AU - Decker, Michael
PY - 2018
DA - 2018/02/05
PB - Wiley
SP - 1700032
IS - 1
VL - 1
SN - 2366-3987
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2018_Dolles,
author = {Dominik Dolles and Andrea Strasser and Hans-Joachim Wittmann and Oliviero Marinelli and Massimo Nabissi and Roger G. Pertwee and Michael Decker},
title = {The First Photochromic Affinity Switch for the Human Cannabinoid Receptor 2},
journal = {Advanced Therapeutics},
year = {2018},
volume = {1},
publisher = {Wiley},
month = {feb},
url = {https://onlinelibrary.wiley.com/doi/10.1002/adtp.201700032},
number = {1},
pages = {1700032},
doi = {10.1002/adtp.201700032}
}
Cite this
MLA
Copy
Dolles, Dominik, et al. “The First Photochromic Affinity Switch for the Human Cannabinoid Receptor 2.” Advanced Therapeutics, vol. 1, no. 1, Feb. 2018, p. 1700032. https://onlinelibrary.wiley.com/doi/10.1002/adtp.201700032.
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